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Characterization of alpha-adrenergic receptors in guinea pig cerebral cortex: Effect of chronic antidepressant treatments

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Abstract

Alpha-adrenergic receptor sites in cerebral cortex membranes of the guinea pig brain have been characterized by the specific binding of 3H-WB4101, an alpha-adrenergic antagonist. The binding was rapid, reversible, saturable, and stereoselective. The maximal binding site (B max) and disociation constant (k d) for 3H-WB4101 were calculated to be 251 fmol/mg protein and 1.23 nM, respectively. Ligand displacement experiments suggest that 3H-WB4101 binds to alpha1-adrenergic receptors. Chronic treatment of guinea pigs with desipramine, amitriptyline, phenelzine, or electroconvulsive shock failed to show any statistically significant change in alpha-adrenergic receptor sensitivity as measured by the binding of 3H-WB4101.

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References

  • Banerjee SP, Kung LS, Riggi SJ, Chanda SK (1977) Development of beta-adrenergic receptor subsensitivity by antidepressants. Nature 268:455–456

    Google Scholar 

  • Bergstrom DA, Kellar KJ (1979a) Effect of electroconvulsive shock on monoaminergic receptor binding sites in rat brain. Nature 278:464–465

    Google Scholar 

  • Bergstrom DA, Kellar KJ (1979b) Adrenergic and serotonergic receptor binding in rat brain after chronic desmethylimipramine treatment. J Pharmacol Exp Ther 209:256–261

    Google Scholar 

  • Chasin M, Rivkin I, Mamrak F, Samaniego SG, Hess SM (1971) Alpha-and beta-adrenergic receptors as mediators of accumulation of cyclic adenosine 3′,5′-monophosphate in specific areas of guinea pig brain. J Biol Chem 246:3037–3041

    Google Scholar 

  • Chasin M, Mamrak F, Samaniego SG, Hess SM (1973) Characteristics of the catecholamine and histamine receptor sites mediating accumulation of cyclic adenosine 3′,5′-monophosphate formation in guinea pig brain. J Neurochem 21:1415–1427

    Google Scholar 

  • Clements-Jewery S (1978) The development of cortical beta-adrenoceptor subsensitivity in the rat by chronic treatment with trazodone, doxepin and mianserine. Neuropharmacology 17:779–781

    Google Scholar 

  • Davis JM, Arnett CD, Hoyler E, Stalvey LP, Daly JW, Skilnick P (1978) Brain alpha-adrenergic receptors: Comparison of 3H-WB4101 binding with norepinephrine-stimulated cyclic AMP accumulation in rat cerebral cortex. Brain Res 159:125–135

    Google Scholar 

  • Garver DL, Davis JM (1979) Biogenic amine hypothesis of affective disorders. Life Sci 24:383–394

    Google Scholar 

  • Gillespie DD, Manier DH, Sulser F (1979) Electroconvulsive treatment: Rapid subsensitivity of the norepinephrine receptor-coupled adenylate cyclase system in brain linked to down regulation of beta-adrenergic receptors. Commun Psychopharmacol 3:191–195

    Google Scholar 

  • Greenberg DA, U'Prichard DC, Snyder SH (1976) Alpha-noradrenergic receptor binding in mammalian brain: Differential labeling of agonist and antagonist states. Life Sci 19:69–76

    Google Scholar 

  • Hendley ED (1978) Iprimdole is a potent enhancer of spontaneous and KCl-induced efflux of norepinephrine from rat brain slices. Neurosci Abstr 4:494

    Google Scholar 

  • Hu HY, Davis JM, Heinze WJ, Pandey GN (1980) Effect of chronic treatment with antidepressants on beta-adrenergic receptor binding in guinea pig brain. Biochem Pharmacol 29:2895–2896

    Google Scholar 

  • Huang M, Shimizu H, Daly JW (1972) Accumulation of cyclic adenosine monophosphate in incubated slices of brain tissue. 2. Effect of depolarizing agents, membrane stabilizers, phosphodiesterase inhibitors and adenosine analogs. J Med Chem 15:462–466

    Google Scholar 

  • Lowry OH, Rosebrough NJ, Farr AL, Randall RJ (1951) Protein measurement with Folin phenol reagent. J Biol Chem 193:265–275

    Google Scholar 

  • Pandey GN, Heinze WJ, Brown BD, Davis JM (1979) Electroconvulsive shock treatment decrease beta-adrenergic receptor binding in rat cerebral cortex. Nature 280:234–235

    Google Scholar 

  • Rosenblatt JE, Pert CB, Tallman JF, Pert A, Bunney WE Jr (1979) The effect of imipramine and lithium on alpha- and beta-receptor binding in rat brain. Brain Res 160:186–191

    Google Scholar 

  • Sarai K, Frazer A, Brunswick D, Mendels J (1978) Desmethylimipramine-induced decrease in beta-adrenergic receptor binding in rat cerebral cortex. Biochem Pharmacol 27:2179–2181

    Google Scholar 

  • Sattin A, Rall TW, Zanella J (1975) Regulation of cyclic adenosine 3′,5′-monophosphate levels in guinea pig cerebral cortex by interaction of alpha-adrenergic and adenosine receptor activity. J Pharmacol Exp Ther 192:22–32

    Google Scholar 

  • Schultz J, Daly JW (1973) Adenosine 3′,5′-monophosphate in guinea pig cerebral cortical slices: Effects of alpha- and beta-adrenergic agents, histamine, serotonin and adenosine. J Neurochem 21:573–579

    Google Scholar 

  • Schultz J, Kleefeld G (1975) Stimulation of adenosine 3′,5′-monophosphate formation in guinea pig cerebral cortical slices in a calcium-free medium. Naunyn-Schmiedeberg's Arch Pharmacol 287:289–296

    Google Scholar 

  • Treiser S, Kellar KJ (1979) Lithium effects on adrenergic effects or supersensitivity in rat brain. Eur J Pharmacol 58:85–86

    Google Scholar 

  • U'Prichard DC, Snyder SH (1978) 3H-Catecholamine binding to alpha-receptors in rat brain enhancement by reserpine. Eur J Pharmacol 51:145–155

    Google Scholar 

  • U'Prichard DC, Snyder SH (1979) Distinct alpha-noradrenergic receptors differentiated by binding and physiological relationships. Life Sci 24:79–80

    Google Scholar 

  • U'Prichard DC, Greenberg DA, Snyder SH (1977) Binding characteristics of a radiolabeled agonist and antagonist at central nervous system alpha-noradrenergic receptors. Mol Pharmacol 13:454–473

    Google Scholar 

  • Wolfe BB, Harden TK, Sporn JR, Molinnoff PE (1978) Presynaptic modulation of beta-adrenergic receptors in rat cerebral cortex after treatment with antidepressants. J Pharmacol Exp Ther 207:446–457

    Google Scholar 

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Hu, Hy.Y., Davis, J.M. & Pandey, G.N. Characterization of alpha-adrenergic receptors in guinea pig cerebral cortex: Effect of chronic antidepressant treatments. Psychopharmacology 74, 201–203 (1981). https://doi.org/10.1007/BF00427093

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  • DOI: https://doi.org/10.1007/BF00427093

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