Richard B Rothman

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. pmc Studies of the biogenic amine transporters. 14. Identification of low-efficacy "partial" substrates for the biogenic amine transporters
    Richard B Rothman
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, 333 Cassell Drive, Suite 4500, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 341:251-62. 2012
  2. ncbi request reprint Dual dopamine-5-HT releasers: potential treatment agents for cocaine addiction
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, PO Box 5180, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Trends Pharmacol Sci 27:612-8. 2006
  3. pmc Appetite suppressants, cardiac valve disease and combination pharmacotherapy
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institutes of Health, National Institute on Drug Abuse, Department of Health and Human Services, Baltimore, MD 21224, USA
    Am J Ther 16:354-64. 2009
  4. pmc Altered gene expression in pulmonary tissue of tryptophan hydroxylase-1 knockout mice: implications for pulmonary arterial hypertension
    Richard B Rothman
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland, United States of America
    PLoS ONE 6:e17735. 2011
  5. pmc Dual dopamine/serotonin releasers: potential treatment agents for stimulant addiction
    Richard B Rothman
    Clinical Psychopharmacology Section, IRP NIDA NIH, Clinical Psychopharmacology Section, Suite 4500, Triad building, 333 Cassell Drive, Baltimore, MD 21224, USA
    Exp Clin Psychopharmacol 16:458-74. 2008
  6. pmc Serotonergic drugs and valvular heart disease
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Expert Opin Drug Saf 8:317-29. 2009
  7. ncbi request reprint Dopamine/serotonin releasers as medications for stimulant addictions
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, MD, USA
    Prog Brain Res 172:385-406. 2008
  8. doi request reprint Serotonin (5-HT) transporter ligands affect plasma 5-HT in rats
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, Maryland, USA
    Ann N Y Acad Sci 1139:268-84. 2008
  9. ncbi request reprint Balance between dopamine and serotonin release modulates behavioral effects of amphetamine-type drugs
    Richard B Rothman
    CPS, IRP, NIDA, NIH, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Ann N Y Acad Sci 1074:245-60. 2006
  10. pmc Dual dopamine/serotonin releasers as potential medications for stimulant and alcohol addictions
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Baltimore, MD 21224, USA
    AAPS J 9:E1-10. 2007

Collaborators

Detail Information

Publications90

  1. pmc Studies of the biogenic amine transporters. 14. Identification of low-efficacy "partial" substrates for the biogenic amine transporters
    Richard B Rothman
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, 333 Cassell Drive, Suite 4500, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 341:251-62. 2012
    ..We speculate that partial biogenic amine transporter substrates bind to the transporter but are less effective in inducing conformational changes required for reverse transport activity...
  2. ncbi request reprint Dual dopamine-5-HT releasers: potential treatment agents for cocaine addiction
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, PO Box 5180, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Trends Pharmacol Sci 27:612-8. 2006
    ....
  3. pmc Appetite suppressants, cardiac valve disease and combination pharmacotherapy
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institutes of Health, National Institute on Drug Abuse, Department of Health and Human Services, Baltimore, MD 21224, USA
    Am J Ther 16:354-64. 2009
    ....
  4. pmc Altered gene expression in pulmonary tissue of tryptophan hydroxylase-1 knockout mice: implications for pulmonary arterial hypertension
    Richard B Rothman
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland, United States of America
    PLoS ONE 6:e17735. 2011
    ..These observations emphasize the intrinsic limitation of interpreting data from studies conducted in transgenic mice that are not fully characterized...
  5. pmc Dual dopamine/serotonin releasers: potential treatment agents for stimulant addiction
    Richard B Rothman
    Clinical Psychopharmacology Section, IRP NIDA NIH, Clinical Psychopharmacology Section, Suite 4500, Triad building, 333 Cassell Drive, Baltimore, MD 21224, USA
    Exp Clin Psychopharmacol 16:458-74. 2008
    ..It is concluded that DA/5-HT releasers could be useful therapeutic adjuncts for the treatment of cocaine and alcohol addictions, as well as for obesity, attention-deficit disorder, and depression...
  6. pmc Serotonergic drugs and valvular heart disease
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Expert Opin Drug Saf 8:317-29. 2009
    ..One prevailing hypothesis (i.e., the '5-HT hypothesis') suggests that fenfluramine-induced increases in plasma 5-HT underlie the disease...
  7. ncbi request reprint Dopamine/serotonin releasers as medications for stimulant addictions
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, MD, USA
    Prog Brain Res 172:385-406. 2008
    ..It is concluded that DA/5-HT releasers could be useful therapeutic adjuncts for the treatment of cocaine and alcohol addictions as well as for obesity, attention deficit disorder and depression...
  8. doi request reprint Serotonin (5-HT) transporter ligands affect plasma 5-HT in rats
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, Maryland, USA
    Ann N Y Acad Sci 1139:268-84. 2008
    ..Chronic fenfluramine and fluoxetine have minimal effects on plasma 5-HT, suggesting that the increased risk for IPAH associated with fenfluramine does not depend upon elevations in plasma 5-HT...
  9. ncbi request reprint Balance between dopamine and serotonin release modulates behavioral effects of amphetamine-type drugs
    Richard B Rothman
    CPS, IRP, NIDA, NIH, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Ann N Y Acad Sci 1074:245-60. 2006
    ..Moreover, the relationship between DA and 5-HT releasing potency is an important determinant in developing new agonist medications with reduced stimulant properties...
  10. pmc Dual dopamine/serotonin releasers as potential medications for stimulant and alcohol addictions
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Baltimore, MD 21224, USA
    AAPS J 9:E1-10. 2007
    ..It is concluded that DA/5-HT releasers might be useful therapeutic adjuncts for the treatment of cocaine and alcohol addiction, obesity, and even attention deficit disorder and depression...
  11. ncbi request reprint Salvinorin A: allosteric interactions at the mu-opioid receptor
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute of Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 320:801-10. 2007
    ..Viewed collectively, these data support the hypothesis that Salvinorin A allosterically modulates the mu-opioid receptor...
  12. pmc Studies of the biogenic amine transporters. 13. Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine release
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 329:718-28. 2009
    ..Such agents may have therapeutic potential for the treatment of stimulant addiction, Parkinson's disease, and other psychiatric disorders...
  13. ncbi request reprint Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine
    Elisabeth Greiner
    Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases NIDDK, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 46:1465-9. 2003
    ..Several analogues have been identified with high affinity for the DAT, up to 500-fold selectivity over the SERT and about 170-fold selectivity over the NET in binding and uptake inhibition assays...
  14. ncbi request reprint Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters
    Han Yu
    Laboratory of Medicinal Chemistry, Building 8, Room B1 23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland, 20892 0815, USA
    J Med Chem 47:2624-34. 2004
    ..Ex vivo autoradiography, however, demonstrated that iv administration of (-)-(1R,3S)-11 produced a dose-dependent, persistent occupation of 5-HT transporter binding sites but not DA transporter sites...
  15. pmc Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinil
    Dorota Zolkowska
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 329:738-46. 2009
    ..Nondopaminergic mechanisms may also contribute to the pharmacology of modafinil. Finally, the results suggest that modafinil should be tested as an adjunct for treating METH addiction...
  16. ncbi request reprint Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter
    Barbara Nightingale
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 314:906-15. 2005
    ..Viewed collectively, these results support the hypothesis that TB-1-099 allosterically modulates hSERT binding and function...
  17. pmc Differential effects of opioid agonists on G protein expression in CHO cells expressing cloned human opioid receptors
    Heng Xu
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, MD 21224, USA
    Brain Res Bull 77:49-54. 2008
    ....
  18. ncbi request reprint Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents
    Ling Wei Hsin
    Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
    Bioorg Med Chem Lett 13:553-6. 2003
    ..Compound (+)-11 showed high affinity and selectivity for DAT over the SERT and, therefore, is a potential candidate for the development of a long-acting cocaine abuse therapeutic agent...
  19. ncbi request reprint Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter
    Thomas Prisinzano
    Laboratory of Medicinal Chemistry, NIDDK, National Institutes of Health, Bethesda, MD 20892, USA
    J Med Chem 45:4371-4. 2002
    ..4-[2-[Bis(4-fluorophenyl)methoxy]ethyl-1-(2-naphthylmethyl)piperidine was found to possess subnanomolar affinity (K(i) = 0.7 nM) and good selectivity for the DAT (SERT/DAT = 323)...
  20. ncbi request reprint Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, NIDA, NIH, 5500 Nathan Shock Drive, 21224, Baltimore, MD, USA
    Eur J Pharmacol 447:51-7. 2002
    ..The collective findings suggest that phendimetrazine is a "prodrug" that is converted to the active metabolite phenmetrazine, a potent substrate for norepinephrine and dopamine transporters...
  21. pmc Identification of a novel "almost neutral" micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptor
    Elliott J Sally
    Clinical Psychopharmacology Section, IRP, NIDA, NIH, DHHS, Baltimore, Maryland 21224, USA
    Synapse 64:280-8. 2010
    ..LTC-274 is a promising lead compound for developing a true MOR neutral antagonist...
  22. pmc Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans
    Yi Zhang
    Department of Health and Human Services, Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, Maryland 20892 9415, USA
    J Med Chem 52:7570-9. 2009
    ..Structural features of the conformers of N-substituted benzofuro[2,3-c]pyridin-6-ols were compared to provide the rationale for their binding affinity...
  23. ncbi request reprint A comparison of noninternalizing (herkinorin) and internalizing (DAMGO) mu-opioid agonists on cellular markers related to opioid tolerance and dependence
    Heng Xu
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, Maryland 21224, USA
    Synapse 61:166-75. 2007
    ..Viewed collectively with published data, the current data indicate that both internalizing and noninternalizing mu-agonists produce cellular signs of tolerance and dependence...
  24. ncbi request reprint Identification and characterization of a novel allosteric modulator (SoRI-6238) of the serotonin transporter
    Ayon Nandi
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute of Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Synapse 53:176-83. 2004
    ..We conclude that SoRI-6238 partially inhibits SERT binding and function, most likely via an allosteric mechanism...
  25. ncbi request reprint Structure-activity relationships of substituted N-benzyl piperidines in the GBR series: Synthesis of 4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(2-trifluoromethylbenzyl)piperidine, an allosteric modulator of the serotonin transporter
    Terrence L Boos
    Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892, USA
    Bioorg Med Chem 14:3967-73. 2006
    ....
  26. ncbi request reprint Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity
    Elisabeth Greiner
    Laboratory of Medicinal Chemistry, NIDDK, National Institutes of Health, DHHS, Bethesda, Maryland 20892, USA
    J Med Chem 49:1766-72. 2006
    ..Some of the new ligands can serve as pharmacological tools to block DAT or DAT and another transporter simultaneously...
  27. ncbi request reprint High-dose fenfluramine administration decreases serotonin transporter binding, but not serotonin transporter protein levels, in rat forebrain
    Richard B Rothman
    Clinical Psychopharmacology Section, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Synapse 50:233-9. 2003
    ..These results support the hypothesis that decreases in tissue 5-HT and SERT binding sites induced by D-FEN and PCA reflect neuroadaptive changes, rather than neurotoxic effects...
  28. pmc Synthesis and pharmacological effects of the enantiomers of the N-phenethyl analogues of the ortho and para e- and f-oxide-bridged phenylmorphans
    Josef Zezula
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, National Institutes of Health, MD 20852, USA
    Org Biomol Chem 6:2868-83. 2008
    ....
  29. pmc Probes for narcotic receptor mediated phenomena. 47. Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols
    Malliga R Iyer
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892 9415, USA
    Bioorg Med Chem 21:3298-309. 2013
    ..Binding studies and functional assays revealed a moderately selective δ-antagonist (2l), selective μ-δ antagonists (3d, 3g), and a μ-κ antagonist (3f)...
  30. pmc Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity
    Malliga R Iyer
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, MD 20892 9415, USA
    Eur J Med Chem 50:44-54. 2012
    ..The modest change in spatial position of the hydroxyl moiety, and not the N-substituent, induced the change from potent agonist to an antagonist of moderate potency...
  31. pmc The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissue
    Michael H Baumann
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Neuropsychopharmacology 37:1192-203. 2012
    ..Given the widespread use of mephedrone and methylone, determining the consequences of repeated drug exposure warrants further study...
  32. ncbi request reprint N-substituted piperazines abused by humans mimic the molecular mechanism of 3,4-methylenedioxymethamphetamine (MDMA, or 'Ecstasy')
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Neuropsychopharmacology 30:550-60. 2005
    ..Our results show that BZP/TFMPP and MDMA share the ability to evoke monoamine release, but dangerous drug-drug synergism may occur when piperazines are coadministered at high doses...
  33. ncbi request reprint Preclinical evaluation of GBR12909 decanoate as a long-acting medication for methamphetamine dependence
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Ann N Y Acad Sci 965:92-108. 2002
    ..The findings suggest that GBR-decanoate, or similar long-acting agents, should be evaluated further as potential treatment adjuncts in the management of METH addiction in humans...
  34. pmc Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity
    Feng Li
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, MD 20892 9415, USA
    Bioorg Med Chem 19:4330-7. 2011
    ....
  35. ncbi request reprint Diaryldimethylpiperazine ligands with mu- and delta-opioid receptor affinity: Synthesis of (+)-4-[(alphaR)-alpha-(4-allyl-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide and (-)-4-[(alphaR)-alpha-(2S,5S)-dimethylpiperazi
    In Jong Kim
    Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
    Bioorg Med Chem 11:4761-8. 2003
    ..Those were established from the synthesis via a dipeptide cyclo-L-Ala-L-Ala in which the absolute stereochemistry was established...
  36. ncbi request reprint In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 307:138-45. 2003
    ....
  37. ncbi request reprint Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary disease
    Dorota Zolkowska
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 318:604-10. 2006
    ..Additional studies are needed to determine the effects of chronic administration of amphetamines on circulating 5-HT...
  38. ncbi request reprint 3,4-methylenedioxymethamphetamine (MDMA) administration to rats decreases brain tissue serotonin but not serotonin transporter protein and glial fibrillary acidic protein
    Xiaoying Wang
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Synapse 53:240-8. 2004
    ..In the present study, we studied the effect of MDMA and 5,7-dihydroxytryptamine (5,7-DHT) on tissue 5-HT levels and the protein expression level of SERT and glial fibrillary acidic protein (GFAP), a validated neurotoxicity marker...
  39. ncbi request reprint Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter
    David Lewis
    Laboratory of Medicinal Chemistry, NIDDK, NIH, Bethesda, MD 20892, USA
    Bioorg Med Chem Lett 13:1385-9. 2003
    ..Both trans- (43) and cis- (47) (+/-)-2-(4-[2-[bis-(4-fluorophenyl)-methoxy]ethyl]piperazin-1-ylmethyl)-6-methoxy-1,2,3,4-tetrahydronaphthalen-1-ol had relatively good SERT selectivity and, as well, showed high affinity for SERT...
  40. ncbi request reprint Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorph
    Anne Cécile Hiebel
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, National Institutes of Health, DHHS, Bethesda, MD 20892, USA
    J Med Chem 50:3765-76. 2007
    ....
  41. ncbi request reprint Development of a rationally designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administration
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 313:1361-9. 2005
    ..0 mg/kg/h. Collectively, the findings reported here demonstrate that nonamphetamine monoamine releasing agents such as PAL-287 might be promising candidate medications for the treatment of stimulant dependence...
  42. ncbi request reprint Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phe
    Ling Wei Hsin
    Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Med Chem 45:1321-9. 2002
    ..In accord with the in vitro data, 6 showed greater potency than 7 in elevating extracellular dopamine levels in a microdialysis assay and in inhibiting cocaine-maintained responding in rhesus monkeys...
  43. ncbi request reprint Appetite suppressants as agonist substitution therapies for stimulant dependence
    Richard B Rothman
    Clinical Psychopharmacology Section, NIDA, NIH, Baltimore, Maryland 21224, USA
    Ann N Y Acad Sci 965:109-26. 2002
    ..Future efforts should focus on developing new medications that possess the desired therapeutic activity but lack the adverse effects associated with older amphetamine-type anorectics...
  44. pmc Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans
    Jin Hee Kim
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892 9415, USA
    Bioorg Med Chem 19:3434-43. 2011
    ..1 nM) of all of the a- through f-oxide-bridged phenylmorphans. Functional data ([³⁵S]GTP-γ-S) showed that the racemate 12 was more than three times more potent than naloxone as an μ-opioid antagonist...
  45. pmc Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols
    Malliga R Iyer
    Drug Design and Synthesis Section, Department of Health and Human Services, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Room 4N03, Bethesda, MD 20892 9415, USA
    Bioorg Med Chem 18:91-9. 2010
    ..The N-para-fluorophenethyl derivative had the highest mu-opioid receptor affinity of the examined compounds (K(i)=0.35 microM)...
  46. pmc Probes for narcotic receptor mediated phenomena. 37. Synthesis and opioid binding affinity of the final pair of oxide-bridged phenylmorphans, the ortho- and para-b-isomers and their N-phenethyl analogues, and the synthesis of the N-phenethyl analogues of
    Muneaki Kurimura
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, Maryland 20892 9415, USA
    J Med Chem 51:7866-81. 2008
    ....
  47. ncbi request reprint (+/-)-3,4-Methylenedioxymethamphetamine administration to rats does not decrease levels of the serotonin transporter protein or alter its distribution between endosomes and the plasma membrane
    Xiaoying Wang
    Clinical Psychopharmacology Section, Intramural Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland, USA
    J Pharmacol Exp Ther 314:1002-12. 2005
    ....
  48. ncbi request reprint Evidence for a mu-delta opioid receptor complex in CHO cells co-expressing mu and delta opioid peptide receptors
    John M Rutherford
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, DHHS, Baltimore, MD 21224, USA
    Peptides 29:1424-31. 2008
    ..SUPERFIT-treated dimer cells may provide a useful model to study the properties of mu-delta heterodimers...
  49. ncbi request reprint Studies of the biogenic amine transporters. 10. Characterization of a novel cocaine binding site in brain membranes prepared from dopamine transporter knockout mice
    Richard B Rothman
    IRP, NIDA, NIH, Baltimore, Maryland 21224, USA
    Synapse 44:94-105. 2002
    ..Further progress in delineating the function of site "X" will depend on developing potent and selective agents for this site...
  50. pmc Evidence for noncompetitive modulation of substrate-induced serotonin release
    Richard B Rothman
    Clinical Psychopharmacology, IRP, NIDA, NIH, DHHS, Baltimore, Maryland, USA
    Synapse 64:862-9. 2010
    ..Viewed collectively, these findings suggest that it may be possible to design SERT inhibitors that differentially regulate SERT function...
  51. ncbi request reprint Substituted amphetamines that produce long-term serotonin depletion in rat brain ("neurotoxicity") do not decrease serotonin transporter protein expression
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Ann N Y Acad Sci 1025:151-61. 2004
    ..These results support the hypothesis that D-FEN- and PCA-induced decreases in tissue 5-HT and SERT binding sites reflect neuroadaptive changes rather than neurotoxic effects...
  52. pmc Probes for narcotic receptor mediated phenomena. 48. C7- and C8-substituted 5-phenylmorphan opioids from diastereoselective alkylation
    Hwan Jung Lim
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, MD 20892 9415, USA
    Eur J Med Chem 67:335-43. 2013
    ..Unexpectedly, the N-methyl substituted compounds generally had higher affinity than comparable N-phenethyl-substituted relatives. The configurations of two compounds were determined by single-crystal X-ray crystallographic analyses. ..
  53. pmc Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans
    Kejun Cheng
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, Maryland 20892 9415, United States
    J Med Chem 54:957-69. 2011
    ..By comparison of the geometry-optimized structures of the newly synthesized compounds, an attempt was made to rationalize their μ-opioid receptor affinity in terms of the spatial position of N-substituents...
  54. ncbi request reprint Opioid peptide receptor studies. 17. Attenuation of chronic morphine effects after antisense oligodeoxynucleotide knock-down of RGS9 protein in cells expressing the cloned Mu opioid receptor
    Heng Xu
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Synapse 52:209-17. 2004
    ..These results provide additional evidence for involvement of RGS9 protein in modulating opioid signaling, which may contribute to the development of morphine tolerance and dependence...
  55. pmc In vivo effects of amphetamine analogs reveal evidence for serotonergic inhibition of mesolimbic dopamine transmission in the rat
    Michael H Baumann
    Translational Pharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    J Pharmacol Exp Ther 337:218-25. 2011
    ..029). Collectively, our findings are consistent with the hypothesis that 5-HT release dampens stimulant effects of amphetamine-type drugs, but further studies are required to address the precise mechanisms underlying this phenomenon...
  56. ncbi request reprint Noradrenergic and dopaminergic effects of (+)-amphetamine-like stimulants in the baboon Papio anubis
    Mohab Alexander
    Division of Nuclear Medicine, Russell H Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287, USA
    Synapse 56:94-9. 2005
    ..Viewed collectively, the present data indicate that typical clinical doses of phentermine and (+/-)-ephedrine may not release central DA in humans, a hypothesis that should ultimately be tested in controlled clinical studies...
  57. pmc Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction
    Richard B Rothman
    Clinical Psychopharmacology Section, National Institute on Drug Abuse, Intramural Research Program, National Institutes of Health, 333 Cassell Dr, Baltimore, MD 21224, USA
    Biochem Pharmacol 75:2-16. 2008
    ....
  58. ncbi request reprint Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists
    Santosh S Kulkarni
    Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Bioorg Med Chem Lett 16:3371-5. 2006
    ..Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro...
  59. pmc Probes for narcotic receptor mediated phenomena. 46. N-substituted-2,3,4,9,10,10a-hexahydro-1H-1,4a-(epiminoethano)phenanthren-6- and 8-ols - carbocyclic relatives of f-oxide-bridged phenylmorphans
    Fuying Li
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, and the National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Department of Health and Human Services, 5625 Fishers Lane, Room 4N03, Bethesda, MD 20892 9415, USA
    Eur J Med Chem 58:557-67. 2012
    ..They were also much more potent μ-antagonists, with activities comparable to naltrexone in the [(35)S]GTP-γ-S assay...
  60. ncbi request reprint Studies of the biogenic amine transporters. VIII: identification of a novel partial inhibitor of dopamine uptake and dopamine transporter binding
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Synapse 43:268-74. 2002
    ..Further studies will be needed to determine the underlying mechanism of this effect and if partial inhibition of DA uptake results in any unique behavioral effects...
  61. ncbi request reprint Probes for narcotic receptor mediated phenomena. Part 28: new opioid antagonists from enantiomeric analogues of 5-(3-hydroxyphenyl)-N-phenylethylmorphan
    Akihiro Hashimoto
    Laboratory of Medicinal Chemistry, Building 8, Room B1 23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892 0815, USA
    Bioorg Med Chem 10:3319-29. 2002
    ..3.1]non-5-yl]-phenol (30), and both showed the same 1H NMR spectrum, the structure of 32 was unequivocally determined by X-ray structure analysis...
  62. ncbi request reprint Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a micro-agonist delta-antagonist and delta-inverse agonists
    Kejun Cheng
    Drug Design and Synthesis Section, Chemical Biology Research Branch, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 0815, USA
    Org Biomol Chem 5:1177-90. 2007
    ..The absolute configuration of all of the reported compounds was established by chemical conversion of (-)- to 1R,5S-(-)-.HBr...
  63. ncbi request reprint Effects of "Legal X" piperazine analogs on dopamine and serotonin release in rat brain
    Michael H Baumann
    Clinical Psychopharmacology Section, IRP, NIDA, National Institutes of Health, Baltimore, Maryland 21224, USA
    Ann N Y Acad Sci 1025:189-97. 2004
    ..Additionally, the findings suggest possible drug-drug synergism when piperazine drugs are coadministered at high doses...
  64. pmc 3,4-Methylenedioxymethamphetamine (MDMA) neurotoxicity in rats: a reappraisal of past and present findings
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program IRP, National Institute on Drug Abuse NIDA, National Institutes of Health NIH, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Psychopharmacology (Berl) 189:407-24. 2007
    ..g., depletion of forebrain 5-HT) that have been interpreted as neurotoxicity. Whether such 5-HT deficits reflect neuronal damage is a matter of ongoing debate...
  65. ncbi request reprint Persistent antagonism of methamphetamine-induced dopamine release in rats pretreated with GBR12909 decanoate
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 301:1190-7. 2002
    ..Our data suggest that GBR-decanoate, or similar agents, may be useful adjuncts in treating methamphetamine dependence. This therapeutic strategy would be especially useful for noncompliant patient populations...
  66. ncbi request reprint Serotonergic responsiveness in human cocaine users
    Udi E Ghitza
    Clinical Pharmacology and Therapeutics Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Drug Alcohol Depend 86:207-13. 2007
    ..Studies of human cocaine users given a serotonergic challenge have produced inconsistent results...
  67. ncbi request reprint A critical structural determinant of opioid receptor interaction with phenolic 5-phenylmorphans
    In Jong Kim
    Laboratory of Medicinal Chemistry, Building 8, Room B1 23, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Department of Health and Human Services, Bethesda, MD 20892 0815, USA
    Bioorg Med Chem 12:4543-50. 2004
    ....
  68. pmc Studies of the biogenic amine transporters. 12. Identification of novel partial inhibitors of amphetamine-induced dopamine release
    Joseph J Pariser
    National Institute on Drug Abuse, National Institutes of Health, Clinical Psychopharmacology Section, 333 Cassell Dr, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 326:286-95. 2008
    ..Viewed collectively, we report several compounds that allosterically modulate hDAT binding and function, and we identify novel partial inhibitors of amphetamine-induced dopamine release...
  69. ncbi request reprint (+)-Fenfluramine and its major metabolite, (+)-norfenfluramine, are potent substrates for norepinephrine transporters
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Dr, P O Box 5180, Baltimore, MD 21224, USA
    J Pharmacol Exp Ther 305:1191-9. 2003
    ..Release of NE and DA evoked by (+)-norfenfluramine is at least partly mediated via NE transporters. Our results emphasize the potential involvement of noradrenergic mechanisms in the actions of fenfluramines...
  70. ncbi request reprint Serotonin releasing agents. Neurochemical, therapeutic and adverse effects
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, P O Box 5180, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Pharmacol Biochem Behav 71:825-36. 2002
    ..Viewed collectively, it seems possible to develop new medications that selectively release 5-HT without the adverse effects of PPH, VHD or neurotoxicity. Such agents may have utility in treating a variety of psychiatric disorders...
  71. ncbi request reprint Endogenous CART peptide regulates mu opioid and serotonin 5-HT(2A) receptors
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, PO Box 5180, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Peptides 24:413-7. 2003
    ..The results demonstrated that anti-CART peptide IgG up-regulates mu and 5-HT(2A) receptor in the hippocampus and caudate We conclude that CART peptides in the cerebrospinal fluid may exert regulatory effects in the brain...
  72. pmc Effects of dose and route of administration on pharmacokinetics of (+ or -)-3,4-methylenedioxymethamphetamine in the rat
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 333 Cassell Dr, Suite 4500, Baltimore, MD 21224, USA
    Drug Metab Dispos 37:2163-70. 2009
    ..Finally, given key similarities between MDMA pharmacokinetics in rats and humans, data from rats may be clinically relevant when appropriate dosing conditions are used...
  73. ncbi request reprint Endogenous corticotropin releasing factor regulates adrenergic and opioid receptors
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, USA
    Peptides 23:2177-80. 2002
    ..The results demonstrated that anti-CRF IgG upregulates mu and beta-adrenergic receptors. We conclude that CRF in the cerebrospinal fluid may exert regulatory effects throughout the brain...
  74. ncbi request reprint Therapeutic and adverse actions of serotonin transporter substrates
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, P O Box 5180, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Pharmacol Ther 95:73-88. 2002
    ..Such agents may be useful for treating a variety of psychiatric disorders...
  75. ncbi request reprint Monoamine transporters and psychostimulant drugs
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, PO Box 5180, Baltimore, MD 21224, USA
    Eur J Pharmacol 479:23-40. 2003
    ..Future medications discovery efforts should focus on identifying new compounds which possess the equipotent substrate activity at DAT and SERT, but which lack the adverse effects of stimulants developed decades ago...
  76. pmc Locomotor stimulation produced by 3,4-methylenedioxymethamphetamine (MDMA) is correlated with dialysate levels of serotonin and dopamine in rat brain
    Michael H Baumann
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, MD 21224, United States
    Pharmacol Biochem Behav 90:208-17. 2008
    ..0001) and with dialysate DA in accumbens and striatum (P<0.001-0.0001). These data support previous work and suggest the complex spectrum of behaviors produced by MDMA involves 5-HT and DA in a region- and modality-specific manner...
  77. ncbi request reprint Targeted screening for biogenic amine transporters: potential applications for natural products
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, NIDA, NIH, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Life Sci 78:512-8. 2005
    ..The potential application of these methods to characterizing natural products will be discussed in reference to results obtained with "purified" natural products, such as ephedrine stereoisomers...
  78. ncbi request reprint Therapeutic potential of monoamine transporter substrates
    Richard B Rothman
    Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA
    Curr Top Med Chem 6:1845-59. 2006
    ..g., fenfluramine) and DA releasers (e.g., amphetamine). Our findings demonstrate the feasibility of developing non-amphetamine releasing agents as potential treatments for substance abuse disorders and other psychiatric conditions...
  79. ncbi request reprint Depressive-like effects of the kappa-opioid receptor agonist salvinorin A on behavior and neurochemistry in rats
    William A Carlezon
    Department of Psychiatry, McLean Hospital, MRC 217, 115 Mill Street, Belmont, MA 02478
    J Pharmacol Exp Ther 316:440-7. 2006
    ....
  80. ncbi request reprint Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines
    Subramaniam Ananthan
    Organic Chemistry Department, Southern Research Institute, Birmingham, AL 35255, USA
    Bioorg Med Chem Lett 12:2225-8. 2002
    ..Among the compounds studied, 4-[(diphenylmethyl)amino]-2-phenylquinazoline (4 g) was identified as a novel partial inhibitor of [(125)I]RTI-55 binding to the dopamine transporter and a partial inhibitor of [(3)H]dopamine uptake...
  81. ncbi request reprint Synthesis of salvinorin A analogues as opioid receptor probes
    Kevin Tidgewell
    Division of Medicinal and Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA
    J Nat Prod 69:914-8. 2006
    ..Here, we report the semisynthesis of neoclerodane diterpenes and their structure-affinity relationships at opioid receptors. This work will allow the further development of novel opioid receptor ligands...
  82. ncbi request reprint Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues
    Denise S Simpson
    Division of Medicinal and Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA
    J Med Chem 50:3596-603. 2007
    ..This indicates that additional structural modifications of 1a may lead to analogues with higher potency and utility as drug abuse medications...
  83. ncbi request reprint Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring
    Wayne W Harding
    Division of Medicinal and Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, IA 52242, USA
    Bioorg Med Chem Lett 16:3170-4. 2006
    ..In addition, a procedure has been found to remove the furan skeleton completely. Biological results indicate that replacement of the furan ring with an N-sulfonylpyrrole leads to reduced affinity and efficacy at kappa opioid receptors...
  84. pmc Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position
    Kenneth G Holden
    Holden Laboratories, Carmel, CA 93923, USA
    Bioorg Med Chem Lett 17:6111-5. 2007
    ..These observations suggest that the ketone of 2b is a key structural feature responsible for mu agonist activity...
  85. ncbi request reprint Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands
    Wayne W Harding
    Division of Medicinal and Natural Products Chemistry, College of Pharmacy, The University of Iowa, Iowa City, Iowa 52242, USA
    J Med Chem 48:4765-71. 2005
    ..This represents the identification of a novel structural class of mu opioid receptor agonists...
  86. ncbi request reprint Antinociceptive and hypothermic effects of Salvinorin A are abolished in a novel strain of kappa-opioid receptor-1 knockout mice
    Michael A Ansonoff
    Department of Neuroscience and Cell Biology, University of Medicine and Dentistry of New Jersey Robert Wood Johnson Medical School UMDNJ RWJMS, 675 Hoes Lane, Piscataway, NJ 08854, USA
    J Pharmacol Exp Ther 318:641-8. 2006
    ..divinorum, selective for kappa(1)-opioid receptors, and that salvinorin A and specific structurally related analogs produce behavioral effects that require the kappa-opioid receptor...
  87. ncbi request reprint Novel ligands for the opioid receptors: synthesis and structure-activity relationships among 5'-aryl and 5'-heteroaryl 17-cyclopropylmethyl-4,5 alpha-epoxypyrido[2',3':6,7]morphinans
    Subramaniam Ananthan
    Organic Chemistry Department, Southern Research Institute, Birmingham, AL 35255, USA
    Bioorg Med Chem 11:4143-54. 2003
    ..The in vitro delta antagonist profile of this pyridomorphinan 10c resembles that of the widely used delta selective antagonist ligand naltrindole...
  88. ncbi request reprint Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist
    James B Thomas
    Chemistry and Life Sciences, Research Triangle Institute, 3040 Cornwallis Road, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 46:3127-37. 2003
    ..The unique structural features of JDTic will make this compound highly useful in further characterization of the kappa receptor...
  89. ncbi request reprint 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro
    Vincent Setola
    Department of Biochemistry, Case Western Reserve University, 2109 Adelbert Road, Cleveland, OH 44106 4935, USA
    Mol Pharmacol 63:1223-9. 2003
    ..These findings also underscore the necessity of screening current and future drugs at h5-HT2B receptors for agonist actions before their use in humans...
  90. ncbi request reprint Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans
    James B Thomas
    Chemistry and Life Sciences, Research Triangle Institute, Research Triangle Park, NC 27709, USA
    J Med Chem 45:3524-30. 2002
    ....