Literature DB >> 24292660

Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype-targeted drugs.

Herbert Y Meltzer, Bryan L Roth.   

Abstract

Serotonin (5-hydroxytryptamine, or 5-HT) receptors mediate a plethora of physiological phenomena in the brain and the periphery. Additionally, serotonergic dysfunction has been implicated in nearly every neuropsychiatric disorder. The effects of serotonin are mediated by fourteen GPCRs. Both the therapeutic actions and side effects of commonly prescribed drugs are frequently due to nonspecific actions on various 5-HT receptor subtypes. For more than 20 years, the search for clinically efficacious drugs that selectively target 5-HT receptor subtypes has been only occasionally successful. This review provides an overview of 5-HT receptor pharmacology and discusses two recent 5-HT receptor subtype-selective drugs, lorcaserin and pimavanserin, which target the 5HT2C and 5HT2A receptors and provide new treatments for obesity and Parkinson's disease psychosis, respectively.

Entities:  

Mesh：

Substances：

Year:  2013        PMID： 24292660      PMCID： PMC3859385          DOI： 10.1172/JCI70678

Source DB:  PubMed          Journal:  J Clin Invest        ISSN： 0021-9738            Impact factor:   14.808


  77 in total

1.  Enhancement of cognitive performance in schizophrenia by addition of tandospirone to neuroleptic treatment.

Authors:  T Sumiyoshi; M Matsui; S Nohara; I Yamashita; M Kurachi; C Sumiyoshi; K Jayathilake; H Y Meltzer
Journal:  Am J Psychiatry       Date:  2001-10       Impact factor: 18.112

Review 2.  Drug efficacy at G protein-coupled receptors.

Authors:  Terry Kenakin
Journal:  Annu Rev Pharmacol Toxicol       Date:  2002       Impact factor: 13.820

Review 3.  The molecular biology of serotonin receptors: therapeutic implications for the interface of mood and psychosis.

Authors:  W K Kroeze; B L Roth
Journal:  Biol Psychiatry       Date:  1998-12-01       Impact factor: 13.382

4.  Cloning of the gene and cDNA for mammalian beta-adrenergic receptor and homology with rhodopsin.

Authors:  R A Dixon; B K Kobilka; D J Strader; J L Benovic; H G Dohlman; T Frielle; M A Bolanowski; C D Bennett; E Rands; R E Diehl; R A Mumford; E E Slater; I S Sigal; M G Caron; R J Lefkowitz; C D Strader
Journal:  Nature       Date:  1986 May 1-7       Impact factor: 49.962

5.  Randomized placebo-controlled clinical trial of lorcaserin for weight loss in type 2 diabetes mellitus: the BLOOM-DM study.

Authors:  Patrick M O'Neil; Steven R Smith; Neil J Weissman; Meredith C Fidler; Matilde Sanchez; Jinkun Zhang; Brian Raether; Christen M Anderson; William R Shanahan
Journal:  Obesity (Silver Spring)       Date:  2012-03-16       Impact factor: 5.002

Review 6.  Update on typical and atypical antipsychotic drugs.

Authors:  Herbert Y Meltzer
Journal:  Annu Rev Med       Date:  2012-09-27       Impact factor: 13.739

7.  The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons.

Authors:  A Dumuis; M Sebben; J Bockaert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-10       Impact factor: 3.000

8.  Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol.

Authors:  D N Middlemiss
Journal:  Eur J Pharmacol       Date:  1984-06-01       Impact factor: 4.432

9.  Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment.

Authors:  Xi-Ping Huang; Vincent Setola; Prem N Yadav; John A Allen; Sarah C Rogan; Bonnie J Hanson; Chetana Revankar; Matt Robers; Chris Doucette; Bryan L Roth
Journal:  Mol Pharmacol       Date:  2009-07-01       Impact factor: 4.436

Review 10.  Clozapine: balancing safety with superior antipsychotic efficacy.

Authors:  Herbert Y Meltzer
Journal:  Clin Schizophr Relat Psychoses       Date:  2012-10
View more
  32 in total

1.  Development of the 5-HT2CR-Tango System Combined with an EGFP Reporter Gene.

Authors:  Yoshihisa Watanabe; Atsushi Tsujimura; Miku Aoki; Katsutoshi Taguchi; Masaki Tanaka
Journal:  J Mol Neurosci       Date:  2015-09-15       Impact factor: 3.444

Review 2.  Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily.

Authors:  Bryan L Roth; Wesley K Kroeze
Journal:  J Biol Chem       Date:  2015-06-22       Impact factor: 5.157

Review 3.  Structure and function of serotonin G protein-coupled receptors.

Authors:  John D McCorvy; Bryan L Roth
Journal:  Pharmacol Ther       Date:  2015-01-17       Impact factor: 12.310

4.  Serotonin-2C and -2a receptor co-expression on cells in the rat medial prefrontal cortex.

Authors:  C Nocjar; K D Alex; A Sonneborn; A I Abbas; B L Roth; E A Pehek
Journal:  Neuroscience       Date:  2015-03-27       Impact factor: 3.590

5.  Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.

Authors:  Jianjun Cheng; Patrick M Giguère; Oluseye K Onajole; Wei Lv; Arsen Gaisin; Hendra Gunosewoyo; Claire M Schmerberg; Vladimir M Pogorelov; Ramona M Rodriguiz; Giulio Vistoli; William C Wetsel; Bryan L Roth; Alan P Kozikowski
Journal:  J Med Chem       Date:  2015-02-10       Impact factor: 7.446

6.  Clemizole and modulators of serotonin signalling suppress seizures in Dravet syndrome.

Authors:  Aliesha Griffin; Kyla R Hamling; Kelly Knupp; SoonGweon Hong; Luke P Lee; Scott C Baraban
Journal:  Brain       Date:  2017-03-01       Impact factor: 13.501

7.  The atypical antipsychotic olanzapine causes weight gain by targeting serotonin receptor 2C.

Authors:  Caleb C Lord; Steven C Wyler; Rong Wan; Carlos M Castorena; Newaz Ahmed; Dias Mathew; Syann Lee; Chen Liu; Joel K Elmquist
Journal:  J Clin Invest       Date:  2017-08-14       Impact factor: 14.808

Review 8.  Pimavanserin: A Novel Drug Approved to Treat Parkinson's Disease Psychosis.

Authors:  Amanda K Kitten; Sarah A Hallowell; Stephen R Saklad; Kirk E Evoy
Journal:  Innov Clin Neurosci       Date:  2018-02-01

9.  Design and Synthesis of (2-(5-Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist.

Authors:  Jianjun Cheng; Patrick M Giguere; Wei Lv; Bryan L Roth; Alan P Kozikowski
Journal:  Tetrahedron Lett       Date:  2015-06-03       Impact factor: 2.415

10.  5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.

Authors:  Yao Peng; John D McCorvy; Kasper Harpsøe; Katherine Lansu; Shuguang Yuan; Petr Popov; Lu Qu; Mengchen Pu; Tao Che; Louise F Nikolajsen; Xi-Ping Huang; Yiran Wu; Ling Shen; Walden E Bjørn-Yoshimoto; Kang Ding; Daniel Wacker; Gye Won Han; Jianjun Cheng; Vsevolod Katritch; Anders A Jensen; Michael A Hanson; Suwen Zhao; David E Gloriam; Bryan L Roth; Raymond C Stevens; Zhi-Jie Liu
Journal:  Cell       Date:  2018-02-01       Impact factor: 41.582
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.