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Titolo:
EP 60761-and EP 50885-induced penile erection: structure-activity studies and comparison with apomorphine, oxytocin and N-methyl-D-aspartic acid
Autore:
Melis, MR; Spano, MS; Succu, S; Locatelli, V; Torsello, A; Muller, EE; Deghenghi, R; Argiolas, A;
Indirizzi:
Univ Cagliari, Bernard B Brodie Dept Neurosci, I-09124 Cagliari, Italy Univ Cagliari Cagliari Italy I-09124 t Neurosci, I-09124 Cagliari, Italy Univ Milan, Dept Pharmacol, I-20129 Milan, Italy Univ Milan Milan Italy I-20129 lan, Dept Pharmacol, I-20129 Milan, Italy Europeptides, Argenteuil, France Europeptides Argenteuil FranceEuropeptides, Argenteuil, France
Titolo Testata:
INTERNATIONAL JOURNAL OF IMPOTENCE RESEARCH
fascicolo: 5, volume: 12, anno: 2000,
pagine: 255 - 262
SICI:
0955-9930(200010)12:5<255:E6E5PE>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
PARAVENTRICULAR NITRIC-OXIDE; HORMONE-RELEASING PEPTIDE; OMEGA-CONOTOXIN; MALE-RATS; PITUITARY; HEXARELIN; BRAIN; HYPOTHALAMUS; SECRETAGOGUES; INVOLVEMENT;
Keywords:
penile erection; EP peptides; growth hormone (GH) releasing peptides; oxytocin; paraventricular nucleus of the hypothalamus rat;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
39
Recensione:
Indirizzi per estratti:
Indirizzo: Argiolas, A Univ Cagliari, Bernard B Brodie Dept Neurosci, Via Porcell 4, I-09124 Cagliari, Italy Univ Cagliari Via Porcell 4 Cagliari Italy I-09124ari, Italy
Citazione:
M.R. Melis et al., "EP 60761-and EP 50885-induced penile erection: structure-activity studies and comparison with apomorphine, oxytocin and N-methyl-D-aspartic acid", INT J IMPOT, 12(5), 2000, pp. 255-262

Abstract

The effect of 10 peptides structurally related to the growth hormone (GH) releasing peptide hexarelin, injected into the paraventricular nucleus of the hypothalamus (PVN), on penile erection was studied in male rats. Six outof the 10 peptides tested induced penile erection in a dose-dependent manner. Among them, the most potent were EP 80661, EP 60761 and EP 91072, whichwere active at doses of 20-200 ng. The potency of these peptides in inducing penile erection is comparable to that of apomorphine, oxytocin and N-methyl-D-aspartic acid similarly injected into the PVN. Other peptides found active were EP 50885, EP 90101 and EP 91071, which induced penile erection at doses of zoo - 2000 ng. In contrast, EP 51322, EP 70555, EP 51216 and EP 91073 were inactive, as were hexarelin, EP 40904 and EP 40737 in a previousstudy. The majority of EP peptides found active when injected into the PVNinduced penile erection, although to a lesser extent, also when given systemically (endovenously). The proerectile effect of EP peptides was prevented by the oxytocin receptor antagonist [d(CH2)(5) Tyr(Me)(2)-Orn(8)]-vasotocin given into the lateral ventricles but not into the PVN, by the nitric oxide (NO) synthase inhibitor N-G-nitro-l-arginine methyl ester given either into the lateral ventricles or into the PVN, by the N-type Ca2+ channel blocker omega -conotoxin GVIA and by morphine, but not by the dopamine receptor antagonist cis-flupenthixol or by the N-methyl-D-aspartic acid receptor antagonist dizolcipine, given into the PVN. As the structure - activity relationship of EP peptides for proerectile activity is different from those ofother biological actions of these compounds, ie for GH release and eating behaviour, the present results suggest that EP peptides induce penile erection by acting on specific hypothalamic receptor sites that activate paraventricular oxytocinergic neurons projecting to extrahypothalamic brain areas that mediate this sexual function by a mechanism similar to that of dopamine receptor agonists, oxytocin and N-methyl-D-aspartic acid.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 15/07/20 alle ore 08:51:04