In Vitro Uptake of Benzodiazepines by Rat Pineal Gland
As a part of a study aiming to characterize the physiological and pharmacological significance of the high affinity pineal benzodiazepine (BZP) binding sites reported previously, we examined the uptake of the BZP derivative 3H‐flunitrazepam (FNZP) by rat pineal glands in vitro. At 37 °C, 3H‐radioact...
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1984
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| Acceso en línea: | Registro en Scopus DOI Handle Registro en la Biblioteca Digital |
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| LEADER | 07598caa a22009017a 4500 | ||
|---|---|---|---|
| 001 | PAPER-18316 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518204941.0 | ||
| 008 | 190411s1984 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-0021710841 | |
| 024 | 7 | |2 cas |a benzodiazepine, 12794-10-4; Flunitrazepam, 1622-62-4; Receptors, GABA-A | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 100 | 1 | |a Lowenstein, P.R. | |
| 245 | 1 | 3 | |a In Vitro Uptake of Benzodiazepines by Rat Pineal Gland |
| 260 | |c 1984 | ||
| 270 | 1 | 0 | |m Cardinali, D.P.; CEFAPRIN, Serrano 665/669, Buenos Aires, 1414, Argentina |
| 506 | |2 openaire |e Política editorial | ||
| 504 | |a Asano, T., Ogasawara, N., Prostaglandin A as a possible endogenous ligand of benzodiazepine receptor (1982) Eur. J. Pharmacol., 80, pp. 271-274 | ||
| 504 | |a Chan, A., Ebadi, M., The kinetics of norepinephrine‐induced stimulation of serotonin‐N‐acetyltransferase in bovine pineal gland (1980) Neuroendocrinology, 31, pp. 224-251 | ||
| 504 | |a Ebadi, M., Chan, A., Characteristics of GABA binding sites in bovine pineal gland (1980) Brain Res. Bull, 5, pp. 179-187 | ||
| 504 | |a Haefely, W., Polc, P., Pieri, R., Schaffner, R., Laurent, J.‐P., Neuropharmacology of benzodiazepines: Synaptic mechanisms and neural basis of action (1983) The Benzodiazepines: From Molecular Biology to Clinical Practice, pp. 21-66. , E. Costa, Raven Press, New York, pp | ||
| 504 | |a Hamon, M., Soubrié, P., Searching for endogenous ligand(s) of central benzodiazepine receptors (1983) Neurochem. Int., 5, pp. 663-672 | ||
| 504 | |a Kari, L., 6‐Methoxy‐l, 2, 3, 4‐tetrahydro‐β‐carboline in pineal gland of chicken and cock (1981) FEES Lett., 127, pp. 277-280 | ||
| 504 | |a Lowenstein, P.R., Cardinali, D.P., Benzodiazepine receptor sites in bovine pineal (1983) Eur. J. Pharmacol., 86, pp. 287-289 | ||
| 504 | |a Lowenstein, P.R., Cardinali, D.P., Characterization of flunitrazepam and beta‐carboline high affinity binding in bovine pineal gland (1983) Neuroendocrinology, 37, pp. 150-154 | ||
| 504 | |a Marangos, P.J., Patel, J., Hirata, F., Sonhein, D., Paul, S.M., Skolnick, P., Goodwin, F.K., Inhibition of diazepam binding by tryptophan derivatives including melatonin and its brain metabolite N‐acety1‐5‐methoxy kynurenamine (1981) Life Sci., 29, pp. 259-267 | ||
| 504 | |a Mata, M., Schrier, B.K., Klein, D.C., Weller, J.L., Chiou, C.T., On GABA function and physiology in the pineal gland (1976) Brain Res., 118, pp. 384-394 | ||
| 504 | |a Möhler, H., Pole, P., Cumin, R., Pieri, L., Kettler, R., Nicotinamide is a brain constituent with benzodiazepine‐like actions (1979) Nature, 278, pp. 563-565 | ||
| 504 | |a Olsen, R.W., GABA‐benzodiazepine‐barbiturate receptor interactions (1981) J. Neurochem., 37, pp. 1-13 | ||
| 504 | |a Rommelspacher, H., The β‐carbolines (harmanes)—a new class of endogenous compounds. Their relevance for the pathogenesis and treatment of psychiatric and neurological diseases (1981) Pharmacopsychiatry, 14, pp. 117-125 | ||
| 504 | |a Skolnic, P., Marangos, P.J., Goodwin, F.K., Edwards, M., Paul, S., Identification of inosine and hypoxanthine as endogenous inhibitors of 3H‐diazepam binding in the central nervous system (1978) Life Sci., 23, pp. 1473-1480 | ||
| 504 | |a Snedecor, G.W., Cochran, W.G., (1967) Statistical Methods, , ed.6, Iowa State University Press, Ames | ||
| 504 | |a Tallman, J.F., Mallorga, P., Thomas, J.W., Gallager, D.W., Benzodiazepine binding sites. Properties and modulation (1981) GABA and Benzodiazepine Receptors, pp. 9-18. , E. Costa, G.D. Chiara, G.L. Gessa, Raven, New York, pp | ||
| 504 | |a Toffano, G., GABA receptor function (1983) Neural Transmission, Learning and Memory, pp. 97-104. , R. Caputto, C. Ajmone Marsan, Raven, New York, pp | ||
| 504 | |a Waniewski, R.A., Suria, A., Modulation of cyclic GMP in the rat pineal gland by GABA (1980) Brain Res. Bull., 5, pp. 347-354 | ||
| 520 | 3 | |a As a part of a study aiming to characterize the physiological and pharmacological significance of the high affinity pineal benzodiazepine (BZP) binding sites reported previously, we examined the uptake of the BZP derivative 3H‐flunitrazepam (FNZP) by rat pineal glands in vitro. At 37 °C, 3H‐radioactivity was taken up by tissue up to a pineal/medium concentration of about 12, while at 0 °C the uptake amounted to only one‐third that at 37 °C. Reciprocal of uptake analyzed by Lineweaver‐Burk plots indicated apparent Km's of 1.74 and 1.45 μM, and Vmax's of 1.32 and 1.04 pmol per min per mg tissue, for control and superior cervical ganglionectomized rats, respectively, suggesting that the neural compartment does not participate significantly in 3H‐FNZP uptake. Cerebral cortex explants of similar size and weight as the pineal ones took up 3H‐FNZP to a maximum tissue/ medium concentration of about 2. Neither pineal nor cerebral cortex 3H‐radioactivity uptake exhibited significant changes as a function of time of day. A number of agents, including several BZP analogues, cocaine, desipramine, melatonin, fluoxetine, nomifensine, and dipiridamol, as well as changes in the ionic environment or metabolic inhibitors, did not affect 3H‐FNZP uptake significantly. Other tissues, such as liver, muscle, kidney, adrenal gland, or anterior pituitary, took up 3H‐radioactivity to tissue concentrations slightly lower than those of the cerebral cortex, suggesting that drug liposolubility accounted only to a limited extent for the high in vitro uptake detected in incubated pineals. Copyright © 1984, Wiley Blackwell. All rights reserved |l eng | |
| 593 | |a Centro de Estudios Farmacologicos y de Principios Naturales (CEFAPRIN), Buenos Aires, Argentina | ||
| 690 | 1 | 0 | |a BENZODIAZEPINE UPTAKE |
| 690 | 1 | 0 | |a DIURNAL RHYTHMS |
| 690 | 1 | 0 | |a PINEAL GLAND |
| 690 | 1 | 0 | |a SUPERIOR CERVICAL GANGLIONECTOMY |
| 690 | 1 | 0 | |a BENZODIAZEPINE |
| 690 | 1 | 0 | |a BENZODIAZEPINE RECEPTOR |
| 690 | 1 | 0 | |a RADIOISOTOPE |
| 690 | 1 | 0 | |a ANIMAL CELL |
| 690 | 1 | 0 | |a CENTRAL NERVOUS SYSTEM |
| 690 | 1 | 0 | |a CIRCADIAN RHYTHM |
| 690 | 1 | 0 | |a DRUG ACCUMULATION |
| 690 | 1 | 0 | |a DRUG RECEPTOR BINDING |
| 690 | 1 | 0 | |a ENDOCRINE SYSTEM |
| 690 | 1 | 0 | |a FLUNITRAZEPAM H 3 |
| 690 | 1 | 0 | |a NONHUMAN |
| 690 | 1 | 0 | |a PHARMACOKINETICS |
| 690 | 1 | 0 | |a PINEAL BODY |
| 690 | 1 | 0 | |a RAT |
| 690 | 1 | 0 | |a SUPERIOR CERVICAL GANGLIONECTOMY |
| 690 | 1 | 0 | |a ANIMAL |
| 690 | 1 | 0 | |a BIOLOGICAL TRANSPORT |
| 690 | 1 | 0 | |a CEREBRAL CORTEX |
| 690 | 1 | 0 | |a FEMALE |
| 690 | 1 | 0 | |a FLUNITRAZEPAM |
| 690 | 1 | 0 | |a KINETICS |
| 690 | 1 | 0 | |a ORGAN SPECIFICITY |
| 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 |
| 700 | 1 | |a Solveyra, C.G. | |
| 700 | 1 | |a Cardinali, D.P. | |
| 773 | 0 | |d 1984 |g v. 1 |h pp. 207-213 |k n. 3 |p J. Pineal Res. |x 07423098 |t Journal of Pineal Research | |
| 856 | 4 | 1 | |u https://www.scopus.com/inward/record.uri?eid=2-s2.0-0021710841&doi=10.1111%2fj.1600-079X.1984.tb00212.x&partnerID=40&md5=8a456cce1d7b88c4bcbf4f6aa7c00e97 |y Registro en Scopus |
| 856 | 4 | 0 | |u https://doi.org/10.1111/j.1600-079X.1984.tb00212.x |y DOI |
| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_07423098_v1_n3_p207_Lowenstein |y Handle |
| 856 | 4 | 0 | |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_07423098_v1_n3_p207_Lowenstein |y Registro en la Biblioteca Digital |
| 961 | |a paper_07423098_v1_n3_p207_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 79269 | ||