Life Sciences 1983-10-17

Analgesic properties of N-terminal substituted phenylalanyl-alanine.

G Borin, P Giusti, L Cima

Index: Life Sci. 33(16) , 1575-80, (1983)

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Abstract

Phenylalanylalanine, an in vitro inhibitor of enkephalinase, and some of its N alpha-derivatives are shown to possess an analgesic action when injected i.p. and i.c.v. into mice in the presence or absence of Leu5-enkephalin. In the second case a synergistic response is observed. The intensity of the analgesic response depends markedly on the nature of the N-terminal substituent which affects the hydrophobic character of the resulting dipeptide, its subsequent transport and probably its rate of biotransformation by cleaving enzymes.