
Journal of Medicinal Chemistry p. 1445 - 1447 (1983)
Update date:2022-09-26
Topics:
Darlak, Krzysztof
Grzonka, Zbigniew
Janicki, Piotr
Czlonkowski, Andrzej
Gumulka, S. Witold
Dermorphin and its analogues substituted at position 1 by N-acetyltyrosine, O-methyltyrosine, phenylalanine, D-phenylalanine, or alanine were obtained by solid-phase peptide synthesis.Their pharmacological effects were studied in vitro by the guinea pig ileum method and in vivo by the hot plate method, and the results were compared with those of morphine.The most pronounced activity was shown for dermorphin.A radioreceptor study showed a moderate affinity of dermorphin and its Tyr(Me)1 analogue for the opiate receptor sites from striatal homogenates.
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(1983)