title: Effect of piperidine and related alicyclic amines on nicotinic and muscarinic agonist binding sites in the mammalian brain.
abstract: The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [3H]nicotine and [3H]cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1 microM-30 mM completed dose-dependently with [3H]nicotine and [3H]CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [3H]nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [3H]nicotine binding sites in the rat cerebral cortex than of [3H]CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [3H]CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [3H]nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [3H]nicotine binding between species such as rat, mouse, guinea-pig and rabbit. Thus, the present study demonstrates a high affinity of piperidine for nicotinic cholinoceptors in the mammalian brain.
mesh_terms: D000588:Amines / Q000494:pharmacology*; D000818:Animals; D000831:Animals, Newborn; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D051379:Mice; D009538:Nicotine / Q000378:metabolism; D010277:Parasympathomimetics / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D011976:Receptors, Muscarinic / Q000187:drug effects*; D011978:Receptors, Nicotinic / Q000187:drug effects*; D013045:Species Specificity
chemical_list: D000588:Amines; D010277:Parasympathomimetics; D010880:Piperidines; D011976:Receptors, Muscarinic; D011978:Receptors, Nicotinic; C032727:piperidine; D009538:Nicotine