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Abstract:

Catecholestrogen (CE) binding to guinea-pig hypothalamic membranes was assessed by using [3H]2-hydroxyestrone (2-OHE2) as a ligand. Binding was maximal at pH 7.4 and 37°C, and after 10 min incubations. A high affinity binding site with dissociation constant (KD) = 0.20 ± 0.02 nM and site concentration (Bmax) = 38 ± 2 fmol/mg protein, and a low affinity binding site with KD = 235 ± 10 nM and Bmax = 4.2 ± 1.0 pmol/mg protein (n = 7) were detected. The order of affinity (Ki, μM) for displacement of 10 nM [3H]2-OHE1 from hypothalamic binding sites was 2-OHE1 (0.8), 2-hydroxyestradiol (2-OHE2) (1.0), epinephrine (5.9), norepinephrine (NE) (7.7), dopamine (270), estradiol, estrone, propranolol, phentolamine, domperidone (>10 000). NE inhibition of 2-OHE1 binding was non-competitive, Only 0.5 mM 2-OHE2 depressed in a non-competitive way the hypothalamic β-adrenoceptor binding (measured by using [3H]dihydroalprenolol) without affecting α-adrenoceptor binding (measured by using [3H]dihydroergocryptine). Both 2-OHE2 and 2-OHE1 impaired NE-stimulated adenylate cyclase activity in hypothalamic membranes with EC50 of about 5 and 10 μM, respectively. CE decreased [3H]γ-aminobutyric acid binding by hypothalamic membranes with Ki = 8 μM (2-OHE2) and 50 μM (2-OHE1). The binding of [3H]flunitrazepam to the same membrane preparation was not affected by CE. These results support the existence of significant CE binding and effects in guinea-pig hypothalamic membranes. © 1986.

Registro:

Documento: Artículo
Título:Binding and effects of catecholestrogens on adenylate cyclase activity, and adrenoceptors, benzodiazepine and GABA receptors in guinea-pig hypothalamic membranes
Autor:Etchegoyen, G.S.; Cardinali, D.P.; Pérez, A.E.; Tamayo, J.; Pérez-Palacios, G.
Filiación:Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRin), Buenos Aires, Argentina
Departmentos de Biología de la Reproducción, Instituto Nacional de la Nutrición Salvador Zubirán, Universidad Autónoma Metropolitana, Iztapalapa, Mexico, D.F., Mexico
Palabras clave:Adenylate cyclase; Adrenoceptor binding; Benzodiazepine binding; Catecholestrogens; GABAergic binding; Hypothalamus; 2 hydroxyestradiol; 2 hydroxyestrone; 2 hydroxyestrone h 3; 4 aminobutyric acid h 3; 4 aminobutyric acid receptor; adenylate cyclase; adrenalin; alpha adrenergic receptor; benzodiazepine receptor; beta adrenergic receptor; catechol estrogen; dihydroalprenolol h 3; dihydroergocryptine h 3; domperidone; dopamine; estradiol; estrone; flunitrazepam h 3; noradrenalin; phentolamine; propranolol; radioisotope; unclassified drug; animal cell; article; central nervous system; drug binding; drug receptor binding; guinea pig; hypothalamus; nervous system; nonhuman; pharmacokinetics; priority journal; synaptosome; Adenylate Cyclase; Animals; Binding, Competitive; Cell Membrane; Enzyme Activation; Estrogens, Catechol; Guinea Pigs; Hypothalamus; Norepinephrine; Receptors, Adrenergic; Receptors, GABA-A
Año:1986
Volumen:129
Número:1-2
Página de inicio:1
Página de fin:10
DOI: http://dx.doi.org/10.1016/0014-2999(86)90329-8
Título revista:European Journal of Pharmacology
Título revista abreviado:Eur. J. Pharmacol.
ISSN:00142999
CODEN:EJPHA
CAS:2 hydroxyestradiol, 362-05-0; 2 hydroxyestrone, 362-06-1, 39455-26-0; adenylate cyclase, 9012-42-4; adrenalin, 51-43-4, 55-31-2, 6912-68-1; domperidone, 57808-66-9; dopamine, 51-61-6, 62-31-7; estradiol, 50-28-2; estrone, 53-16-7; noradrenalin, 1407-84-7, 51-41-2; phentolamine, 50-60-2, 73-05-2; propranolol, 13013-17-7, 318-98-9, 3506-09-0, 4199-09-1, 525-66-6; Adenylate Cyclase, 4.6.1.1; Estrogens, Catechol; Norepinephrine, 51-41-2; Receptors, Adrenergic; Receptors, GABA-A
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00142999_v129_n1-2_p1_Etchegoyen

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Citas:

---------- APA ----------
Etchegoyen, G.S., Cardinali, D.P., Pérez, A.E., Tamayo, J. & Pérez-Palacios, G. (1986) . Binding and effects of catecholestrogens on adenylate cyclase activity, and adrenoceptors, benzodiazepine and GABA receptors in guinea-pig hypothalamic membranes. European Journal of Pharmacology, 129(1-2), 1-10.
http://dx.doi.org/10.1016/0014-2999(86)90329-8
---------- CHICAGO ----------
Etchegoyen, G.S., Cardinali, D.P., Pérez, A.E., Tamayo, J., Pérez-Palacios, G. "Binding and effects of catecholestrogens on adenylate cyclase activity, and adrenoceptors, benzodiazepine and GABA receptors in guinea-pig hypothalamic membranes" . European Journal of Pharmacology 129, no. 1-2 (1986) : 1-10.
http://dx.doi.org/10.1016/0014-2999(86)90329-8
---------- MLA ----------
Etchegoyen, G.S., Cardinali, D.P., Pérez, A.E., Tamayo, J., Pérez-Palacios, G. "Binding and effects of catecholestrogens on adenylate cyclase activity, and adrenoceptors, benzodiazepine and GABA receptors in guinea-pig hypothalamic membranes" . European Journal of Pharmacology, vol. 129, no. 1-2, 1986, pp. 1-10.
http://dx.doi.org/10.1016/0014-2999(86)90329-8
---------- VANCOUVER ----------
Etchegoyen, G.S., Cardinali, D.P., Pérez, A.E., Tamayo, J., Pérez-Palacios, G. Binding and effects of catecholestrogens on adenylate cyclase activity, and adrenoceptors, benzodiazepine and GABA receptors in guinea-pig hypothalamic membranes. Eur. J. Pharmacol. 1986;129(1-2):1-10.
http://dx.doi.org/10.1016/0014-2999(86)90329-8