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Synthesis and pharmacological evaluation of some (pyridyl)cyclopropylmethyl amines and their methiodides as nicotinic receptor ligands.

作者信息

Guandalini Luca, Dei Silvia, Manetti Dina, Romanelli Maria Novella, Scapecchi Serena, Teodori Elisabetta, Varani Katia

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Firenze, Florence, Italy.

出版信息

Farmaco. 2002 Jun;57(6):487-96. doi: 10.1016/s0014-827x(02)01234-x.

DOI:10.1016/s0014-827x(02)01234-x
PMID:12088064
Abstract

A series of 3- and (4-pyridyl)cyclopropylmethyl amines and their quaternary ammonium derivatives have been synthesized; they can be considered as rigid analogues of nicotine. The compounds have been tested on rat cerebral cortex to measure the affinity for the central nicotinic receptor. Only the methiodides show affinity in the micromolar range. The results obtained can provide useful information on the topography of the nicotinic receptor-binding site.

摘要

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