Literature DB >> 17227285

Pharmacological profile of the 5-HT(2C) receptor agonist WAY-163909; therapeutic potential in multiple indications.

John Dunlop1, Karen L Marquis, H K Lim, Louis Leung, John Kao, Cynthia Cheesman, Sharon Rosenzweig-Lipson.   

Abstract

The 5-HT(2C) receptor subtype has been implicated in a wide variety of conditions including obesity, anxiety, depression, obsessive compulsive disorder, schizophrenia, migraine and erectile dysfunction and as a consequence has received considerable attention as a target for drug discovery. Here we review the pharmacological, pharmacokinetic and toxicological profile of WAY-163909 {(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole}, a novel 5-HT(2C) receptor selective agonist. Consistent with a potential therapeutic utility in obesity, schizophrenia and depression WAY-163909 was found to have robust dose-dependent effects in animal models of obesity, psychotic-like behavior or depression.

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Year:  2006        PMID： 17227285      PMCID： PMC6506193          DOI： 10.1111/j.1527-3458.2006.00167.x

Source DB:  PubMed          Journal:  CNS Drug Rev        ISSN： 1080-563X


  30 in total

Review 1.  A review of central 5-HT receptors and their function.

Authors:  N M Barnes; T Sharp
Journal:  Neuropharmacology       Date:  1999-08       Impact factor: 5.250

2.  Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.

Authors:  Annmarie L Sabb; Robert L Vogel; Gregory S Welmaker; Joan E Sabalski; Joseph Coupet; John Dunlop; Sharon Rosenzweig-Lipson; Boyd Harrison
Journal:  Bioorg Med Chem Lett       Date:  2004-05-17       Impact factor: 2.823

Review 3.  Animal models of depressive illness: the importance of chronic drug treatment.

Authors:  P J Mitchell; P H Redfern
Journal:  Curr Pharm Des       Date:  2005       Impact factor: 3.116

4.  Comparative effects of continuous infusion of mCPP, Ro 60-0175 and d-fenfluramine on food intake, water intake, body weight and locomotor activity in rats.

Authors:  S P Vickers; K R Benwell; R H Porter; M J Bickerdike; G A Kennett; C T Dourish
Journal:  Br J Pharmacol       Date:  2000-07       Impact factor: 8.739

5.  Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.

Authors:  G S Welmaker; J A Nelson; J E Sabalski; A L Sabb; J R Potoski; D Graziano; M Kagan; J Coupet; J Dunlop; H Mazandarani; S Rosenzweig-Lipson; S Sukoff; Y Zhang
Journal:  Bioorg Med Chem Lett       Date:  2000-09-04       Impact factor: 2.823

6.  Desmethylimipramine (DMI) counteracts learned helplessness in rats.

Authors:  A I Leshner; H Remler; A Biegon; D Samuel
Journal:  Psychopharmacology (Berl)       Date:  1979-11       Impact factor: 4.530

7.  Acceleration of onset of action in schedule-induced polydipsia: combinations of SSRI and 5-HT1A and 5-HT1B receptor antagonists.

Authors:  Sandy Hogg; Ashutosh Dalvi
Journal:  Pharmacol Biochem Behav       Date:  2004-01       Impact factor: 3.533

8.  Oral administration of the 5-HT2Creceptor agonist, mCPP, reduces body weight gain in rats over 28 days as a result of maintained hypophagia.

Authors:  S P Vickers; N Easton; L J Webster; A Wyatt; M J Bickerdike; C T Dourish; G A Kennett
Journal:  Psychopharmacology (Berl)       Date:  2003-04-11       Impact factor: 4.530

9.  Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.

Authors:  Yasuharu Kimura; Ken-ichi Hatanaka; Yuki Naitou; Kyoichi Maeno; Itsuro Shimada; Akiko Koakutsu; Fumikazu Wanibuchi; Tokio Yamaguchi
Journal:  Eur J Pharmacol       Date:  2004-01-01       Impact factor: 4.432

10.  Antiobesity effect of YM348, a novel 5-HT2C receptor agonist, in Zucker rats.

Authors:  Aska Hayashi; Rie Sonoda; Yasuharu Kimura; Toshiyuki Takasu; Masanori Suzuki; Masao Sasamata; Keiji Miyata
Journal:  Brain Res       Date:  2004-06-18       Impact factor: 3.252
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  21 in total

1.  HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia.

Authors:  Alan P Kozikowski; Sung Jin Cho; Niels H Jensen; John A Allen; Andreas M Svennebring; Bryan L Roth
Journal:  ChemMedChem       Date:  2010-08-02       Impact factor: 3.466

2.  Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.

Authors:  Gang Chen; Sung Jin Cho; Xi-Ping Huang; Niels H Jensen; Andreas Svennebring; Maria F Sassano; Bryan L Roth; Alan P Kozikowski
Journal:  ACS Med Chem Lett       Date:  2011-10-10       Impact factor: 4.345

Review 3.  A short history of the 5-HT2C receptor: from the choroid plexus to depression, obesity and addiction treatment.

Authors:  Jose M Palacios; Angel Pazos; Daniel Hoyer
Journal:  Psychopharmacology (Berl)       Date:  2017-03-07       Impact factor: 4.530

4.  PSD-95 is essential for hallucinogen and atypical antipsychotic drug actions at serotonin receptors.

Authors:  Atheir I Abbas; Prem N Yadav; Wei-Dong Yao; Margaret I Arbuckle; Seth G N Grant; Marc G Caron; Bryan L Roth
Journal:  J Neurosci       Date:  2009-06-03       Impact factor: 6.167

5.  WAY-163909, a 5-HT2C agonist, enhances the preclinical potency of current antipsychotics.

Authors:  Steven M Grauer; Radka Graf; Rachel Navarra; Amy Sung; Sheree F Logue; Gary Stack; Christine Huselton; Zhi Liu; Thomas A Comery; Karen L Marquis; Sharon Rosenzweig-Lipson
Journal:  Psychopharmacology (Berl)       Date:  2008-12-20       Impact factor: 4.530

6.  Selective serotonin 5-HT(2C) receptor activation suppresses the reinforcing efficacy of cocaine and sucrose but differentially affects the incentive-salience value of cocaine- vs. sucrose-associated cues.

Authors:  Kathryn A Cunningham; Robert G Fox; Noelle C Anastasio; Marcy J Bubar; Sonja J Stutz; F Gerard Moeller; Scott R Gilbertson; Sharon Rosenzweig-Lipson
Journal:  Neuropharmacology       Date:  2011-05-11       Impact factor: 5.250

Review 7.  Marine indole alkaloids: potential new drug leads for the control of depression and anxiety.

Authors:  Anna J Kochanowska-Karamyan; Mark T Hamann
Journal:  Chem Rev       Date:  2010-08-11       Impact factor: 60.622

8.  Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.

Authors:  Sung Jin Cho; Niels H Jensen; Toru Kurome; Sudhakar Kadari; Michael L Manzano; Jessica E Malberg; Barbara Caldarone; Bryan L Roth; Alan P Kozikowski
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

9.  Synergism between a serotonin 5-HT2A receptor (5-HT2AR) antagonist and 5-HT2CR agonist suggests new pharmacotherapeutics for cocaine addiction.

Authors:  Kathryn A Cunningham; Noelle C Anastasio; Robert G Fox; Sonja J Stutz; Marcy J Bubar; Sarah E Swinford; Cheryl S Watson; Scott R Gilbertson; Kenner C Rice; Sharon Rosenzweig-Lipson; F Gerard Moeller
Journal:  ACS Chem Neurosci       Date:  2012-08-11       Impact factor: 4.418

10.  Overexpression of 5-HT2C receptors in forebrain leads to elevated anxiety and hypoactivity.

Authors:  Atsuko Kimura; Paula L Stevenson; Roderick N Carter; Gavin Maccoll; Karen L French; J Paul Simons; Raya Al-Shawi; Valerie Kelly; Karen E Chapman; Megan C Holmes
Journal:  Eur J Neurosci       Date:  2009-07-15       Impact factor: 3.386
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