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Titolo:
Identification and characterization of a new growth hormone-releasing peptide receptor in the heart
Autore:
Bodart, V; Bouchard, JF; McNicoll, N; Escher, E; Carriere, P; Ghigo, E; Sejlitz, T; Sirois, MG; Lamontagne, D; Ong, H;
Indirizzi:
Univ Montreal, Fac Pharm, Montreal, PQ H3C 3J7, Canada Univ Montreal Montreal PQ Canada H3C 3J7 rm, Montreal, PQ H3C 3J7, Canada Univ Sherbrooke, Dept Pharmacol, Sherbrooke, PQ, Canada Univ Sherbrooke Sherbrooke PQ Canada t Pharmacol, Sherbrooke, PQ, Canada Univ Montreal, Fac Med Vet, St Hyacinthe, PQ J2S 7C6, Canada Univ Montreal St Hyacinthe PQ Canada J2S 7C6 yacinthe, PQ J2S 7C6, Canada Univ Turin, Dept Internal Med, I-10124 Turin, Italy Univ Turin Turin Italy I-10124 , Dept Internal Med, I-10124 Turin, Italy Pharmacia & Upjohn Inc, Stockholm, Sweden Pharmacia & Upjohn Inc Stockholm Sweden & Upjohn Inc, Stockholm, Sweden Montreal Heart Inst, Montreal, PQ H1T 1C8, Canada Montreal Heart Inst Montreal PQ Canada H1T 1C8 ntreal, PQ H1T 1C8, Canada
Titolo Testata:
CIRCULATION RESEARCH
fascicolo: 9, volume: 85, anno: 1999,
pagine: 796 - 802
SICI:
0009-7330(19991029)85:9<796:IACOAN>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-KINASE-C; RAT-HEART; PITUITARY; BINDING; SECRETAGOGUES; HEXARELIN; INHIBITOR; SUBTYPES; FAILURE; MUSCLE;
Keywords:
growth hormone-releasing peptide; receptor; heart; photoaffinity labeling; Langendorff perfused heart;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
29
Recensione:
Indirizzi per estratti:
Indirizzo: Ong, H Univ Montreal, Fac Pharm, CP 6128,Succursale Ctr Ville, Montreal, PQ H3C 3J7, Canada Univ Montreal CP 6128,Succursale Ctr Ville Montreal PQ Canada H3C 3J7
Citazione:
V. Bodart et al., "Identification and characterization of a new growth hormone-releasing peptide receptor in the heart", CIRCUL RES, 85(9), 1999, pp. 796-802

Abstract

Hexarelin, a synthetic hexapeptide of the growth hormone-releasing peptide(GHRP) family with strong growth hormone (GH)-releasing activity, featuresprotecting: activity against postischemic ventricular dysfunction in hearts from GH-deficient and senescent rats. To document whether hexarelin action is mediated through specific cardiac receptors, perfusion of Langendorff rat hearts with hexarelin and binding studies were carried out. In the Langendorff rat heart system, hexarelin induced a dose-dependent increase in coronary perfusion pressure. Nifedipine, chelerythrine, and bisindolylmaleimide partially inhibited the vasoconstriction induced by hexarelin, suggesting that this effect was mediated at least in part by L-type Ca2+ channels and protein kinase C. In contrast, diclofenac and 1-(7-carboxyheptyl)imidazole were without effect, suggesting that prostaglandins and thromboxanes werenot involved in the coronary vasoconstriction induced by hexarelin. To characterize the hexarelin binding sites in the rat heart, [I-125]Tyr-Bpa-Ala-hexarelin was used as photoactivatable radioligand in saturation and competitive binding studies. We specifically labeled a hexarelin receptor with anM-r of 84 000 in rat cardiac membranes. Saturation binding curves revealeda single class of binding sites with a K-d of 14.5 nmol/L and a density of91 fmol/mg of protein. Competition binding studies gave an IC50 of 2.9 mu mol/L for hexarelin; MK-0677 and EP51389, both potent GH secretagogues, didnot displace the binding of the photoactivatable derivative from rat cardiac membranes. Interestingly, both compounds were devoid of any vasoconstrictive activity. These results suggest the existence of a new class of hexarelin receptor in the heart, whose role in the regulation of the coronary vascular tone is yet to be determined.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 18:34:56