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Bioorg Med Chem Lett. 2002 Jan 21;12(2):243-8.

Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.

Author information

1
Janssen-Cilag, Basic Research Centre, Jarama s/n, 45007 Toledo, Spain. jandres@jaces.jnj.com

Abstract

The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT(2A/2C) and H(1) receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT(2A/2C) receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent.

PMID:
11755364
DOI:
10.1016/s0960-894x(01)00721-1
[Indexed for MEDLINE]

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