492-02-4Relevant academic research and scientific papers
Synthesis and preliminary pharmacological evaluation of some cytisine derivatives
Canu Boido, Caterina,Sparatore, Fabio
, p. 438 - 451 (2007/10/03)
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, β-adrenergic antagonism, α1- and α2-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 K(i) values in the range 30-163 nM.
