α-Phenyl-β-(3,4-dimethoxy)phenethylamines: Novel Inhibitors of Choline Acetyltransferase from Torpedo Electric Organ

Add time:07/12/2019    Source:sciencedirect.com

Some derivatives of α-phenyl-β-(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-α-phenyl-β-(3,4-dimethoxy)phenethylammonium iodide, with an I50 of 1.3 × 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 × 10−6 M on choline acetyltransferase from this source.

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