Artículo
Abstract:
High affinity binding of melatonin in crude membrane preparations of bovine brain was examined by a rapid filtration procedure through Whatman GFB paper. Melatonin binding to medial basal hypothalamic (MBH) membranes attained its maximum at the first, third, and fifth hours of incubation at. 37, 18, and 0 C, respectively. Specific binding was linear up to 3 mg membrane protein, was thermolabile, and decreased after incubation with trypsin; it was also pH dependent, the maximum being observed at pH 7.4. Melatonin binding was affected by a variety of ionic manipulations; it was inhibited 55% and 62% after addition of 10 mM KC1 and 120 mM NaCl, respectively, and it was increased 40% and 50% after the addition of 4 or 6 mM CaCl2. Melatonin binding was increased 25% by 1.25 mM MgCl2, whereas it was depressed at higher concentrations. Among the various brain regions studied, melatonin binding was maximal in the MBH; indole binding in occipital and cerebellar cortexes was 73% and 34% that of MBH. Subcellular fractionation studies indicated that about 70% of the binding was located in the 27, 000 × g pellet. Scatchard analysis revealed a single population of binding sites with a Kd value of 1.2 ± 0.4 × 10-8M in three successive experiments; binding site concentration ranged from 8-14 fmol/mg protein. When various indole analogs were tested for their ability to inhibit [3H]-melatonin binding at different concentrations, the following half-maximal inhibition values were obtained: melatonin, 20 nM; 5-methoxytryptophol, 80 nM; 5-methoxyindoleacetic acid, 100 nM; serotonin, 160 nM; 5-hydroxytryptophol, 200 nM; 5-methoxytryptamine, 250 nM; Nacetylserotonin, 250 nM; tryptamine, 250 nM; 2-methyl indole, 1, 500 nM; 5-hydroxytryptophan, 1, 600 nM; 5-hydroxyindoleacetic acid, 2, 000 nM; 6-hydroxymelatonin, >10, 000 nM; and indomethacin, > 10, 000 nM. These results suggest that melatonin receptors are present in the brain. © 1979 by The Endocrine Society.
Registro:
| Documento: | Artículo |
| Título: | Specific binding of melatonin in bovine brain |
| Autor: | Cardinali, D.P.; Vacas, M.I.; Boyer, E.E. |
| Filiación: | Centro de Estudios Farmacologicos y de Principios Naturales, Obligado 2490, Buenos Aires, 1428, Argentina |
| Palabras clave: | brain receptor; drug receptor; melatonin; radioisotope; animal experiment; brain; cattle; central nervous system; endocrine system; hypothalamus; in vitro study; melatonin h 3; methodology; nerve fiber membrane; nervous system; pharmacokinetics; pineal body; Animal; Binding, Competitive; Brain; Cattle; Cell Membrane; Kinetics; Melatonin; Osmolar Concentration; Receptors, Cell Surface; Tissue Distribution |
| Año: | 1979 |
| Volumen: | 105 |
| Número: | 2 |
| Página de inicio: | 437 |
| Página de fin: | 441 |
| DOI: | http://dx.doi.org/10.1210/endo-105-2-437 |
| Título revista: | Endocrinology |
| Título revista abreviado: | Endocrinology |
| ISSN: | 00137227 |
| CAS: | melatonin, 73-31-4; Melatonin, 73-31-4; Receptors, Cell Surface |
| Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00137227_v105_n2_p437_Cardinali |
Referencias:
- Cardinali, D.P., Melatonin and the endocrine role of the pineal organ (1974) Current Topics in Experimental Endocrinology, p. 107. , James, V. H. T. and L. Martini (eds.), Academic Press, New York
- Reiter, R.J., (1977) The Pineal-1977, , Eden Press, Montreal
- Anton-Tay, F., Wurtman, R.J., Regional uptake of [3H]-mela-tonin from blood or cerebrospinal fluid by rat brain (1969) Nature, 221, p. 474
- Cardinali, D.P., Hyyppa, M.T., Wurtman, R.J., Fate of intracisternally injected melatonin by the rat brain (1973) Neuroendocrinology, 12, p. 30
- Cardinali, D.P., Nagle, C.A., Rosner, J.M., Uptake and effects of melatonin on the synthesis of proteins by the rat cerebral cortex (1973) Life Sci, 13, p. 823
- Anton-Tay, F., Chou, C., Anton, S., Wurtman, R.J., Brain serotonin concentration: Elevation following intraperitoneal administration of melatonin (1968) Science, 162, p. 277
- Anton-Tay, F., Pineal-brain relationships (1971) The Pineal Gland, p. 213. , Wolstenholme, G. E. W., and J. Knight (eds.), Churchill Livingstone, London
- Cardinali, D.P., Nagle, C.A., Freire, F., Rosner, J.M., Effects of melatonin on neurotransmitter uptake and release by synaptosome-rich homogenates of the rat hypothalamus (1975) Neuroendocrinology, 18, p. 72
- Cardinali, D.P., Freire, F., Melatonin effects on brain. Interaction with microtubule protein, inhibition of fast axoplasmic flow and induction of crystaloid and tubular formations in the hypothalamus (1975) Mol Cell Endocrinol, 2, p. 317
- Kao, L.W.L., Weisz, J., Release of gonadotrophin-releasing hormone (Gn-RH) from isolated, perifused medial basal hypothalamus by melatonin (1977) Endocrinology, 100, p. 1723
- Cohen, M., Roselle, D., Chabner, B., Schmidt, T.J., Lippman, M., Evidence for a cytoplasmic melatonin receptor (1978) Nature, 274, p. 894
- Bennet, J.P., Jr., Snyder, S.H., Stereospecificity binding of D-lisergic acid diethylamide (LSD) to brain membranes: Relationship to serotonin receptors (1975) Brain Res, 94, p. 507
- Lowry, O., Rosebrough, N., Farr, A., Randall, R., Protein measurement with the Folin phenol reagent (1951) J Biol Chem, 193, p. 265
- Pert, C.B., Snyder, S.H., Properties of opiate-receptor binding in rat brain (1973) Proc Natl Acad Sci USA, 70, p. 2243
- Scatchard, G., The attraction of proteins for small molecules and ions (1949) Ann NY Acad Sci, 51, p. 660
- Klein, D.C., Notides, A., Thin-layer chromatographic separation of pineal gland derivatives of serotonin-l4C (1969) Anal Biochem, 31, p. 480
- Cardinali, D.P., Rosner, J.M., Metabolism of serotonin by the rat retina in vitro (1971) J Neurochem, 18, p. 1769
- Marczynski, T.J., Yamaguchi, N., Ling, G.M., Grodzinska, L., Sleep induced by the administration of melatonin (5-methoxy-N-acetyltryptamine) to the hypothalamus in unrestrained cats (1964) Ex-Perientia, 20, p. 435
- Barchas, J.D., Da Costa, F., Spector, S., Acute pharmacology of melatonin (1967) Nature, 214, p. 919
- Hishikawa, Y., Cramer, H., Kuhlo, W., Natural and melatonin-induced sleep in young chicken-a behavioral and electrographic study (1969) Exp Brain Res, 7, p. 84
- Anton-Tay, F., Diaz, J.L., Fernandez-Guardiola, A., On the effect of melatonin upon human brain. Its possible therapeutic implications (1971) Life Sci, 10, p. 841
- Carman, J.S., Post, R.M., Buswell, R., Goodwin, F.K., Negative effects of melatonin on depression (1976) Am J Psychiatry, 133, p. 1181
- Cardinali, D.P., Changes in hypothalamic neurotransmitter uptake following pinealectomy, superior cervical ganglionectomy or melatonin administration to rats (1975) Neuroendocrinology, 19, p. 91
- Heward, C., Hadley, M.E., Structure-activity relationships of melatonin and related indoleamines (1975) Life Sci, 17, p. 1167
- Messenger, E.A., Warner, A.E., The action of melatonin on single amphibian pigment cells in tissue culture (1977) Br J Pharmacol, 61, p. 107
- Wurtman, R.J., Axelrod, J., Potter, L.T., The uptake of H1 2 3-melatonin in endocrine and nervous tissues and the effects of constant light exposure (1964) J Pharmacol Exp Ther, 143, p. 314
- Snyder, S.H., Bennet, J.P., Neurotransmitter receptors in the brain: Biochemical identification (1976) Annu Rev Physiol, 38, p. 153
Citas:
---------- APA ----------
Cardinali, D.P., Vacas, M.I. & Boyer, E.E. (1979) . Specific binding of melatonin in bovine brain. Endocrinology, 105(2), 437-441.http://dx.doi.org/10.1210/endo-105-2-437
---------- CHICAGO ----------
Cardinali, D.P., Vacas, M.I., Boyer, E.E. "Specific binding of melatonin in bovine brain" . Endocrinology 105, no. 2 (1979) : 437-441.http://dx.doi.org/10.1210/endo-105-2-437
---------- MLA ----------
Cardinali, D.P., Vacas, M.I., Boyer, E.E. "Specific binding of melatonin in bovine brain" . Endocrinology, vol. 105, no. 2, 1979, pp. 437-441.http://dx.doi.org/10.1210/endo-105-2-437
---------- VANCOUVER ----------
Cardinali, D.P., Vacas, M.I., Boyer, E.E. Specific binding of melatonin in bovine brain. Endocrinology. 1979;105(2):437-441.http://dx.doi.org/10.1210/endo-105-2-437
