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Synthesis of spasmolytic N-[(diphenylacetamido)methyl]dimethylalkyammonium iodides

Petter, A. ; Schönenberger, Helmut ; Gutschow, K. ; Kuehling, V. ; Taneja, V.


Ten Ph2CHCONHCH2N+Me2(CH2)nMe I- (I, n = 0-9) were prepd. by reaction of Ph2CHCONH2, paraformaldehyde, and HNMe(CH2)nMe and subsequent quaternization. I (n = 0-2) and I (n = 3-9) had competitive and noncompetitive, resp., antagonistic effects against acetylcholine on the isolated rat jejunum. Increased chain length led to increased spasmolytic activity of the latter. I (n = 9) was 20 times more active than papaverine, but showed no mydriatic effect.

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