David E Nichols

Summary

Affiliation: Purdue University
Country: USA

Publications

  1. ncbi request reprint 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists
    Thomas H McLean
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 1333, USA
    J Med Chem 49:5794-803. 2006
  2. ncbi request reprint Hallucinogens
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 2091, USA
    Pharmacol Ther 101:131-81. 2004
  3. ncbi request reprint Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands
    James J Chambers
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 1333, USA
    J Med Chem 46:3526-35. 2003
  4. ncbi request reprint C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor
    Thomas H McLean
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 1333, USA
    J Med Chem 49:4269-74. 2006
  5. ncbi request reprint Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity
    James J Chambers
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 1333, USA
    Bioorg Med Chem Lett 12:1997-9. 2002
  6. ncbi request reprint Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD)
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 45:4344-9. 2002
  7. ncbi request reprint trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist
    Juan Pablo Cueva
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 49:6848-57. 2006
  8. pmc High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 1333 Robert E Heine Pharmacy Building, West Lafayette, IN 47907, USA
    Bioorg Med Chem 16:6116-23. 2008
  9. doi request reprint Serotonin receptors
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47906 2091, USA
    Chem Rev 108:1614-41. 2008
  10. doi request reprint Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences RHPH, Purdue University, 575 Stadium Mall Dr, West Lafayette, IN 47907 2091, USA
    Psychopharmacology (Berl) 203:265-77. 2009

Collaborators

  • Charles Nichols
  • Sarah K Leonard
  • JON ERIC SPRAGUE
  • V J Watts
  • Raymond Booth
  • Bruce K Cassels
  • Harel Weinstein
  • ANITA LEWIN
  • Arthur Christopoulos
  • Bryan Roth
  • P M Sexton
  • Kenneth M Boy
  • Sing Yuen Sit
  • B Kobilka
  • Michael Nader
  • JONATHAN JAVITCH
  • F Ivy Carroll
  • Danuta Marona-Lewicka
  • Jason C Parrish
  • Benjamin R Chemel
  • Eric L Barker
  • James J Chambers
  • Deborah M Kurrasch-Orbaugh
  • Richard B Mailman
  • Michael R Braden
  • Alejandra Gallardo-Godoy
  • Thomas H McLean
  • Melissa I Torres-Altoro
  • Kellie J White
  • Jonathan D Urban
  • Russell A Grubbs
  • Elaine A Gay
  • Lisa A Bonner
  • Mechelle M Lewis
  • Julie A Przybyla
  • Danielle M Schultz
  • Matthew A Parker
  • Crystal C Walline
  • Matthew L Banks
  • Juan Pablo Cueva
  • J C Callaway
  • Jessica P Ryman-Rasmussen
  • Aaron Monte
  • Deborah Kurrasch-Orbaugh
  • Sandra L Hrometz
  • David L Roman
  • Amjad M Qandil
  • Erin M Falk
  • Michael S Whiteside
  • David M Mottola
  • Charles P Kuntz
  • Juan P Cueva
  • K Joseph Hsu
  • John D McCorvy
  • Julia A Chester
  • David J Riese
  • Jennifer A Prescher
  • Stephanie Kidd
  • Deborah M Kurrasch
  • David F Kisor
  • William P Clarke
  • Keith J Miller
  • Michael Spedding
  • Paul W Czoty
  • Mark von Zastrow
  • Kenneth W Tupper
  • Dennis J McKenna
  • Blaine Armbruster
  • Philip D Kiser
  • Charles S Grob
  • Gianfabio Giorgioni
  • Alexander Shulgin
  • Mariano Castillo
  • Angelica Fierro
  • Ronald A Thisted
  • Emily Gundy
  • Miguel Reyes-Parada
  • Amy K Jassen
  • Gerry S Oxford
  • Shannon N Saldana
  • Andrew W Brown
  • Connie Owens-Vance
  • Niels H Jensen
  • Amy Jassen
  • Jason D Kilts
  • Valerie J Cook
  • Q David Walker
  • Medhane G Cumbay
  • Monford Piercey
  • R Mark Wightman

Detail Information

Publications44

  1. ncbi request reprint 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists
    Thomas H McLean
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 1333, USA
    J Med Chem 49:5794-803. 2006
    ..If hallucinogenic effects are correlated with arachidonic acid production, such functionally selective 5-HT(2A) receptor agonists may lack the intoxicating properties of hallucinogens such as LSD...
  2. ncbi request reprint Hallucinogens
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 2091, USA
    Pharmacol Ther 101:131-81. 2004
    ..In addition, it appears entirely possible that utility may still emerge for the use of hallucinogens in treating alcoholism, substance abuse, and certain psychiatric disorders...
  3. ncbi request reprint Synthesis and pharmacological characterization of a series of geometrically constrained 5-HT(2A/2C) receptor ligands
    James J Chambers
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 1333, USA
    J Med Chem 46:3526-35. 2003
    ..Thus, although conformational constraint has led to high-affinity 5-HT(2A) ligands with partial agonist activity, all of the spatial and steric properties of the ligand necessary for full receptor activation have not yet been identified...
  4. ncbi request reprint C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor
    Thomas H McLean
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 1333, USA
    J Med Chem 49:4269-74. 2006
    ..Resolution of this analogue into its enantiomers corroborated the docking experiments, showing the R-(+) isomer to have higher affinity and potency and to have efficacy similar to that of mescaline at the 5-HT(2A) receptor...
  5. ncbi request reprint Translocation of the 5-alkoxy substituent of 2,5-dialkoxyarylalkylamines to the 6-position: effects on 5-HT(2A/2C) receptor affinity
    James J Chambers
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 1333, USA
    Bioorg Med Chem Lett 12:1997-9. 2002
    ....
  6. ncbi request reprint Lysergamides of isomeric 2,4-dimethylazetidines map the binding orientation of the diethylamide moiety in the potent hallucinogenic agent N,N-diethyllysergamide (LSD)
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    J Med Chem 45:4344-9. 2002
    ..The incorporation of isomeric dialkylazetidines into other biologically active molecules may be a useful strategy to model the active conformations of dialkylamines and dialkylamides...
  7. ncbi request reprint trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist
    Juan Pablo Cueva
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Med Chem 49:6848-57. 2006
    ..The binding and functional properties of this compound illustrate again the utility of constructing dopamine D1 agonist ligands around the beta-phenyldopamine pharmacophore template...
  8. pmc High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 1333 Robert E Heine Pharmacy Building, West Lafayette, IN 47907, USA
    Bioorg Med Chem 16:6116-23. 2008
    ..The new radioligand was suitable for labeling human 5-HT(2A) receptors in two heterologous cell lines and had about 20-fold higher affinity than [(3)H]ketanserin...
  9. doi request reprint Serotonin receptors
    David E Nichols
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47906 2091, USA
    Chem Rev 108:1614-41. 2008
  10. doi request reprint Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences RHPH, Purdue University, 575 Stadium Mall Dr, West Lafayette, IN 47907 2091, USA
    Psychopharmacology (Berl) 203:265-77. 2009
    ..Lysergic acid diethylamide (LSD) differs from other types of hallucinogens in that it possesses direct dopaminergic effects. The exact nature of this component has not been elucidated...
  11. ncbi request reprint Serotonin 5-hydroxytryptamine 2A receptor-coupled phospholipase C and phospholipase A2 signaling pathways have different receptor reserves
    Deborah M Kurrasch-Orbaugh
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacological Sciences, Purdue University, West Lafayette, Indiana 47907, USA
    J Pharmacol Exp Ther 304:229-37. 2003
    ..From these data we conclude that structurally distinct ligands can differentially regulate 5-HT 2A receptor signal transduction...
  12. ncbi request reprint Further evidence that the delayed temporal dopaminergic effects of LSD are mediated by a mechanism different than the first temporal phase of action
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, RHPH, 575 Stadium Mall Dr Purdue University, West Lafayette, IN 47907 2091, United States
    Pharmacol Biochem Behav 87:453-61. 2007
    ..The results reported here support and extend our previous conclusion that the delayed temporal effects of LSD are mediated by activation of a dopaminergic system...
  13. ncbi request reprint Distinct temporal phases in the behavioral pharmacology of LSD: dopamine D2 receptor-mediated effects in the rat and implications for psychosis
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, Heine Pharmacy Building, 575 Stadium Mall Dr, West Lafayette, IN 47907 2091, USA
    Psychopharmacology (Berl) 180:427-35. 2005
    ..The effect of LSD in humans has been described as occurring in two temporal phases. The behavioral effects in rats also occur in two temporal phases: an initial suppression of exploration followed by increased locomotor activity...
  14. ncbi request reprint Differential phospholipase C activation by phenylalkylamine serotonin 5-HT 2A receptor agonists
    Jason C Parrish
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 2091, USA
    J Neurochem 95:1575-84. 2005
    ....
  15. ncbi request reprint A complex signaling cascade links the serotonin2A receptor to phospholipase A2 activation: the involvement of MAP kinases
    Deborah M Kurrasch-Orbaugh
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana, USA
    J Neurochem 86:980-91. 2003
    ....
  16. ncbi request reprint Distinct molecular recognition of psychostimulants by human and Drosophila serotonin transporters
    David L Roman
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 2091, USA
    J Pharmacol Exp Ther 308:679-87. 2004
    ..For the substituted amphetamines, key areas for interaction exist around the amine, an electrostatic component surrounding the 3-position on the aromatic ring, and a steric component surrounding the 4-position...
  17. ncbi request reprint Synthesis and pharmacological evaluation of substituted naphth[1,2,3-de]isoquinolines (dinapsoline analogues) as D1 and D2 dopamine receptor ligands
    Amjad M Qandil
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    Bioorg Med Chem 11:1451-64. 2003
    ..Moreover, as rigid ligands in which small substituents can cause significant changes in selectivity, they are important tools for deriving 'differential' SARs of the dopamine receptor isoforms...
  18. pmc Comparison of the enantiomers of (+/-)-doxanthrine, a high efficacy full dopamine D(1) receptor agonist, and a reversal of enantioselectivity at D(1) versus alpha(2C) adrenergic receptors
    Julie A Przybyla
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA
    Eur Neuropsychopharmacol 19:138-46. 2009
    ..These findings demonstrate a reversed stereoselectivity for the enantiomers of DOX at D(1) and alpha(2C) receptors and have implications for the therapeutic utility of doxanthrine...
  19. ncbi request reprint WAY-100635 is a potent dopamine D4 receptor agonist
    Benjamin R Chemel
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907 2091, USA
    Psychopharmacology (Berl) 188:244-51. 2006
    ..Results from our studies suggested that WAY-100635 was potently inducing effects unrelated to its 5-HT1A receptor affinity. In the present work, we evaluated the in vitro pharmacology of this compound at two D2-like receptor subtypes...
  20. pmc 1-Methylpyridinium-4-(4-phenylmethanethiosulfonate) iodide, MTS-MPP+, a novel scanning cysteine accessibility method (SCAM) reagent for monoamine transporter studies
    Alejandra Gallardo-Godoy
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47906, USA
    Bioorg Med Chem 15:305-11. 2007
    ..Although it did not prove to be a substrate, as is MPP(+), it appears to label cysteine residues lining the permeation pore of the transporter more readily than currently available nonspecific SCAM reagents...
  21. pmc Structural analysis of the extracellular entrance to the serotonin transporter permeation pathway
    Melissa I Torres-Altoro
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University School of Pharmacy and Pharmaceutical Sciences, West Lafayette, Indiana 47907 2091, USA
    J Biol Chem 285:15369-79. 2010
    ..Our studies suggest that substrate and ligand binding may induce conformational shifts in TMH I and/or VI, providing new opportunities to refine existing homology models of SERT and related monoamine transporters...
  22. ncbi request reprint Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    Psychopharmacology (Berl) 164:93-107. 2002
    ....
  23. ncbi request reprint A homology-based model of the human 5-HT2A receptor derived from an in silico activated G-protein coupled receptor
    James J Chambers
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907 1333, USA
    J Comput Aided Mol Des 16:511-20. 2002
    ..The ligand/receptor complexes that ensued were refined and the final binding orientations were observed to be compatible with much of the data acquired through both diversified ligand design and site directed mutagenesis...
  24. pmc The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands
    Matthew A Parker
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47906, USA
    Bioorg Med Chem 16:4661-9. 2008
    ..The results suggest a possible method for distinguishing agonists from antagonists in high-throughput screening when a direct assay for functional activity is either unavailable or impractical...
  25. pmc Comparative molecular field analysis using selectivity fields reveals residues in the third transmembrane helix of the serotonin transporter associated with substrate and antagonist recognition
    Crystal C Walline
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, USA
    J Pharmacol Exp Ther 325:791-800. 2008
    ..A SERT homology model developed from the Aquifex aeolicus leucine transporter structure provides a structural context for further interpreting the results of the TMH III mutations...
  26. doi request reprint WAY 100635 produces discriminative stimulus effects in rats mediated by dopamine D(4) receptor activation
    Danuta Marona-Lewicka
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 47907 2091, USA
    Behav Pharmacol 20:114-8. 2009
    ..These results indicate that the discriminative stimulus effect produced by WAY 100635 is mediated by activation of dopamine D(4) receptors...
  27. pmc Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists
    Lisa A Bonner
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, United States
    Bioorg Med Chem 18:6763-70. 2010
    ..Importantly, we demonstrate that the 7,8-dihydroxy-5-phenyl-substituted ligand is an extremely potent, high-affinity, full D1 dopamine receptor-selective agonist...
  28. ncbi request reprint Serotonin 5-HT(2A) receptor activation induces 2-arachidonoylglycerol release through a phospholipase c-dependent mechanism
    Jason C Parrish
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, Indiana 4790, USA
    J Neurochem 99:1164-75. 2006
    ....
  29. ncbi request reprint 8,9-dihydroxy-1,2,3,11b-tetrahydrochromeno[4,3,2,-de]isoquinoline (dinoxyline), a high affinity and potent agonist at all dopamine receptor isoforms
    Russell A Grubbs
    Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA
    Bioorg Med Chem 12:1403-12. 2004
    ..These rigid ligands also will be useful tools to determine specific residues of the receptor transmembrane domains that are critical for agonist ligand selectivity for the D(4) receptor...
  30. ncbi request reprint Assessment of the roles of serines 5.43(239) and 5.46(242) for binding and potency of agonist ligands at the human serotonin 5-HT2A receptor
    Michael R Braden
    Dept of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, 575 Stadium Mall Drive, Purdue University, West Lafayette, IN 47907 2091, USA
    Mol Pharmacol 72:1200-9. 2007
    ..50, a strong interaction with Ser5.43(239) may be more effective in straightening the kink in helix 5, a feature that is possibly common to all type A GPCRs that have polar residues at position 5.43...
  31. pmc Engineered zinc-binding sites confirm proximity and orientation of transmembrane helices I and III in the human serotonin transporter
    Kellie J White
    Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University School of Pharmacy and Pharmaceutical Sciences, West Lafayette, Indiana 47907, USA
    Protein Sci 15:2411-22. 2006
    ..Homology modeling of the proposed Zn2+-binding sites using the coordinates of the Aquifex aeolicus leucine transporter structure provided a structural basis for interpreting the results and developing conclusions...
  32. ncbi request reprint Substituted hexahydrobenzodipyrans as 5-HT2A/2C receptor probes
    Michael S Whiteside
    Department of Chemistry, University of Wisconsin La Crosse, La Crosse, WI 54601, USA
    Bioorg Med Chem 10:3301-6. 2002
    ....
  33. pmc 'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines
    Danielle M Schultz
    Department of Chemistry, University of Wisconsin La Crosse, 1725 State Street, La Crosse, WI 54601, USA
    Bioorg Med Chem 16:6242-51. 2008
    ..In drug discrimination experiments using rats trained to discriminate LSD from saline, 4b was more than two times more potent than 5b, with the latter having a potency similar to the classic hallucinogenic amphetamine 1 (DOB)...
  34. ncbi request reprint Sulfur-substituted alpha-alkyl phenethylamines as selective and reversible MAO-A inhibitors: biological activities, CoMFA analysis, and active site modeling
    Alejandra Gallardo-Godoy
    Department of Chemistry, Faculty of Sciences, Universidad de Chile, Casilla 653, Santiago, Chile
    J Med Chem 48:2407-19. 2005
    ..On the basis of these results, structural determinants for selectivity of substituted amphetamines for MAO-A are discussed...
  35. ncbi request reprint An antisense oligonucleotide targeted at MAO-B attenuates rat striatal serotonergic neurotoxicity induced by MDMA
    Erin M Falk
    The Department of Pharmaceutical and Biomedical Sciences, The Raabe College of Pharmacy, Ohio Northern University, Ada 45810, USA
    Pharmacol Biochem Behav 72:617-22. 2002
    ..These results indicate that MAO-B plays an integral role in the development of MDMA-induced neurotoxicity while not affecting MDMA-induced hyperthermia or acute DA release...
  36. ncbi request reprint Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase
    David M Mottola
    Department of Psychiatry, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599 7160, USA
    J Pharmacol Exp Ther 301:1166-78. 2002
    ....
  37. ncbi request reprint Synthesis and SAR exploration of dinapsoline analogues
    Sing Yuen Sit
    Department of Neuroscience Drug Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492 7660, USA
    Bioorg Med Chem 12:715-34. 2004
    ..It was found that affinity for both D(1)and D(2) receptors was decreased by most substituents on the A, B', and C rings, whereas D ring substitutions preserved much of the dopamine receptor binding activity...
  38. ncbi request reprint A demand for clarity regarding a case report on the ingestion of 5-methoxy-N, N-dimethyltryptamine (5-MeO-DMT) in an Ayahuasca preparation
    J C Callaway
    J Anal Toxicol 30:406-7; author reply 407. 2006
  39. ncbi request reprint Functional selectivity and classical concepts of quantitative pharmacology
    Jonathan D Urban
    Curriculum in Toxicology, University of North Carolina School of Medicine, Chapel Hill, NC 27599 7160, USA
    J Pharmacol Exp Ther 320:1-13. 2007
    ..It also may be timely to revise classic concepts in quantitative pharmacology and relevant pharmacological conventions to incorporate these new concepts...
  40. ncbi request reprint Functional selectivity of D2 receptor ligands in a Chinese hamster ovary hD2L cell line: evidence for induction of ligand-specific receptor states
    Elaine A Gay
    Department of Psychiatry, University of North Carolina School of Medicine, Chapel Hill, NC 27599 7160, USA
    Mol Pharmacol 66:97-105. 2004
    ..We hypothesize that this functional selectivity may be a result of ligand induction of specific conformations of the D(2L) receptor that activate only selected signaling pathways...
  41. ncbi request reprint Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists
    Jessica P Ryman-Rasmussen
    Department of Psychiatry, University of North Carolina School of Medicine, Chapel Hill, NC 27599 7160, USA
    Mol Pharmacol 68:1039-48. 2005
    ..These data are consistent with the hypothesis that functional selectivity reflects subtle ligand-induced conformational changes as opposed to simple agonist trafficking among discrete receptor active states...
  42. ncbi request reprint 3,4-methylenedioxymethamphetamine (MDMA, ecstasy)-mediated production of hydrogen peroxide in an in vitro model: the role of dopamine, the serotonin-reuptake transporter, and monoamine oxidase-B
    Sandra L Hrometz
    The Department of Pharmaceutical and Biomedical Sciences, The Raabe College of Pharmacy, Ohio Northern University, Ada, OH 45810, USA
    Neurosci Lett 367:56-9. 2004
    ..These findings support the hypothesis that the deamination of DA by MAO-B within the serotonergic cell can lead to hydrogen peroxide formation and ultimately cell death...
  43. ncbi request reprint Ambient temperature effects on 3,4-methylenedioxymethamphetamine-induced thermodysregulation and pharmacokinetics in male monkeys
    Matthew L Banks
    Department of Physiology and Pharmacology, Wake Forest University School of Medicine, Winston Salem, NC, USA
    Drug Metab Dispos 35:1840-5. 2007
    ..Overall, induction of hypothermia in a cool environment by MDMA may alter its disposition. These results could have implications for MDMA-induced serotonergic consequences...
  44. ncbi request reprint Neurotoxicity of MDMA (ecstasy): beyond metabolism
    Jon E Sprague
    Trends Pharmacol Sci 26:59-60; author reply 60-1. 2005