Allenic Amines: A New Class of Nonhydrazine MAO Inhibitors

N-2,3-Butadienyl-N-methylbenzylamine HCl (U-1247) and N-2,3-butadienyl-N-methyl-o-chlorobenzylamine HCl (U-1379) have been synthesized and potent in vivo monoamine oxidase inhibition demonstrated. Antihypertensive activity comparable to that produced by pargyline was demonstrated in hypertensive rat...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1968-03, Vol.57 (3), p.430-433
Main Authors: Halliday, R.P., Davis, C.S., Heotis, J.P., Pals, D.T., Watson, E.J., Bickerton, R.K.
Format: Article
Language:English
Subjects:
Allenic amines-synthesis
Amines - chemical synthesis
Amines - pharmacology
Amines - toxicity
Animals
antihypertensive activity
Antihypertensive Agents - chemical synthesis
Antihypertensive Agents - pharmacology
Antihypertensive Agents - toxicity
Brain - drug effects
Hypotensive
Hypotensive, antihypertensive activity
IR spectrophotometry-structure
LD50 value-allenic amines
Liver - drug effects
Monoamine oxidase inhibitors
Monoamine Oxidase Inhibitors - chemical synthesis
Monoamine Oxidase Inhibitors - pharmacology
Monoamine Oxidase Inhibitors - toxicity
Pargyline - administration & dosage
Pargyline - pharmacology
Pargyline - toxicity
Rats
Tyramine - pharmacology
Vapor-phase chromatography-identity
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Summary:N-2,3-Butadienyl-N-methylbenzylamine HCl (U-1247) and N-2,3-butadienyl-N-methyl-o-chlorobenzylamine HCl (U-1379) have been synthesized and potent in vivo monoamine oxidase inhibition demonstrated. Antihypertensive activity comparable to that produced by pargyline was demonstrated in hypertensive rats with U-1247. When administered to mice, U-1247 and U-1379 produced initial stimulation of motor activity in contrast with pargyline which produced initial depression.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600570312