Nociceptin, nociceptin-1–13.-NH2, Ac-RYYRWK-NH2, wPhe1cCH2`NH.Gly 2 xnociceptin-1–13.-NH2, the new nociceptin analog wNphe1xnociceptin-1–13.-NH2, and endomorphin-1 have been tested in the isolated mouse colon. All peptides, except wNphe1xnocicep- tin-1–13.-NH2, caused concentration-dependent, tetrodotoxin-sensitive contractions showing similar maximal effects. Naloxone 1 mM. blocked the effect of endomorphin-1 but not that of the other peptides. wNphe1xnociceptin-1–13.-NH2 10 mM. was inactive against endomorphin-1, but antagonized the contractile effects of nociceptin receptor ligands showing similar p A2 values f6.0.. The present findings indicate that wNphe1xnociceptin-1–13.-NH2 is a low-potency, selective nociceptin receptor antagonist, devoid of residual agonist activity.
[Nphe(1)]nociceptin-(1-13)-NH2 antagonizes nociceptin effects in the mouse colon
CALO', Girolamo;
1999
Abstract
Nociceptin, nociceptin-1–13.-NH2, Ac-RYYRWK-NH2, wPhe1cCH2`NH.Gly 2 xnociceptin-1–13.-NH2, the new nociceptin analog wNphe1xnociceptin-1–13.-NH2, and endomorphin-1 have been tested in the isolated mouse colon. All peptides, except wNphe1xnocicep- tin-1–13.-NH2, caused concentration-dependent, tetrodotoxin-sensitive contractions showing similar maximal effects. Naloxone 1 mM. blocked the effect of endomorphin-1 but not that of the other peptides. wNphe1xnociceptin-1–13.-NH2 10 mM. was inactive against endomorphin-1, but antagonized the contractile effects of nociceptin receptor ligands showing similar p A2 values f6.0.. The present findings indicate that wNphe1xnociceptin-1–13.-NH2 is a low-potency, selective nociceptin receptor antagonist, devoid of residual agonist activity.Pubblicazioni consigliate
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