Discovery of highly selective imidazoline receptor ligands

作者: L. Brasili , M. Pigini , P. Bousquet , A. Carotti , M. Dontenwill

DOI: 10.1016/S0165-7208(96)80029-8

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摘要: Publisher Summary This chapter discusses the discovery of highly selective imidazoline receptor ligands. Phenylethylamines and imidazolines are traditionally thought as representing two major classes α-adrenergic agonists, yet there is evidence to suggest that these compounds do not interact with receptors in an identical manner. The separation procedure α 1 agonist activity from affinity. There also some discussion about comparative molecular field analysis (CoMFA) modeling application. concept I has gained consensus since hypothesis Bousquet hypothensive action clonidine could be related its structure rather than interaction 2 -adrenergic receptors. Investigations radiolabeled ligands have shown existence binding sites several tissues species including humans. Furthermore, functional studies, though still few number, demonstrated may represent receptors, agmantine natural neurotrasmitter seems support this view.

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