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Titolo:
Acetyl-RYYRIK-NH2 is a highly efficacious OP4 receptor agonist in the cardiovascular system of anesthetized rats
Autore:
Malinowska, B; Kozlowska, H; Berger, H; Schlicker, E;
Indirizzi:
Univ Bonn, Dept Pharmacol & Toxicol, D-53113 Bonn, Germany Univ Bonn Bonn Germany D-53113 harmacol & Toxicol, D-53113 Bonn, Germany Res Inst Mol Pharmacol, D-10315 Berlin, Germany Res Inst Mol Pharmacol Berlin Germany D-10315 l, D-10315 Berlin, Germany Med Acad Bialystok, Dept Expt Physiol, PL-15230 Bialystok, Poland Med AcadBialystok Bialystok Poland PL-15230 PL-15230 Bialystok, Poland
Titolo Testata:
PEPTIDES
fascicolo: 12, volume: 21, anno: 2000,
pagine: 1875 - 1880
SICI:
0196-9781(200012)21:12<1875:AIAHEO>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
ORPHANIN-FQ; IN-VITRO; NOCICEPTIN; ORL1;
Keywords:
nociceptin ORL1 receptor; OP4 receptors; [Phe(1)psi(CH2-NH)Gly2]-nociceprin(1-13)NH2 acetyl-RYYRIK-NH2; naloxone benzoylhydrazone; cardiovascular system;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Schlicker, E Univ Bonn, Dept Pharmacol & Toxicol, Reuterstr 2b, D-53113 Bonn, Germany Univ Bonn Reuterstr 2b Bonn Germany D-53113 13 Bonn, Germany
Citazione:
B. Malinowska et al., "Acetyl-RYYRIK-NH2 is a highly efficacious OP4 receptor agonist in the cardiovascular system of anesthetized rats", PEPTIDES, 21(12), 2000, pp. 1875-1880

Abstract

Nociceptin, the endogenous ligand of the OF4 or ORL1 (opioid receptor-like,) receptor, decreases blood pressure and heart rare in anesthetized rats, Since the OP4 receptor antagonist [Phe(1)Psi (CH2-NH)Gly(2)]-nociceptin(1-13)NH2 possesses an agonistic effect in this model, we examined whether other purported OP4 receptor antagonists, acetyl-RYYRIK-NH2 and naloxone benzoylhydrazone, antagonize the depressant effects of nociceptin. Acetyl-RYYRIK-NH2, like nociceptin and [Phe(1)Psi (CH2-NH)Gly(2)]-nociceptin(1-13)NH2 andunlike naloxone benzoylhydrazone, decreased diastolic blood pressure and heart rate (rank order of potencies: nociceptin approximate to acetyl-RYYRIK-NH2 much greater than [Phe(1)Psi (CH2-NH)Gly(2)]-nociceptin(1-13)NH2). Thedepressant effects were insensitive to the OP1-3 receptor antagonist naloxone but diminished by naloxone benzoylhydrazone. In conclusion, the hypotensive and bradycardic effects of nociceptin in the anesthetized rat are mediated via OP4 receptors, at which acetyl-RYYRIK-NH2 is a highly potent and efficacious agonist. (C) 2000 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 07:23:00