de Castiglione R, Faoro F, Perseo G, Piani S, Santangelo F, Melchiorri P, Falconieri Erspamer G, Erspamer V, Guglietta A
Peptides. 1981 Fall;2(3):265-9. doi: 10.1016/s0196-9781(81)80117-9.
Dermorphins are potent opiate-like peptides isolated from the skin of some species of frogs. They are characterized by the presence of a D-amino acid residue, which is crucial for bioactivity. A number of analogues were prepared in order to evaluate the structure-activity relationships. The syntheses were accomplished either by conventional or solid-phase procedures. In vitro assays included both guinea pig ileum (GPI) and mouse vas deferens (MVD) preparations. Central analgesic (tail-flick and hot plate tests) and cataleptic activities were determined in the rat by intracerebroventricular route. The potency of dermorphin (H- Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) in the different tests was: GPI: IC50 = 3.3 nM; MVD: IC50 = 29 nM; hot plate: ED50 = 13.3 pmol/rat; tail-flick: ED50 = 23 pmol/rat; catalepsy: ED50 = 130 pmol/rat.
皮啡肽是从某些蛙类皮肤中分离出的强效类阿片肽。它们的特征是存在一个D-氨基酸残基，这对生物活性至关重要。为了评估构效关系，制备了许多类似物。合成通过常规方法或固相方法完成。体外试验包括豚鼠回肠（GPI）和小鼠输精管（MVD）制剂。通过脑室内途径在大鼠中测定中枢镇痛（甩尾和热板试验）和僵住活性。皮啡肽（H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2）在不同试验中的效力为：GPI：IC50 = 3.3 nM；MVD：IC50 = 29 nM；热板：ED50 = 13.3 pmol/大鼠；甩尾：ED50 = 23 pmol/大鼠；僵住：ED50 = 130 pmol/大鼠。
