Abstract:
: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.
journal_name
Peptidesjournal_title
Peptidesauthors
de Castiglione R,Faoro F,Perseo G,Piani S,Santangelo F,Melchiorri P,Falconieri Erspamer G,Erspamer V,Guglietta Adoi
10.1016/s0196-9781(81)80117-9subject
Has Abstractpub_date
1981-10-01 00:00:00pages
265-9issue
3eissn
0196-9781issn
1873-5169pii
S0196-9781(81)80117-9journal_volume
2pub_type
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