Beck, D. and Fink, K. and Hoelzl, J. and Krieglstein, J. and Petter, A. and Rieger, H. and Schönenberger, Helmut (1983) Pharmacology of potential antidepressants of the N-L-phenylalanyl-beta -phenylalkylamine class. Arzneimittel-Forschung = Drug research 33 (3), pp. 404-410.
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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.
|Additional information (public):||CAN 98:172581 1-3 Pharmacology 35402-94-9; 35402-94-9D; 61925-91-5; 61925-92-6; 61925-93-7; 61925-94-8; 61925-95-9; 61950-61-6; 61950-62-7; 61950-63-8; 61950-64-9 Role: BAC (Biological activity or effector, except adverse), BSU (Biological study, unclassified), THU (Therapeutic use), BIOL (Biological study), USES (Uses) (antidepressant activity of, structure in relation to)|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Antidepressants (phenylalanylphenylalkylamine derivs. as, structure in relation to) Molecular structure-biological activity relationship (antidepressant, of phenylalanylphenylalkylamines) phenylalanylphenylalkylamine deriv antidepressant structure|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Unknown|
|Deposited On:||22 Nov 2010 13:59|
|Last Modified:||22 Nov 2010 13:59|
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