Effects of some isomers and analogues of nicotine on junctional transmission.

摘要: A number of isomers and homologues nicotine, (2-, 3- 4-pyridylmethyl)- [2-(2-, 4-pyridyl)ethyl]- dialkylamines trialkylammonium salts, have been prepared. They tested for their ability to act like acetylcholine in causing contracture the chick biventer-cervicis and, some them, stimulate superior cervical ganglion cat, nictitating membrane. All compounds block transmission on cat rat diaphragm preparation, most them inhibit enzymatic hydrolysis acetylcholine, using an acetone-powder dog caudate nucleus as a source acetylcholinesterase. The dissociation constants measured by electrometric titration. were used compute amount monovalent ion present conditions biological tests, activities have, accordingly, compared ionic, well molecular, basis. two sets figures do not differ greatly. Trimethyl[2-(3-pyridyl)ethyl]ammonium (23) was potent compound preparations. On ionic basis (that is, with nicotinium ion) this 2.6 times active nicotine biventer 11 ganglion. it 7.1 less than 1-methyl-1-(3-pyridylmethyl)-pyrrolidinium (26) (9.5 trimethyl(4-pyridylmethyl)-ammonium (21) (11 times). relationships between structure constant, anticholinesterase activity, activity pharmacological tests discussed.