α-Adrenergic supersensitivity and decreased number of α-adrenoceptors in heart from acute diabetic rats
The inotropic effect of methoxamine, as well as the α-adrenoceptor population, were measured in cardiac tissue from normal and short-term (3 days) diabetic rats. Methoxamine increased the tension of both normal and diabetic ventricles, but in diabetic ones, the dose-response curve to methoxamine was...
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| Otros Autores: | , |
| Formato: | Capítulo de libro |
| Lenguaje: | Inglés |
| Publicado: |
1988
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| Materias: | |
| Acceso en línea: | Registro en Scopus Handle Registro en la Biblioteca Digital |
| Aporte de: | Registro referencial: Solicitar el recurso aquí |
| LEADER | 04637caa a22006857a 4500 | ||
|---|---|---|---|
| 001 | PAPER-18052 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518204925.0 | ||
| 008 | 190411s1988 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-0023689819 | |
| 024 | 7 | |2 cas |a 1 (5 isoquinolinesulfonyl) 2 methylpiperazine, 84477-87-2; methoxamine, 390-28-3, 61-16-5; n (2 aminoethyl) 5 isoquinolinesulfonamide, 84468-17-7; phentolamine, 50-60-2, 73-05-2; prazosin, 19216-56-9, 19237-84-4; propranolol, 13013-17-7, 318-98-9, 3506-09-0, 4199-09-1, 525-66-6; Methoxamine, 390-28-3; Prazosin, 19216-56-9; Receptors, Adrenergic, alpha | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a CJPPA | ||
| 100 | 1 | |a Wald, M. | |
| 245 | 1 | 0 | |a α-Adrenergic supersensitivity and decreased number of α-adrenoceptors in heart from acute diabetic rats |
| 260 | |c 1988 | ||
| 506 | |2 openaire |e Política editorial | ||
| 520 | 3 | |a The inotropic effect of methoxamine, as well as the α-adrenoceptor population, were measured in cardiac tissue from normal and short-term (3 days) diabetic rats. Methoxamine increased the tension of both normal and diabetic ventricles, but in diabetic ones, the dose-response curve to methoxamine was shifted to the left and the efficacy of the α-agonist was enhanced. This phenomenon was accompanied by an increase in receptor affinity, while the number of α-adrenoceptor sites decreased. Inhibitors of α1-adrenoceptors blocked, in a competitive manner, the positive inotropic effect of methoxamine in both types of ventricles. Inhibition of phospholipase C blocked the ventricular response to the methoxamine in nondiabetic as well as in diabetic hearts. Synthetic diacylglyceride (DAG) potentiated the inotropic action of the α-agonist in normal ventricles and increased the affinity with a decreased number of α-adrenoceptor sites in normal ventricles, producing values of K(d) of B(max) similar to those of the acute diabetic heart. Inhibitors of protein kinase C partially reduced the supersensitivity to α-agonists in diabetic ventricles and prevented the stimulatory action of DAG upon the positive inotropic effect of methoxamine in normal ventricles. These results suggest that α-adrenergic inotropic stimulation is secondary to receptor-mediated hydrolysis of phosphoinositides, generating some oxidative metabolites (DAG) which, in turn, may be responsible for the inotropic effect. In the acute diabetic state, the supersensitivity to α-agonist could be due to high activity of phospholipase C (with an increase in DAG production) which induces alteration in the membrane α-adrenergic receptors. |l eng | |
| 593 | |a Centrol de Estudios Farmacologicos y de Principios Naturales (CEFAPRIN), Consejo Nacional de Investigaciones Cientificas, (1414) Buenos Aires, Argentina | ||
| 690 | 1 | 0 | |a 1 (5 ISOQUINOLINESULFONYL) 2 METHYLPIPERAZINE |
| 690 | 1 | 0 | |a ALPHA ADRENERGIC RECEPTOR |
| 690 | 1 | 0 | |a DIACYLGLYCEROL |
| 690 | 1 | 0 | |a METHOXAMINE |
| 690 | 1 | 0 | |a N (2 AMINOETHYL) 5 ISOQUINOLINESULFONAMIDE |
| 690 | 1 | 0 | |a PHENTOLAMINE |
| 690 | 1 | 0 | |a PRAZOSIN |
| 690 | 1 | 0 | |a PROPRANOLOL |
| 690 | 1 | 0 | |a ANIMAL CELL |
| 690 | 1 | 0 | |a ANIMAL EXPERIMENT |
| 690 | 1 | 0 | |a CONTROLLED STUDY |
| 690 | 1 | 0 | |a DIABETES MELLITUS |
| 690 | 1 | 0 | |a HEART VENTRICLE |
| 690 | 1 | 0 | |a INOTROPISM |
| 690 | 1 | 0 | |a MALE |
| 690 | 1 | 0 | |a NONHUMAN |
| 690 | 1 | 0 | |a PRIORITY JOURNAL |
| 690 | 1 | 0 | |a RAT |
| 690 | 1 | 0 | |a ANIMAL |
| 690 | 1 | 0 | |a DIABETES MELLITUS, EXPERIMENTAL |
| 690 | 1 | 0 | |a DOSE-RESPONSE RELATIONSHIP, DRUG |
| 690 | 1 | 0 | |a KINETICS |
| 690 | 1 | 0 | |a MALE |
| 690 | 1 | 0 | |a METHOXAMINE |
| 690 | 1 | 0 | |a MYOCARDIAL CONTRACTION |
| 690 | 1 | 0 | |a MYOCARDIUM |
| 690 | 1 | 0 | |a PRAZOSIN |
| 690 | 1 | 0 | |a RATS |
| 690 | 1 | 0 | |a RATS, INBRED STRAINS |
| 690 | 1 | 0 | |a RECEPTORS, ADRENERGIC, ALPHA |
| 690 | 1 | 0 | |a SUPPORT, NON-U.S. GOV'T |
| 653 | 0 | 0 | |a h 9, sigma; h7, sigma |
| 700 | 1 | |a Borda, E.S. | |
| 700 | 1 | |a Sterin-Borda, L. | |
| 773 | 0 | |d 1988 |g v. 66 |h pp. 1154-1160 |k n. 9 |p CAN. J. PHYSIOL. PHARMACOL. |x 00084212 |w (AR-BaUEN)CENRE-2805 |t Canadian Journal of Physiology and Pharmacology | |
| 856 | 4 | 1 | |u https://www.scopus.com/inward/record.uri?eid=2-s2.0-0023689819&partnerID=40&md5=980a2ce033a34b48e5784d6cba828980 |y Registro en Scopus |
| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_00084212_v66_n9_p1154_Wald |y Handle |
| 856 | 4 | 0 | |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00084212_v66_n9_p1154_Wald |y Registro en la Biblioteca Digital |
| 961 | |a paper_00084212_v66_n9_p1154_Wald |b paper |c PE | ||
| 962 | |a info:eu-repo/semantics/article |a info:ar-repo/semantics/artículo |b info:eu-repo/semantics/publishedVersion | ||
| 999 | |c 79005 | ||