Literature DB >> 10987434

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.

G S Welmaker1, 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.   

Abstract

A series 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 was shown to exhibit 5-HT2C agonist binding and functional activity. Compound 21R inhibited food intake over 2 h in fasted, male Sprague Dawley rats with ED50 values of 2 mg/kg (i.p.) and 10 mg/kg (p.o.).

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Year:  2000        PMID: 10987434     DOI: 10.1016/s0960-894x(00)00400-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

Review 1.  Pharmacological profile of the 5-HT(2C) receptor agonist WAY-163909; therapeutic potential in multiple indications.

Authors:  John Dunlop; Karen L Marquis; H K Lim; Louis Leung; John Kao; Cynthia Cheesman; Sharon Rosenzweig-Lipson
Journal:  CNS Drug Rev       Date:  2006 Fall-Winter

2.  Regulation of adipocyte differentiation by activation of serotonin (5-HT) receptors 5-HT2AR and 5-HT2CR and involvement of microRNA-448-mediated repression of KLF5.

Authors:  Minako Kinoshita; Koh Ono; Takahiro Horie; Kazuya Nagao; Hitoo Nishi; Yasuhide Kuwabara; Rieko Takanabe-Mori; Koji Hasegawa; Toru Kita; Takeshi Kimura
Journal:  Mol Endocrinol       Date:  2010-08-18

3.  Oppositional effects of serotonin receptors 5-HT1a, 2, and 2c in the regulation of adult hippocampal neurogenesis.

Authors:  Friederike Klempin; Harish Babu; Davide De Pietri Tonelli; Edson Alarcon; Klaus Fabel; Gerd Kempermann
Journal:  Front Mol Neurosci       Date:  2010-07-30       Impact factor: 5.639

4.  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

5.  Support for 5-HT2C receptor functional selectivity in vivo utilizing structurally diverse, selective 5-HT2C receptor ligands and the 2,5-dimethoxy-4-iodoamphetamine elicited head-twitch response model.

Authors:  Clinton E Canal; Raymond G Booth; Drake Morgan
Journal:  Neuropharmacology       Date:  2013-01-23       Impact factor: 5.250

Review 6.  Innovative approaches for the development of antidepressant drugs: current and future strategies.

Authors:  Lee E Schechter; Robert H Ring; Chad E Beyer; Zoë A Hughes; Xavier Khawaja; Jessica E Malberg; Sharon Rosenzweig-Lipson
Journal:  NeuroRx       Date:  2005-10

7.  Antidepressant-like effects of the novel, selective, 5-HT2C receptor agonist WAY-163909 in rodents.

Authors:  Sharon Rosenzweig-Lipson; Annmarie Sabb; Gary Stack; Paul Mitchell; Irwin Lucki; Jessica E Malberg; Steve Grauer; Julie Brennan; John F Cryan; Stacey J Sukoff Rizzo; John Dunlop; James E Barrett; Karen L Marquis
Journal:  Psychopharmacology (Berl)       Date:  2007-02-13       Impact factor: 4.415

  7 in total

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