Artículo
Lowenstein, P.R.; Rosenstein, R.; Caputti, E.; Cardinali, D.P. "Benzodiazepine binding sites in human pineal gland" (1984) European Journal of Pharmacology. 106(2):399-403
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Abstract:
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.
Registro:
| Documento: | Artículo |
| Título: | Benzodiazepine binding sites in human pineal gland |
| Autor: | Lowenstein, P.R.; Rosenstein, R.; Caputti, E.; Cardinali, D.P. |
| Filiación: | Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRIN), University of Buenos Aires, Buenos Aires, Argentina Faculty of Medicine, University of Buenos Aires, Buenos Aires, Argentina |
| Palabras clave: | Benzodiazepine receptors; Cerebral cortex; GABA; Human; Pineal gland; 4 aminobutyric acid; 4' chlorodiazepam; benzodiazepine derivative; benzodiazepine receptor; bicuculline; clonazepam; diazepam; flumazenil; flunitrazepam; radioisotope; brain cortex; central nervous system; drug binding; drug receptor binding; flunitrazepam h 3; human; human cell; normal human; pharmacokinetics; pineal body; priority journal; Adolescent; Adult; Aged; Animal; Benzodiazepinones; Binding, Competitive; Cerebral Cortex; Child; Child, Preschool; Clonazepam; Diazepam; Flumazenil; Flunitrazepam; gamma-Aminobutyric Acid; Human; In Vitro; Infant; Kinetics; Male; Middle Age; Pineal Gland; Rats; Rats, Inbred Strains; Receptors, GABA-A; Support, Non-U.S. Gov't |
| Año: | 1984 |
| Volumen: | 106 |
| Número: | 2 |
| Página de inicio: | 399 |
| Página de fin: | 403 |
| DOI: | http://dx.doi.org/10.1016/0014-2999(84)90728-3 |
| 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; 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 |
| Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00142999_v106_n2_p399_Lowenstein |
Referencias:
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Citas:
---------- APA ----------
Lowenstein, P.R., Rosenstein, R., Caputti, E. & Cardinali, D.P. (1984) . Benzodiazepine binding sites in human pineal gland. European Journal of Pharmacology, 106(2), 399-403.http://dx.doi.org/10.1016/0014-2999(84)90728-3
---------- CHICAGO ----------
Lowenstein, P.R., Rosenstein, R., Caputti, E., Cardinali, D.P. "Benzodiazepine binding sites in human pineal gland" . European Journal of Pharmacology 106, no. 2 (1984) : 399-403.http://dx.doi.org/10.1016/0014-2999(84)90728-3
---------- MLA ----------
Lowenstein, P.R., Rosenstein, R., Caputti, E., Cardinali, D.P. "Benzodiazepine binding sites in human pineal gland" . European Journal of Pharmacology, vol. 106, no. 2, 1984, pp. 399-403.http://dx.doi.org/10.1016/0014-2999(84)90728-3
---------- VANCOUVER ----------
Lowenstein, P.R., Rosenstein, R., Caputti, E., Cardinali, D.P. Benzodiazepine binding sites in human pineal gland. Eur. J. Pharmacol. 1984;106(2):399-403.http://dx.doi.org/10.1016/0014-2999(84)90728-3
