Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.

Abstract:

:1,2,3,4-Tetrahydropyrazino[1,2-a]indoles are described as a novel class of I(2) imidazoline receptor ligands. In particular, 8-methoxy-1,2,3,4-tetrahydropyrazino[1,2-a]indole (8-OMe THPI; 3c) binds with high affinity at I(2) imidazoline receptors (K(i)=6.2 nM) and with exceptional (> or =1000-fold) selectivity relative to its affinity for I(1) imidazoline receptors, alpha(2)adrenergic receptors, and 5-HT(2A) and 5-HT(2C) serotonin receptors.

journal_name

Bioorg Med Chem Lett

authors

Chang-Fong J,Tyacke RJ,Lau A,Westaway J,Hudson AL,Glennon RA

doi

10.1016/j.bmcl.2003.12.033

subject

Has Abstract

pub_date

2004-02-23 00:00:00

pages

1003-5

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960894X03013209

journal_volume

14

pub_type

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