Ethan S Burstein

Summary

Affiliation: ACADIA Pharmaceuticals
Country: USA

Publications

  1. ncbi request reprint Integrative functional assays, chemical genomics and high throughput screening: harnessing signal transduction pathways to a common HTS readout
    Ethan S Burstein
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    Curr Pharm Des 12:1717-29. 2006
  2. pmc Characterization of the Mas-related gene family: structural and functional conservation of human and rhesus MrgX receptors
    Ethan S Burstein
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Boulevard, San Diego, CA 92121, U S A
    Br J Pharmacol 147:73-82. 2006
  3. ncbi request reprint Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist
    E S Burstein
    ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 315:1278-87. 2005
  4. doi request reprint II. In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors
    Ethan S Burstein
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Neural Transm 118:1523-33. 2011
  5. doi request reprint AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model
    Stefania Risso Bradley
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92129, USA
    Neuropharmacology 58:365-73. 2010
  6. doi request reprint Discovery of potential antipsychotic agents possessing pro-cognitive properties
    Jelveh Lameh
    ACADIA Pharmaceuticals, Inc, San Diego, CA 92121, USA
    Naunyn Schmiedebergs Arch Pharmacol 385:313-23. 2012
  7. ncbi request reprint Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist
    Kimberly E Vanover
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 317:910-8. 2006
  8. ncbi request reprint Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Boulevard, San Diego, CA 92121, USA
    Mol Pharmacol 70:1974-83. 2006
  9. ncbi request reprint Identification of the atypical L-type Ca2+ channel blocker diltiazem and its metabolites as ghrelin receptor agonists
    Jian Nong Ma
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    Mol Pharmacol 72:380-6. 2007
  10. ncbi request reprint Discovery of novel peptide/receptor interactions: identification of PHM-27 as a potent agonist of the human calcitonin receptor
    Jian Nong Ma
    ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92130, USA
    Biochem Pharmacol 67:1279-84. 2004

Collaborators

Detail Information

Publications32

  1. ncbi request reprint Integrative functional assays, chemical genomics and high throughput screening: harnessing signal transduction pathways to a common HTS readout
    Ethan S Burstein
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    Curr Pharm Des 12:1717-29. 2006
    ..Here we review strategies for building homogeneous assay platforms across large gene families by redirecting and/or amplifying signal transduction pathways...
  2. pmc Characterization of the Mas-related gene family: structural and functional conservation of human and rhesus MrgX receptors
    Ethan S Burstein
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Boulevard, San Diego, CA 92121, U S A
    Br J Pharmacol 147:73-82. 2006
    ..These data suggest that the rhesus monkey may be a suitable animal model for exploring the physiological roles of the MrgX receptors...
  3. ncbi request reprint Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist
    E S Burstein
    ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 315:1278-87. 2005
    ....
  4. doi request reprint II. In vitro evidence that (-)-OSU6162 and (+)-OSU6162 produce their behavioral effects through 5-HT2A serotonin and D2 dopamine receptors
    Ethan S Burstein
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Neural Transm 118:1523-33. 2011
    ..Compounds with balanced effects on these two receptor systems may offer promise for treating neuropsychiatric diseases...
  5. doi request reprint AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model
    Stefania Risso Bradley
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92129, USA
    Neuropharmacology 58:365-73. 2010
    ..Therefore, AC-260584 may serve as a lead compound in the development of M(1) selective drugs for the treatment of cognitive impairment associated with schizophrenia and Alzheimer's disease...
  6. doi request reprint Discovery of potential antipsychotic agents possessing pro-cognitive properties
    Jelveh Lameh
    ACADIA Pharmaceuticals, Inc, San Diego, CA 92121, USA
    Naunyn Schmiedebergs Arch Pharmacol 385:313-23. 2012
    ....
  7. ncbi request reprint Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist
    Kimberly E Vanover
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 317:910-8. 2006
    ..6% oral bioavailability in rats. Thus, ACP-103 is a potent, efficacious, orally active 5-HT(2A) receptor inverse agonist with a behavioral pharmacological profile consistent with utility as an antipsychotic agent...
  8. ncbi request reprint Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Boulevard, San Diego, CA 92121, USA
    Mol Pharmacol 70:1974-83. 2006
    ..These results show that M(1) receptors can be activated in at least three distinct ways and that there is no requirement for potent muscarinic agonists to mimic acetylcholine interactions with TM3...
  9. ncbi request reprint Identification of the atypical L-type Ca2+ channel blocker diltiazem and its metabolites as ghrelin receptor agonists
    Jian Nong Ma
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    Mol Pharmacol 72:380-6. 2007
    ..The possible contributions of GHSR1a receptor activation to the clinical actions of diltiazem are discussed in the context of the known beneficial cardiovascular effects of ghrelin...
  10. ncbi request reprint Discovery of novel peptide/receptor interactions: identification of PHM-27 as a potent agonist of the human calcitonin receptor
    Jian Nong Ma
    ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92130, USA
    Biochem Pharmacol 67:1279-84. 2004
    ..These results indicate that the orphan peptide PHM-27 is a potent agonist at the hCTr...
  11. doi request reprint Identification of novel selective V2 receptor non-peptide agonists
    Andria L Del Tredici
    ACADIA Pharmaceuticals Inc, San Diego, CA 92121, USA
    Biochem Pharmacol 76:1134-41. 2008
    ..Thus, AC-94544, AC-88324, and AC-110484 represent novel opportunities for the treatment of disorders associated with V(2) receptor agonist deficiency...
  12. ncbi request reprint Pharmacology of polymorphic variants of the human 5-HT1A receptor
    Andria L Del Tredici
    ACADIA Pharmaceuticals, 3911 Sorrento Valley Blvd, San Diego, CA 92121 1402, USA
    Biochem Pharmacol 67:479-90. 2004
    ..Furthermore, individuals that potentially harbor the A50V polymorphism might display aberrant affective behaviors and altered responses to drugs targeting the 5-HT1A receptor...
  13. ncbi request reprint Identification of the antiarrhythmic drugs amiodarone and lorcainide as potent H3 histamine receptor inverse agonists
    Andria L Del Tredici
    ACADIA Pharmaceuticals Inc, San Diego, California
    J Pharmacol Exp Ther 348:116-24. 2014
    ..These results expand the pharmacophore of H3 histamine receptor antagonist/inverse agonists and may explain, in part, the effects of lorcainide on sleep in humans. ..
  14. doi request reprint The protease activated receptor 2 (PAR2) polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small-molecule PAR2 agonists
    Jian Nong Ma
    ACADIA Pharmaceuticals Inc, San Diego, California
    J Pharmacol Exp Ther 347:697-704. 2013
    ..These results suggest that F240S PAR2 receptors may be useful in screens to detect novel small-molecule PAR2 modulators and that further work on the biological importance of the F240S PAR2 variant is warranted. ..
  15. ncbi request reprint Pharmacology of N-desmethylclozapine
    Jelveh Lameh
    ACADIA Pharmaceuticals Inc, San Diego, California, USA
    Pharmacol Ther 115:223-31. 2007
    ..We also consider whether NDMC, in its own right, might be a superior antipsychotic drug...
  16. ncbi request reprint The second intracellular loop of the m5 muscarinic receptor is the switch which enables G-protein coupling
    E S Burstein
    ACADIA Pharmaceuticals Inc, San Diego, California 92121, USA
    J Biol Chem 273:24322-7. 1998
    ..Therefore, the i2 loop functions as the switch enabling G-protein activation...
  17. pmc AC-186, a selective nonsteroidal estrogen receptor β agonist, shows gender specific neuroprotection in a Parkinson's disease rat model
    Krista McFarland
    ACADIA Pharmaceuticals Inc, San Diego, California 92121, United States
    ACS Chem Neurosci 4:1249-55. 2013
    ..Hence, in addition to a beneficial safety profile for use in both males and females, a selective ERβ agonist has a differentiated pharmacological profile compared to 17β-estradiol in males. ..
  18. doi request reprint Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor
    Jian Nong Ma
    ACADIA Pharmaceuticals, Inc, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 337:275-84. 2011
    ..Thus, these highly efficacious CaSR allosteric agonists represent leads for developing therapeutic agents with potential advantages over existing therapies...
  19. doi request reprint Identification and characterization of novel small-molecule protease-activated receptor 2 agonists
    Luis R Gardell
    ACADIA Pharmaceuticals, Inc, San Diego, CA 92121, USA
    J Pharmacol Exp Ther 327:799-808. 2008
    ..These compounds represent novel small-molecule PAR2 agonists that will be useful in probing the physiological functions of PAR2 receptors...
  20. pmc Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson's disease
    Krista McFarland
    ACADIA Pharmaceuticals Inc, 11085 Torreyana Road, Suite 100, San Diego, California 92121, United States
    ACS Chem Neurosci 4:1430-8. 2013
    ..On the basis of extrapolations from rat to human doses, we hypothesize that low oral doses of bexarotene may provide an effective and tolerated therapy for Parkinson's disease (PD). ..
  21. pmc Chemical genomics: massively parallel technologies for rapid lead identification and target validation
    Uli Hacksell
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Boulevard, San Diego, CA, 92121, USA
    Cytotechnology 38:3-10. 2002
    ....
  22. ncbi request reprint G-protein-coupled receptor-mediated activation of rap GTPases: characterization of a novel Galphai regulated pathway
    Jacques T Weissman
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Blvd, San Diego, CA 92121, USA
    Oncogene 23:241-9. 2004
    ..A constitutively active mutant of Galphai2 also mediated Ras/rap-dependent responses. These data indicate that GPCRs coupled to pertussis-toxin-sensitive G-proteins activate Rap through a Galpha subunit, C3G, and Src-dependent pathway...
  23. ncbi request reprint Discovery of an ectopic activation site on the M(1) muscarinic receptor
    Tracy A Spalding
    ACADIA Pharmaceuticals, Inc, San Diego, California 92121, USA
    Mol Pharmacol 61:1297-302. 2002
    ....
  24. ncbi request reprint Constitutively active muscarinic receptors
    T A Spalding
    ACADIA Pharmaceuticals Inc, San Diego, CA 92121, USA
    Life Sci 68:2511-6. 2001
    ..The i2 loop where mutations also increase constitutive activity was found to loop away from the i3 loop, which has been found to modulate G-protein coupling specificity...
  25. ncbi request reprint 5-hydroxytryptamine2A receptor inverse agonists as antipsychotics
    D M Weiner
    ACADIA Pharmaceuticals Inc, San Diego, California 92121, USA
    J Pharmacol Exp Ther 299:268-76. 2001
    ..The behavioral pharmacology of AC-90179 is characteristic of an atypical antipsychotic agent...
  26. ncbi request reprint The role of M1 muscarinic receptor agonism of N-desmethylclozapine in the unique clinical effects of clozapine
    D M Weiner
    ACADIA Pharmaceuticals, Inc, 3911 Sorrento Valley Boulevard, San Diego, CA, USA
    Psychopharmacology (Berl) 177:207-16. 2004
    ..Despite its unique clinical actions, no specific molecular mechanism responsible for these actions has yet been described...
  27. ncbi request reprint Identification of a ligand-dependent switch within a muscarinic receptor
    T A Spalding
    ACADIA Pharmaceuticals, Inc, San Diego, California 92121, USA
    J Biol Chem 273:21563-8. 1998
    ..These results suggest that TM6 is a switch that defines the activation state of the receptor, and that ligand interactions with TM6 stabilize the receptor in either an active or an inactive conformation...
  28. ncbi request reprint Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954)
    Glenn E Croston
    ACADIA Pharmaceuticals Inc, 3911 Sorrento Valley Boulevard, San Diego, California 92121, USA
    J Med Chem 45:4950-3. 2002
    ..Being a selective nonpeptidic druglike UII receptor agonist, (+)-1 will be useful as a pharmacological research tool and a potential drug lead...
  29. ncbi request reprint Constitutive activity of muscarinic acetylcholine receptors
    Tracy A Spalding
    Genomics Institute of the Novartis Research Foundation, San Diego, California 92121, USA
    J Recept Signal Transduct Res 26:61-85. 2006
    ..Finally, we discuss the possible physiological significance of constitutive activity of muscarinic receptors, incorporating information provided by targeted deletion of each of the muscarinic subtypes...
  30. ncbi request reprint Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H(3) receptor
    P Wellendorph
    ACADIA Pharmaceuticals Inc, San Diego, CA 92121, USA
    Neuropharmacology 42:929-40. 2002
    ....
  31. ncbi request reprint Homologous mutations near the junction of the sixth transmembrane domain and the third extracellular loop lead to constitutive activity and enhanced agonist affinity at all muscarinic receptor subtypes
    Diane J Ford
    Department of Pharmacology, The Pennsylvania State University College of Medicine, Hershey, Pennsylvania 17033, USA
    J Pharmacol Exp Ther 300:810-7. 2002
    ..Based on the results of the present study, it is possible that TM6 represents a general switch for the activation of the muscarinic receptor family...
  32. doi request reprint The human angiotensin AT(1) receptor supports G protein-independent extracellular signal-regulated kinase 1/2 activation and cellular proliferation
    Jakob Lerche Hansen
    Laboratory for Molecular Cardiology, The Danish National Research Foundation Centre for Cardiac Arrhythmia, The Heart Centre, Copenhagen University Hospital Rigshospitalet, Copenhagen, Denmark
    Eur J Pharmacol 590:255-63. 2008
    ..The realization of G protein-independent signalling by the human angiotensin AT(1) receptor has clear pharmacological implications for development of drugs with pathway-specific actions and defined biological outcomes...