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Abstract:

[3H]Flunitrazepam (FNZP) binds to a single class of high affinity binding sites in bovine pineal membranes (KD 2.8 nM). FNZP binding increased by 25% after exposure to γ-aminobutyric acid and exhibits a high degree of specificity for drugs acting on the central type of benzodiazepine receptor. High affinity binding of [3H]ethyl-3-carboline ester to pineal membranes has a KD 0.8 nM and about 60% of the maximal number of FNZP binding sites. © 1983.

Registro:

Documento: Artículo
Título:Benzodiazepine receptor sites in bovine pineal
Autor:Lowenstein, P.R.; Cardinali, D.P.
Filiación:Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRIN), Serrano 665/, 669 Buenos Aires, Argentina
Palabras clave:Benzodiazepine binding; Pineal gland; β-Carboline binding; 4 aminobutyric acid; 4' chlorodiazepam; benzodiazepine; benzodiazepine receptor; chlordiazepoxide; clonazepam; flumazenil; flunitrazepam; radioisotope; animal cell; beta carboline 3 carboxylic acid ethyl ester h 3; cattle; cell membrane; central nervous system; drug receptor binding; endocrine system; flunitrazepam h 3; nonhuman; pharmacokinetics; pineal body; Animal; Cattle; Flunitrazepam; gamma-Aminobutyric Acid; In Vitro; Kinetics; Membranes; Pineal Gland; Receptors, Cell Surface; Receptors, GABA-A; Support, Non-U.S. Gov't
Año:1982
Volumen:86
Número:2
Página de inicio:287
Página de fin:289
DOI: http://dx.doi.org/10.1016/0014-2999(82)90329-6
Título revista:European Journal of Pharmacology
Título revista abreviado:Eur. J. Pharmacol.
ISSN:00142999
CODEN:EJPHA
CAS:4 aminobutyric acid, 28805-76-7, 56-12-2; 4' chlorodiazepam, 14439-61-3; benzodiazepine, 12794-10-4; chlordiazepoxide, 438-41-5, 58-25-3; clonazepam, 1622-61-3; flumazenil, 78755-81-4; flunitrazepam, 1622-62-4; Flunitrazepam, 1622-62-4; gamma-Aminobutyric Acid, 56-12-2; Receptors, Cell Surface; Receptors, GABA-A
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00142999_v86_n2_p287_Lowenstein

Referencias:

  • Baestrup, Nielsen, [3H]Propyl-β-carboline-3-carboxylate as a selective radioligand for BZ1 benzodiazepine receptor subclass (1981) J. Neurochem., 37, p. 333
  • Braestrup, Squires, Specific benzodiazepine receptors in rat brain characterized by high-affinity 3H-diazepam binding (1977) Proc. Natl. Acad. Sci. U.S.A., 74, p. 3805
  • Ebadi, Chan, Characteristics of GABA binding sites in bovine pineal gland (1980) Brain Res. Bull., 5, p. 179
  • Grandison, Cavagnini, Schmid, Invitti, Guidotti, γ-Aminobutyric acid and benzodiazepine binding sites in human anterior pituitary tissue (1982) J. Clin. Endocr., 54, p. 597
  • Kari, 6-Methoxy-1,2,3,4-tetrahydro-β-carboline in pineal gland of chicken and cock (1981) FEBS Lett., 127, p. 277
  • Marangos, Patel, Hirata, Sondhein, Paul, Skolnick, Goodwin, Inhibition of diazepam binding by tryptophan derivatives including melatonin and its brain metabolite N-acetyl-5-methoxy kynurenamine (1981) Life Sci., 29, p. 259
  • Möhler, Burkard, Keller, Richards, Haefely, Benzodiazepine antagonist Ro 15–1788 Binding characteristics and interaction with drug-induced changes in dopamine turnover and cerebellar cGMP levels (1981) Journal of Neurochemistry, 37, p. 714.L
  • Richards, Möhler, Haefely, Benzodiazepine binding sites: receptors or acceptors? (1982) Trends Pharmacol. Sci., 3, p. 233
  • Speth, Wastek, Johnson, Yamamura, Benzodiazepine binding in human brain: characterization using 3H-Flunitrazepam (1978) Life Sci., 22, p. 859
  • Tallman, Mallorga, Thomas, Gallager, Benzodiazepine binding sites: properties and modulation (1981) GABA and Benzodiazepine Receptors, p. 9. , E. Costa, G. di Chiara, G.L. Gessa, Raven Press, New York

Citas:

---------- APA ----------
Lowenstein, P.R. & Cardinali, D.P. (1982) . Benzodiazepine receptor sites in bovine pineal. European Journal of Pharmacology, 86(2), 287-289.
http://dx.doi.org/10.1016/0014-2999(82)90329-6
---------- CHICAGO ----------
Lowenstein, P.R., Cardinali, D.P. "Benzodiazepine receptor sites in bovine pineal" . European Journal of Pharmacology 86, no. 2 (1982) : 287-289.
http://dx.doi.org/10.1016/0014-2999(82)90329-6
---------- MLA ----------
Lowenstein, P.R., Cardinali, D.P. "Benzodiazepine receptor sites in bovine pineal" . European Journal of Pharmacology, vol. 86, no. 2, 1982, pp. 287-289.
http://dx.doi.org/10.1016/0014-2999(82)90329-6
---------- VANCOUVER ----------
Lowenstein, P.R., Cardinali, D.P. Benzodiazepine receptor sites in bovine pineal. Eur. J. Pharmacol. 1982;86(2):287-289.
http://dx.doi.org/10.1016/0014-2999(82)90329-6