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Zusammenfassung
Ten title compds., PhCH2CH(NH2)CONR3CHR2CHR1Ph (R1 = H or OH; R2 and R3 = H or Me), were screened for antidepressant activity. The most active deriv. was N-L-phenylalanyl L-2-amino-1-phenylpropane (I) [85562-33-0]. I exhibited adrenergic activity (noradrenaline potentiation in the rat vas deferens, tetrabenozine antagonism in the mouse), cholinergic blocking activity (acetylcholine antagonism in ...
Zusammenfassung
Ten title compds., PhCH2CH(NH2)CONR3CHR2CHR1Ph (R1 = H or OH; R2 and R3 = H or Me), were screened for antidepressant activity. The most active deriv. was N-L-phenylalanyl L-2-amino-1-phenylpropane (I) [85562-33-0]. I exhibited adrenergic activity (noradrenaline potentiation in the rat vas deferens, tetrabenozine antagonism in the mouse), cholinergic blocking activity (acetylcholine antagonism in the rat jejunum, oxotremorine antagonism in the mouse, antiaggressive activity in isolated mice), and local anesthetic activity (inhibition of conduction in the frog heart ventricular strip). In its pharmacol. behavior, I seemed to be more an antidepressant than a psychotonic drug. The idea that the effects of I involve the metabolic release of the amphetamine component is supported by the fact that at higher doses there was a shortening of the duration of hexobarbital narcosis and an increase in the spontaneous activity of mice. Some structure-activity relations are briefly discussed.
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