Navegar

Colección

Datos Estadísticas

Artículo

Estamos trabajando para incorporar este artículo al repositorio
Consulte el artículo en la página del editor
Consulte la política de Acceso Abierto del editor

Abstract:

The intraperitoneal injection of the methylxanthine derivative pentoxifylline [3,7-dimethyl-1-(5-oxo-hexyl)-xanthine] brought about, 3 hr later, a significant depression of α- and β-adrenoceptor sites in the cerebral cortex, and of β-adrenoceptor sites in medial basal hypothalamus and pineal gland, (assessed from the specific binding of radioactive dihydroergocryptine and dihydroalprenolol respectively). The changes in the density of binding sites were not accompanied by significant modifications of the Kd′s. Sympathetic denervation of the pineal gland by superior cervical ganglionectomy (SCGx) abolished the changes of β-adrenoceptor number in the pineal caused by pentoxifylline. The increase of α-adrenoceptor sites in the hypothalamus brought about by ganglionectomy was not affected by injection of pentoxifylline. Pentoxifylline did not compete in vitro for radioligand binding to brain membranes. These results suggest that methylxanthines depress brain adrenoceptor sites acutely, probably by down-regulation of receptors following the increase in catecholamine release caused by injection of the drug. © 1982.

Registro:

Documento: Artículo
Título:Effect of pentoxifylline on α- and β-adrenoceptor sites in cerebral cortex, medial basal hypothalamus and pineal gland of the rat
Autor:Lowenstein, P.R.; Vacas, M.I.; Cardinali, D.P.
Filiación:Centro de Estudios Farmacológicos y de Principios Naturales (CEFAPRIN), Serrano 665/669, 1414 Buenos Aires, Argentina
Palabras clave:adrenergic receptors; binding studies; cerebral cortex; medial basal hypothalamus; pentoxifylline [3,7-dimethyl-1-(5-oxo-hexyl)-xanthine], methylxanthines; pineal gland; superior cervical ganglion; alpha adrenergic receptor; beta adrenergic receptor; dihydroergocryptine; drug receptor; pentoxifylline; phentolamine; propranolol; radioisotope; animal experiment; brain cortex; central nervous system; dihydroalprenolol h 3; dihydroergocryptine h 3; hypothalamus; pineal body; rat; Animal; Binding Sites; Cerebral Cortex; Dihydroalprenolol; Dihydroergotoxine; Female; Hypothalamus; Pentoxifylline; Pineal Gland; Rats; Rats, Inbred Strains; Receptors, Adrenergic; Receptors, Adrenergic, alpha; Receptors, Adrenergic, beta; Support, Non-U.S. Gov't; Theobromine
Año:1982
Volumen:21
Número:3
Página de inicio:243
Página de fin:248
DOI: http://dx.doi.org/10.1016/0028-3908(82)90194-0
Título revista:Neuropharmacology
Título revista abreviado:Neuropharmacology
ISSN:00283908
CODEN:NEPHB
CAS:dihydroergocryptine, 14271-05-7, 25447-66-9; pentoxifylline, 6493-05-6; phentolamine, 50-60-2, 73-05-2; propranolol, 13013-17-7, 318-98-9, 3506-09-0, 4199-09-1, 525-66-6; Dihydroalprenolol, 60106-89-0; Dihydroergotoxine, 11032-41-0; Pentoxifylline, 6493-05-6; Receptors, Adrenergic; Receptors, Adrenergic, alpha; Receptors, Adrenergic, beta; Theobromine, 83-67-0
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283908_v21_n3_p243_Lowenstein

Referencias:

  • Banerjee, Kung, Riggi, Chanda, Development of beta adrenergic receptor subsensitivity by antidepressants (1977) Nature, 268, pp. 455-456
  • Butcher, Sutherland, Adenosine-3′,5′-phosphate in biologic materials. I. Purification and properties of cyclic 3′,5′-nucleotide phosphodiesterase and use of this enzyme to characterize adenosine-3′,5′-phosphate in human urine (1962) J. biol. Chem., 237, pp. 1244-1250
  • Cantor, Greenberg, Weiss, Effect of long-term changes in sympathetic nervous activity on the beta-adrenergic receptor-adenylate cyclase complex of rat pineal gland (1981) Molec. Pharmac., 19, pp. 21-26
  • Cardinali, Effects of pentoxifylline and theophylline on neurotransmitter uptake and release by synaptosome-rich homogenates of the rat hypothalamus (1977) Neuropharmacology, 16, pp. 785-790
  • Cardinali, Effect of pentoxifylline and aminophylline on biogenic amine metabolism of the rat brain (1978) Eur. J. Pharmac., 47, pp. 239-243
  • Cardinali, Methylxanthines: possible mechanisms of action in brain (1980) Trends Pharmac. Sci., 1, pp. 405-407
  • Cardinali, Gomez, Changes in hypothalamic noradrenaline, dopamine and serotonin uptake after oestradiol administration to rats (1977) J. Endocr., 73, pp. 181-182
  • Cardinali, Vacas, Fortis, Stefano, Superior cervical ganglionectomy depresses norepinephrine uptake, increases the density of α-adrenoceptor sites and induces supersensitivity to adrenergic drugs in rat medial basal hypothalamus (1981) Neuroendocrinology, 33, pp. 199-206
  • Corrodi, Fuxe, Jonsson, Effects of caffeine on central monoamine neurons (1972) J. Pharm. Pharmac., 24, pp. 155-169
  • Creese, Sibley, Receptor adaptations to centrally acting drugs (1981) Ann. Rev. Pharmac. Toxicol., 21, pp. 357-391
  • Dibner, Molinoff, Agonist-induced changes in beta-adrenergic receptor density and receptor-mediated responsiveness in slices of rat cerebral cortex (1979) J. Pharmac. exp. Ther., 210, pp. 433-439
  • Fredholm, Are methylxanthine effects due to antagonism of endogenous adenosine? (1980) Trends in Pharmacological Sciences, 1, pp. 129-132
  • Hoffman, Lefkowitz, Radioligand binding studies of adrenergic receptors: new insights into molecular and physiological regulation (1980) Ann. Rev. Pharmac. Toxicol., 20, pp. 581-608
  • Karasawa, Furukawa, Toshida, Shimizu, Effect of theophylline on monoamine metabolism in the rat brain (1976) Eur. J. Pharmac., 37, pp. 97-104
  • Kinnier, Chuang, Costa, Down regulation of dihydroalprenolol and imipramine binding sites in brain of rats repeatedly treated with imipramine (1980) Eur. J. Pharmac., 67, pp. 289-294
  • Kuba, Release of calcium ions linked to the activation of potassium conductance in a caffeine-treated sympathetic neurone (1980) J. Physiol., Lond., 298, pp. 251-259
  • Lowry, Rosebrough, Farr, Randall, Protein measurement with the Folin phenol reagent (1951) J. biol. Chem., 193, pp. 265-275
  • Marangos, Paul, Goodwin, Skolnick, Putative endogenous ligands for the benzodiazepine receptor (1979) Life Sci., 25, pp. 1093-1102
  • Molinoff, Sporn, Wolfe, Harden, Regulation of β-adrenergic receptors in the cerebral cortex (1978) Adv. Cyclic Nuc. Res., 9, pp. 465-483
  • Rall, The xanthines (1980) The Pharmacological Basis of Therapeutics, pp. 592-607. , A. Goodman Gilman, L.S. Goodman, A. Gilman, 6th edn, Macmillan, New York
  • Romero, Zatz, Kebabian, Axelrod, Circadian cycles in binding of 3H-alprenolol to β-adrenergic receptor sites in rat pineal (1975) Nature, 258, pp. 435-436
  • Sarai, Frazer, Brunswick, Mendels, Desmethylimipramine-induced decrease in beta-adrenergic receptor binding in rat cerebral cortex (1978) Biochem. Pharmac., 27, pp. 2179-2182
  • Snedecor, Cochram, (1967) Statistical Methods, p. 593. , 6th edn, Iowa State Univ. Press, Ames, Iowa
  • Stoclet, Inhibitors of cyclic nucleotide phosphodieterase (1979) Trends Pharmac. Sci., 1, pp. 98-100
  • Vacas, Cardinali, Effect of estradiol on α- and β-adrenoceptor density in medial basal hypothalamus, cerebral cortex and pineal gland of ovariectomized rats (1980) Neurosci. Lett., 17, pp. 73-77
  • Waldeck, Some effects of caffeine and aminophylline on the turnover of catecholamines in the brain (1971) J. Pharmac., 23, pp. 824-830
  • Williams, Lefkowitz, (1978) Receptor Binding Studies in Adrenergic Pharmacolgy, p. 157. , Raven Press, New York
  • Wolfe, Harden, Sporn, Molinoff, Presynaptic modulation of beta-adrenergic receptors in rat cerebral cortex after treatment with antidepressants (1978) J. Pharmac. exp. Ther., 207, pp. 446-457
  • Zatz, Kebabian, Romero, Lefkowitz, Axelrod, Pineal β-adrenergic receptor: correlation of binding of 3H-alprenolol with stimulation of adenylate cyclase (1976) J. Pharmac. exp. Ther., 196, pp. 714-722

Citas:

---------- APA ----------
Lowenstein, P.R., Vacas, M.I. & Cardinali, D.P. (1982) . Effect of pentoxifylline on α- and β-adrenoceptor sites in cerebral cortex, medial basal hypothalamus and pineal gland of the rat. Neuropharmacology, 21(3), 243-248.
http://dx.doi.org/10.1016/0028-3908(82)90194-0
---------- CHICAGO ----------
Lowenstein, P.R., Vacas, M.I., Cardinali, D.P. "Effect of pentoxifylline on α- and β-adrenoceptor sites in cerebral cortex, medial basal hypothalamus and pineal gland of the rat" . Neuropharmacology 21, no. 3 (1982) : 243-248.
http://dx.doi.org/10.1016/0028-3908(82)90194-0
---------- MLA ----------
Lowenstein, P.R., Vacas, M.I., Cardinali, D.P. "Effect of pentoxifylline on α- and β-adrenoceptor sites in cerebral cortex, medial basal hypothalamus and pineal gland of the rat" . Neuropharmacology, vol. 21, no. 3, 1982, pp. 243-248.
http://dx.doi.org/10.1016/0028-3908(82)90194-0
---------- VANCOUVER ----------
Lowenstein, P.R., Vacas, M.I., Cardinali, D.P. Effect of pentoxifylline on α- and β-adrenoceptor sites in cerebral cortex, medial basal hypothalamus and pineal gland of the rat. Neuropharmacology. 1982;21(3):243-248.
http://dx.doi.org/10.1016/0028-3908(82)90194-0