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Some frozen analogues of 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP) and of 1-(3- pyridyl)piperazine have been synthesized and tested on rat cerebral cortex by means of binding studies. Among the synthesized substances, only compound 2c was found to displace ( 3 H)- cytisine from the nicotinic binding sites on rat cerebral cortex. Some possible explanations for the inactivity of the other compounds are given.

arkivoc

Design, synthesis and preliminary pharmacological evaluation of rigid analogues of the nicotinic agonist 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP)