Melchiorri P, Erspamer G F, Erspamer V, Guglietta A, De Castiglione R, Faoro F, Perseo G, Piani S, Santangelo F
Peptides. 1982 Sep-Oct;3(5):745-8. doi: 10.1016/0196-9781(82)90009-2.
A new series of analogues of the potent opiate-like peptides dermorphins (mainly tetra- and pentapeptides) were synthesized in order to better evaluate the structure-activity relationships. Relative potencies were referred to dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2), the prototype of this class of frog skin peptides. Peripheral opioid activity (guinea-pig ileum and mouse vas deferens) was determined for all the dermorphin analogues. For a selected number of them also central analgesic (hot plate and tail-flick tests) and cataleptic activities were assayed in the rat by intracerebroventricular administration.
