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Abstract:

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

Registro:

Documento: Artículo
Título:In Vitro Uptake of Benzodiazepines by Rat Pineal Gland
Autor:Lowenstein, P.R.; Solveyra, C.G.; Cardinali, D.P.
Filiación:Centro de Estudios Farmacologicos y de Principios Naturales (CEFAPRIN), Buenos Aires, Argentina
Palabras clave:benzodiazepine uptake; diurnal rhythms; pineal gland; superior cervical ganglionectomy; benzodiazepine; benzodiazepine receptor; radioisotope; animal cell; central nervous system; circadian rhythm; drug accumulation; drug receptor binding; endocrine system; flunitrazepam h 3; nonhuman; pharmacokinetics; pineal body; rat; superior cervical ganglionectomy; Animal; Biological Transport; Cerebral Cortex; Female; Flunitrazepam; Kinetics; Organ Specificity; Pineal Gland; Rats; Rats, Inbred Strains; Receptors, GABA-A; Support, Non-U.S. Gov't
Año:1984
Volumen:1
Número:3
Página de inicio:207
Página de fin:213
DOI: http://dx.doi.org/10.1111/j.1600-079X.1984.tb00212.x
Título revista:Journal of Pineal Research
Título revista abreviado:J. Pineal Res.
ISSN:07423098
CAS:benzodiazepine, 12794-10-4; Flunitrazepam, 1622-62-4; Receptors, GABA-A
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_07423098_v1_n3_p207_Lowenstein

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Citas:

---------- APA ----------
Lowenstein, P.R., Solveyra, C.G. & Cardinali, D.P. (1984) . In Vitro Uptake of Benzodiazepines by Rat Pineal Gland. Journal of Pineal Research, 1(3), 207-213.
http://dx.doi.org/10.1111/j.1600-079X.1984.tb00212.x
---------- CHICAGO ----------
Lowenstein, P.R., Solveyra, C.G., Cardinali, D.P. "In Vitro Uptake of Benzodiazepines by Rat Pineal Gland" . Journal of Pineal Research 1, no. 3 (1984) : 207-213.
http://dx.doi.org/10.1111/j.1600-079X.1984.tb00212.x
---------- MLA ----------
Lowenstein, P.R., Solveyra, C.G., Cardinali, D.P. "In Vitro Uptake of Benzodiazepines by Rat Pineal Gland" . Journal of Pineal Research, vol. 1, no. 3, 1984, pp. 207-213.
http://dx.doi.org/10.1111/j.1600-079X.1984.tb00212.x
---------- VANCOUVER ----------
Lowenstein, P.R., Solveyra, C.G., Cardinali, D.P. In Vitro Uptake of Benzodiazepines by Rat Pineal Gland. J. Pineal Res. 1984;1(3):207-213.
http://dx.doi.org/10.1111/j.1600-079X.1984.tb00212.x