Summary
CL 218,872, which preferentially binds to benzodiazepine (BZ) type 1 receptors, and flurazepam, which is thought to bind to both types 1 and 2, were given alone and in combination to rats. CL 218,872 had little effect on sleep latency, but significantly increased total sleep time. As expected, flurazepam both shortened sleep latency and prolonged total sleep. Pretreatment with CL 218,872 had no effect on these alterations in sleep induced by flurazepam. The implications for possible significance of sub-typing of BZ receptors are discussed.
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References
Braestrup C, Schmiechen R, Nielsen M, Petersen EN (1982) Benzodiazepine receptor ligands, receptor occupancy, pharmacological effect and GABA receptor coupling. In: Usdin E, Skolnick P, Tallman J, Greenblatt D, Paul S (eds) Pharmacology of benzodiazepines. Macmillan, London, pp 71–85
File SE, Pellow S, Wilks L (1985) The sedative effects of CL 218,872, like those of chlordiazepoxide, are reversed by benzodiazepine antagonists. Psychopharmacology 85: 295–300
Gee KW, Yamamura HI (1982) Benzodiazepine receptor heterogeneity: a consequence of multiple conformational states of a single receptor or multiple population of structurally distinct macromolecules? In: Usdin E, Skolnick P, Tallman J, Greenblatt D, Paul S (eds) Pharmacology of benzodiazepines. Macmillan, London, pp 93–108
Kiepner CA, Lippa AS, Benson DI, Sano MC, Beer B (1979) Resolution of two biochemically and pharmacologically distinct benzodiazepine receptors. Pharmacol Biochem Behav 2: 457–462
Lippa AS, Critchett D, Sano MC, Kiepner CA, Greenblatt EN, Coupet J, Beer B (1979 a) Benzodiazepine receptors: cellular and behavioral characteristics. Pharmacol Biochem Behav 10: 831–843
Lippa AS, Coupet J, Greenblatt EN, Klepner CA, Beer B (1979 b) A synthetic non-benzodiazepine ligand for benzodiazepine receptors: a probe for investigating neuronal substrates of anxiety. Pharmacol Biochem Behav 11: 99–106
Lo MMS, Niehoff DB, Kuhar MJ, Snyder SH (1983) Differential localization of type I and type II benzodiazepine binding sites in substantia nigra. Nature 306: 57–60
Martin IL, Brown CL, Doble A (1983) Multiple benzodiazepine receptors: structures in the brain or structures in the mind? A critical review. Life Sci 32: 1925–1933
McElroy JF, Fleming RL, Feldman RS (1985) A comparison between chlordiazepoxide and CL 218,872 — a synthetic nonbenzodiazepine ligand for benzodiazepine receptors on spontaneous locomotor activity in rats. Psychopharmacology 85: 224–226
Mendelson WB, Guthrie R, Frederick G, Wyatt RJ (1974) An evaluation of the “flower pot method” of REM sleep deprivation. Pharmacol Biochem Behav 2: 553–556
Mendelson WB, Majchrowicz E, Mirmirani N, Dawson S, Gillin JC, Wyatt RJ (1978) Sleep during chronic ethanol administration and withdrawal in rats. J Stud Alcoh 39: 1213–1223
Mendelson WB, Owen C, Skolnick P, Paul SM, Martin JV, Ko G, Wagner R (1984) Nifedipine blocks sleep induction by flurazepam in the rat. Sleep 7: 64–68
Mohler H, Okada T (1977) Benzodiazepine receptor: demonstration in the central nervous system. Science 198: 849–851
Oakley NR, Jones BJ, Straughan DW (1984) The benzodiazepine receptor ligand CL 218,872 has both anxiolytic and sedative properties in rodents. J Neurochem 23: 797–802
Squires RF, Braestrup C (1900) Benzodiazepine receptors in rat brain. Nature 266: 732–734
Teitz EI, Chiu TH, Rosenberg HC (1985) Pre-versus post-synaptic localization of benzodiazepine and B-carboline binding sites. J Neurochem 44: 1524–1534
Young WS, Niehoff D, Kuhar MJ, Beer B, Lippa AS (1981) Multiple benzodiazepine receptor localization by light microscopic radiohistochemistry. J Pharmacol Exp Therap 216: 425–430
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Mendelson, W.B., Martin, J.V., Perils, M. et al. Sleep and benzodiazepine receptor sub-types. J. Neural Transmission 70, 329–336 (1987). https://doi.org/10.1007/BF01253607
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DOI: https://doi.org/10.1007/BF01253607