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Genomes and Genes | Richard B RothmanSummaryAffiliation: National Institutes of Health Country: USA Publications
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Studies of the biogenic amine transporters. 14. Identification of low-efficacy "partial" substrates for the biogenic amine transportersRichard 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...
Dopamine/serotonin releasers as medications for stimulant addictionsRichard 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...- Dual dopamine/serotonin releasers as potential medications for stimulant and alcohol addictionsRichard 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... - Serotonin (5-HT) transporter ligands affect plasma 5-HT in ratsRichard 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... - Dual dopamine/serotonin releasers: potential treatment agents for stimulant addictionRichard 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... 
Salvinorin A: allosteric interactions at the mu-opioid receptorRichard 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...- Appetite suppressants, cardiac valve disease and combination pharmacotherapyRichard 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.... - Dual dopamine-5-HT releasers: potential treatment agents for cocaine addictionRichard 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.... - Studies of the biogenic amine transporters. 13. Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine releaseRichard 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... - Serotonergic drugs and valvular heart diseaseRichard 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... - Balance between dopamine and serotonin release modulates behavioral effects of amphetamine-type drugsRichard 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... - Altered gene expression in pulmonary tissue of tryptophan hydroxylase-1 knockout mice: implications for pulmonary arterial hypertensionRichard 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... - Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transportersHan 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... - 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)piperazineElisabeth 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... - Evidence for the involvement of dopamine transporters in behavioral stimulant effects of modafinilDorota 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... - 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 transporterBarbara 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... - Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agentsLing-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... - Differential effects of opioid agonists on G protein expression in CHO cells expressing cloned human opioid receptorsHeng 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.... - Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporterThomas 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)... - Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brainRichard 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... - A comparison of noninternalizing (herkinorin) and internalizing (DAMGO) mu-opioid agonists on cellular markers related to opioid tolerance and dependenceHeng 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... - Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivityElisabeth 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... - 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 transporterTerrence 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.... - Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphansYi 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... - Identification and characterization of a novel allosteric modulator (SoRI-6238) of the serotonin transporterAyon 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... - Identification of a novel "almost neutral" micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptorElliott 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... - Synthesis and pharmacological effects of the enantiomers of the N-phenethyl analogues of the ortho and para e- and f-oxide-bridged phenylmorphansJosef 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.... - High-dose fenfluramine administration decreases serotonin transporter binding, but not serotonin transporter protein levels, in rat forebrainRichard 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... - The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissueMichael 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... - 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 activityMalliga 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... - 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)-dimethylpiperaziIn 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... - Preclinical evaluation of GBR12909 decanoate as a long-acting medication for methamphetamine dependenceMichael 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... - 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... - 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 affinityFeng 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.... - Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary diseaseDorota 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... - 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 transporterDavid 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... - In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substratesRichard 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.... - 3,4-methylenedioxymethamphetamine (MDMA) administration to rats decreases brain tissue serotonin but not serotonin transporter protein and glial fibrillary acidic proteinXiaoying 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..Viewed collectively with our previous results and other published data, these data indicate that MDMA-induced persistent 5-HT depletion may occur in the absence of axotomy... - Evidence for a mu-delta opioid receptor complex in CHO cells co-expressing mu and delta opioid peptide receptorsJohn 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... - 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.... - Appetite suppressants as agonist substitution therapies for stimulant dependenceRichard 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... - (+/-)-3,4-Methylenedioxymethamphetamine administration to rats does not decrease levels of the serotonin transporter protein or alter its distribution between endosomes and the plasma membraneXiaoying 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.... - 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 phenylmorphansJin 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... - 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-pheLing-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... - Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-olsMalliga 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)... - Development of a rationally designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administrationRichard 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... - Studies of the biogenic amine transporters. 10. Characterization of a novel cocaine binding site in brain membranes prepared from dopamine transporter knockout miceRichard 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... - Substituted amphetamines that produce long-term serotonin depletion in rat brain ("neurotoxicity") do not decrease serotonin transporter protein expressionRichard 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... - 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-phenylethylmorphAnne 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.... - Evidence for noncompetitive modulation of substrate-induced serotonin releaseRichard 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... - 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)morphansKejun 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... - Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addictionRichard 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.... - In vivo effects of amphetamine analogs reveal evidence for serotonergic inhibition of mesolimbic dopamine transmission in the ratMichael 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... - Noradrenergic and dopaminergic effects of (+)-amphetamine-like stimulants in the baboon Papio anubisMohab 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... - 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 receptorHeng 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... - Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonistsSantosh 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... - Studies of the biogenic amine transporters. VIII: identification of a novel partial inhibitor of dopamine uptake and dopamine transporter bindingRichard 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... - Effects of "Legal X" piperazine analogs on dopamine and serotonin release in rat brainMichael 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... - Probes for narcotic receptor mediated phenomena. Part 28: new opioid antagonists from enantiomeric analogues of 5-(3-hydroxyphenyl)-N-phenylethylmorphanAkihiro 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... - 3,4-Methylenedioxymethamphetamine (MDMA) neurotoxicity in rats: a reappraisal of past and present findingsMichael 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... - Persistent antagonism of methamphetamine-induced dopamine release in rats pretreated with GBR12909 decanoateMichael 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... - Serotonergic responsiveness in human cocaine usersUdi 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... - Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a micro-agonist delta-antagonist and delta-inverse agonistsKejun 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... - (+)-Fenfluramine and its major metabolite, (+)-norfenfluramine, are potent substrates for norepinephrine transportersRichard 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... - Studies of the biogenic amine transporters. 12. Identification of novel partial inhibitors of amphetamine-induced dopamine releaseJoseph 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... - A critical structural determinant of opioid receptor interaction with phenolic 5-phenylmorphansIn 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.... - Serotonin releasing agents. Neurochemical, therapeutic and adverse effectsRichard 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... - Effects of dose and route of administration on pharmacokinetics of (+ or -)-3,4-methylenedioxymethamphetamine in the ratMichael 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... - Therapeutic potential of monoamine transporter substratesRichard 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... - Targeted screening for biogenic amine transporters: potential applications for natural productsRichard 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... - Monoamine transporters and psychostimulant drugsRichard 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... - Endogenous CART peptide regulates mu opioid and serotonin 5-HT(2A) receptorsRichard 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... - Locomotor stimulation produced by 3,4-methylenedioxymethamphetamine (MDMA) is correlated with dialysate levels of serotonin and dopamine in rat brainMichael 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... - Endogenous corticotropin releasing factor regulates adrenergic and opioid receptorsRichard 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... - Therapeutic and adverse actions of serotonin transporter substratesRichard 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... - 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]morphinansSubramaniam 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... - Synthesis of salvinorin A analogues as opioid receptor probesKevin 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... - Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analoguesDenise 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... - Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligandsWayne 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... - Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphansJames B Thomas
Chemistry and Life Sciences, Research Triangle Institute, Research Triangle Park, NC 27709, USA
J Med Chem 45:3524-30. 2002.... - Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-positionKenneth 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... - Depressive-like effects of the kappa-opioid receptor agonist salvinorin A on behavior and neurochemistry in ratsWilliam A Carlezon
Department of Psychiatry, McLean Hospital, MRC 217, 115 Mill Street, Belmont, MA 02478
J Pharmacol Exp Ther 316:440-7. 2006.... - 3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitroVincent 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... - 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 antagonistJames 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... - Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolinesSubramaniam 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... - Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ringWayne 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... - Antinociceptive and hypothermic effects of Salvinorin A are abolished in a novel strain of kappa-opioid receptor-1 knockout miceMichael 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...