Click here for full price details of [Phe1Y(CH2-NH)Gly2]Nociceptin(1-13)NH2
Biological Activity:
Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo.
Selective, competitive antagonism at the nociceptin receptor has also been
reported (pA2 = 7.02 and 6.75 in the guinea-pig ileum and mouse vas
deferens respectively).
Guerrini et al (1997) Address and message sequences for the nociceptin
receptor: a structure-activity study of nociceptin (1-13)-peptide amide.
J.Med.Chem. 40 1789. Guerriniet al (1998) A new
selective antagonist of the nociceptin receptor. Br.J.Pharmacol. 123
163. Xuet al (1998) [Phe1j(CH2-NH)Gly2-nociceptin-(1-13)NH2,
a proposed antagonist of the nociceptin receptor, is a potent and stable
agonist in the rat spinal cord. Neurosci.Lett. 249 127. Okawa et
al (1999) Comparison of the effects of [Phe1j(CH2-NH)Gly2-nociceptin-(1-13)NH2
in rat brain, rat vas deferens and CHO cells expressing recombinant human
nociceptin receptors. Br.J.Pharmacol. 127 123.
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