Studies on the mechanisms of action of local anesthetics. Part 9. N-Aminoacyl-beta -phenylalkylamine studies for the development of antidepressants from psychostimulants

Abstract

Of 10 N-L-phenylalanyl-beta -phenylalkylamines[PhCH2CH(NH2)CONR3CHR2CHR1Ph] (I, R1 = H or OH; R2 and R3 = H or Me) prepd. and tested as antidepressants, I(R1 = H; R2 and R3 = Me) [61925-95-9] and I(R1 = OH; R2 = Me; R3 = H) (II) [61950-64-9] were the most active compds. in the inhibition of cond. in strips of frog heart ventrical, I(R1 and R3 = H; R2 = Me) (III) [61925-94-8] and II were the most active in potentiating the effect of noradrenaline in rat vas deferens. III showed cocaine-like activity, whereas II showed desipramine-like activity.