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Synthesis and pharmacological characterization of exo-2-(2'-chloro-5-pyridinyl)-7-(endo and exo)-aminobicyclo[2.2.1]heptanes as novel epibatidine analogues.

Abstract：

:Procedures were developed for the synthesis of exo-(2'-chloro-5-pyridinyl)-7-(endo and exo)-amino[2.2.1]heptanes (3a and 3b). The compounds were evaluated for binding to the alpha4beta2 and alpha7 nicotinic acetylcholine receptors (nAChRs), for pharmacological activity in the mouse tail-flick and hot-plate assays, and for hypothermia and locomotor activity. Compounds 3a and 3b possessed alpha4beta2 nAChR binding properties similar to those of (-)-nicotine and were nAChR agonists in all four mouse assays.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Carroll FI,Brieaddy LE,Navarro HA,Damaj MI,Martin BR

doi

10.1021/jm058243v

keywords:

subject

Has Abstract

pub_date

2005-11-17 00:00:00

pages

7491-5

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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