Benzodiazepine binding sites in human pineal gland
The high affinity binding of [3H]flunitrazepam (FNZP) to crude membrane preparations was examined in human pineal glands. Scatchard analysis of the data at equilibrium revealed a single population of binding sites with dissociation constant = 2.36-2.53 nM and binding site concentration = 59-108 fmol...
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| Formato: | Capítulo de libro |
| Lenguaje: | Inglés |
| Publicado: |
1984
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| Acceso en línea: | Registro en Scopus DOI Handle Registro en la Biblioteca Digital |
| Aporte de: | Registro referencial: Solicitar el recurso aquí |
| LEADER | 07161caa a22011297a 4500 | ||
|---|---|---|---|
| 001 | PAPER-18272 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518204938.0 | ||
| 008 | 190411s1984 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-0021738559 | |
| 024 | 7 | |2 cas |a 4 aminobutyric acid, 28805-76-7, 56-12-2; 4' chlorodiazepam, 14439-61-3; bicuculline, 485-49-4; clonazepam, 1622-61-3; diazepam, 439-14-5; flumazenil, 78755-81-4; flunitrazepam, 1622-62-4; Benzodiazepinones; Clonazepam, 1622-61-3; Diazepam, 439-14-5; Flumazenil, 78755-81-4; Flunitrazepam, 1622-62-4; gamma-Aminobutyric Acid, 56-12-2; Receptors, GABA-A | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a EJPHA | ||
| 100 | 1 | |a Lowenstein, P.R. | |
| 245 | 1 | 0 | |a Benzodiazepine binding sites in human pineal gland |
| 260 | |c 1984 | ||
| 270 | 1 | 0 | |m Cardinali, D.P.; Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRIN), University of Buenos Aires, Buenos Aires, Argentina |
| 506 | |2 openaire |e Política editorial | ||
| 504 | |a Bennett, Jr., Methods in binding studies (1978) Neurotransmitter Receptor Binding, p. 57. , H.I. Yamamura, S.J. Enna, M.J. Kuhar, Raven, New York | ||
| 504 | |a Ebadi, Chan, Itoh, Hammad, Swanson, Govitrapong, The role of γ-aminobutyric acid in regulation of melatonin synthesis in bovine pineal gland (1984) Dynamics of Neurotransmitter Function, p. 177. , I. Hanin, Raven, New York | ||
| 504 | |a Haefely, Bonetti, Burkard, Cumin, Laurent, Möhler, Pieri, Scherschlicht, Benzodiazepine antagonists (1983) The Benzodiazepines: From Molecular Biology to Clinical Practice, p. 134. , E. Costa, Raven, New York | ||
| 504 | |a Haefely, Polc, Pieri, Schaffner, Laurent, Neuropharmacology of benzodiazepines: synaptic mechanisms and neural basis of action (1983) The Benzodiazepines: From Biology to Clinical Practice, p. 21. , E. Costa, Raven, New York | ||
| 504 | |a Lowenstein, Cardinali, Characterization of flunitrazepam and beta-carboline high affinity binding in bovine pineal gland (1983) Neuroendocrinology, 37, p. 150 | ||
| 504 | |a Maggi, Satinover, Oberdorfer, Mann, Enna, Phylogenetic characteristics of muscimolactivated benzodiazepine receptor binding (1980) Brain Res. Bull., 5, p. 167 | ||
| 504 | |a Matthew, Parfitt, Sugden, Engelhardt, Zimmerman, Klein, Benzodiazepines: rat pinealocyte binding sites and augmentation of norepinephrine-stimulated N-acetyltransferase activity (1984) J. Pharmacol. Exp. Ther., 228, p. 434 | ||
| 504 | |a Müller, The benzodiazepine receptor, an update (1981) Pharmacology, 22, p. 153 | ||
| 504 | |a Olsen, GABA-benzodiazepine-barbiturate receptor interactions (1981) J. Neurochem., 37, p. 1 | ||
| 504 | |a Tallman, Mallorga, Thomas, Gallager, Benzodiazepine binding sites. Properties and modulation (1981) Neuropharmacology of Central Nervous System and Behavioral disorders, p. 9. , E. Costa, G. Di Chiara, G.L. Gessa, Raven, New York | ||
| 520 | 3 | |a The high affinity binding of [3H]flunitrazepam (FNZP) to crude membrane preparations was examined in human pineal glands. Scatchard analysis of the data at equilibrium revealed a single population of binding sites with dissociation constant = 2.36-2.53 nM and binding site concentration = 59-108 fmol/mg protein. When various benzodiazepine (BZP) analogues were tested for their ability to inhibit [3H]FNZP binding the following Ki (nM) were found: clonazepam (0.13), RO 15-1788 (0.60), FNZP (2.14), diazepam (13.5), Ro 5-4864 (>10000). In both human pineal gland and cerebral cortex 10-100 μM γ-aminobutyric acid (GABA) increased BZP binding by about 30%, an effect inhibited by the GABA receptor blocker bicuculline. The stimulatory effect of GABA on [3H]FNZP binding in rat cerebral cortex (about 60%) decreased as a function of time elapsed postmortem at room temperature to reach values similar to those observed in human brains. These results suggest the existence of central type BZP receptors in the human pineal glands. © 1984. |l eng | |
| 536 | |a Detalles de la financiación: Dipartimento della Protezione Civile, Presidenza del Consiglio dei Ministri | ||
| 536 | |a Detalles de la financiación: Consejo Nacional de Investigaciones Científicas y Técnicas | ||
| 536 | |a Detalles de la financiación: These studies were supported by grant No. 6638 from CONICET, Argentina, and by Hoechst AG, Werk Albert Wiesbaden, F.R.G. PRL holds a Postdoctoral Research Fellowship from CONICET and DPC is an Established Investigator, CONICET. | ||
| 593 | |a Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRIN), University of Buenos Aires, Buenos Aires, Argentina | ||
| 593 | |a Faculty of Medicine, University of Buenos Aires, Buenos Aires, Argentina | ||
| 690 | 1 | 0 | |a BENZODIAZEPINE RECEPTORS |
| 690 | 1 | 0 | |a CEREBRAL CORTEX |
| 690 | 1 | 0 | |a GABA |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a PINEAL GLAND |
| 690 | 1 | 0 | |a 4 AMINOBUTYRIC ACID |
| 690 | 1 | 0 | |a 4' CHLORODIAZEPAM |
| 690 | 1 | 0 | |a BENZODIAZEPINE DERIVATIVE |
| 690 | 1 | 0 | |a BENZODIAZEPINE RECEPTOR |
| 690 | 1 | 0 | |a BICUCULLINE |
| 690 | 1 | 0 | |a CLONAZEPAM |
| 690 | 1 | 0 | |a DIAZEPAM |
| 690 | 1 | 0 | |a FLUMAZENIL |
| 690 | 1 | 0 | |a FLUNITRAZEPAM |
| 690 | 1 | 0 | |a RADIOISOTOPE |
| 690 | 1 | 0 | |a BRAIN CORTEX |
| 690 | 1 | 0 | |a CENTRAL NERVOUS SYSTEM |
| 690 | 1 | 0 | |a DRUG BINDING |
| 690 | 1 | 0 | |a DRUG RECEPTOR BINDING |
| 690 | 1 | 0 | |a FLUNITRAZEPAM H 3 |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a HUMAN CELL |
| 690 | 1 | 0 | |a NORMAL HUMAN |
| 690 | 1 | 0 | |a PHARMACOKINETICS |
| 690 | 1 | 0 | |a PINEAL BODY |
| 690 | 1 | 0 | |a PRIORITY JOURNAL |
| 690 | 1 | 0 | |a ADOLESCENT |
| 690 | 1 | 0 | |a ADULT |
| 690 | 1 | 0 | |a AGED |
| 690 | 1 | 0 | |a ANIMAL |
| 690 | 1 | 0 | |a BENZODIAZEPINONES |
| 690 | 1 | 0 | |a BINDING, COMPETITIVE |
| 690 | 1 | 0 | |a CEREBRAL CORTEX |
| 690 | 1 | 0 | |a CHILD |
| 690 | 1 | 0 | |a CHILD, PRESCHOOL |
| 690 | 1 | 0 | |a CLONAZEPAM |
| 690 | 1 | 0 | |a DIAZEPAM |
| 690 | 1 | 0 | |a FLUMAZENIL |
| 690 | 1 | 0 | |a FLUNITRAZEPAM |
| 690 | 1 | 0 | |a GAMMA-AMINOBUTYRIC ACID |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a IN VITRO |
| 690 | 1 | 0 | |a INFANT |
| 690 | 1 | 0 | |a KINETICS |
| 690 | 1 | 0 | |a MALE |
| 690 | 1 | 0 | |a MIDDLE AGE |
| 690 | 1 | 0 | |a PINEAL GLAND |
| 690 | 1 | 0 | |a RATS |
| 690 | 1 | 0 | |a RATS, INBRED STRAINS |
| 690 | 1 | 0 | |a RECEPTORS, GABA-A |
| 690 | 1 | 0 | |a SUPPORT, NON-U.S. GOV'T |
| 653 | 0 | 0 | |a ro 15 1788; ro 5 4864 |
| 700 | 1 | |a Rosenstein, R. | |
| 700 | 1 | |a Caputti, E. | |
| 700 | 1 | |a Cardinali, D.P. | |
| 773 | 0 | |d 1984 |g v. 106 |h pp. 399-403 |k n. 2 |p Eur. J. Pharmacol. |x 00142999 |w (AR-BaUEN)CENRE-1772 |t European Journal of Pharmacology | |
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| 856 | 4 | 0 | |u https://doi.org/10.1016/0014-2999(84)90728-3 |y DOI |
| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_00142999_v106_n2_p399_Lowenstein |y Handle |
| 856 | 4 | 0 | |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00142999_v106_n2_p399_Lowenstein |y Registro en la Biblioteca Digital |
| 961 | |a paper_00142999_v106_n2_p399_Lowenstein |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 79225 | ||