alpha-Phenyl-beta-(3,4-dimethoxy)phenethylamines: novel inhibitors of choline acetyltransferase from Torpedo electric organ.
Some derivatives of alpha-phenyl-beta-(3,4-dimethoxy)phenethylamine that might bear a certain conformational resemblance to choline were prepared. The in vitro inhibition of choline acetyltransferase from Torpedo electric organ was investigated. These compounds gave variable degrees of inhibition; the most potent inhibitor was, N,N,N,-trimethyl-alpha-phenyl-beta-(3,4-dimethoxy)phenethylammonium++ + iodide, with an I50 of 1.3 X 10(-5) M. The inhibition of choline acetyltransferase from Spodoptera littoralis larval brains was also determined for comparative study. The aforementioned compound has an I50 of 9 X 10(-6) M on choline acetyltransferase from this source.
D000818:Animals; D001921:Brain / Q000201:enzymology; D055598:Chemical Phenomena; D002621:Chemistry; D002795:Choline O-Acetyltransferase / Q000037:antagonists & inhibitors*; D004557:Electric Organ / Q000201:enzymology*; D066298:In Vitro Techniques; D008566:Membranes / Q000201:enzymology; D010627:Phenethylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D014101:Torpedo / Q000378:metabolism*
D010627:Phenethylamines; D002795:Choline O-Acetyltransferase