吡嗪并[1,2-a]吲哚作为新型高亲和力和选择性咪唑啉I(2)受体配体。

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

作者信息

Chang-Fong Jean, Tyacke Robin J, Lau Alice, Westaway Julie, Hudson Alan L, Glennon Richard A

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540 USA.

出版信息

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5. doi: 10.1016/j.bmcl.2003.12.033.

DOI:10.1016/j.bmcl.2003.12.033

PMID:15013010

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.

摘要

1,2,3,4-四氢吡嗪并[1,2-a]吲哚被描述为一类新型的I(2)咪唑啉受体配体。特别地，8-甲氧基-1,2,3,4-四氢吡嗪并[1,2-a]吲哚（8-OMe THPI；3c）以高亲和力结合I(2)咪唑啉受体（K(i)=6.2 nM），并且相对于其对I(1)咪唑啉受体、α(2)肾上腺素能受体以及5-HT(2A)和5-HT(2C)5-羟色胺受体的亲和力具有极高（≥1000倍）的选择性。