Referenced in: none

Automatically associated channels: Kir2.3

Title: Synthesis and preliminary pharmacological evaluation of some cytisine derivatives.

Authors: C Canu Boido, F Sparatore

Journal, date & volume: Farmaco, 1999 Jul 30 , 54, 438-51

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/10486911

Abstract
Thirty-one N-derivatives of cytisine were prepared in order to modify its pharmacological profile and to obtain compounds of potential therapeutic interest either at a peripheral or central level, particularly as nicotinic ligands with improved ability to cross the blood-brain barrier. Actually, with the introduction of different kinds of substituent on the basic nitrogen of cytisine a variety of activities were observed, both in vivo (analgesic, dopamine antagonism, antihypertensive, inhibition of stress-induced ulcers, antiinflammatory, protection from PAF-induced mortality, hypoglycemic) and in vitro (positive cardio-inotropic, beta-adrenergic antagonism, alpha 1- and alpha 2-antagonism, inhibition of PAF-induced platelet aggregation). Six randomly selected compounds were tested for the ability to recognize a central nicotinic receptor and four of them exhibited Ki values in the range 30-163 nM.