Benzodiazepines (BZs) produce most, if not all, of their pharmacological actions by specifically enhancing the effects of endogenous and exogenous GABA that are mediated by GABA A receptors. This potentiation consists in an increase of the apparent affinity of GABA for increasing chloride conductance ...
Most patients with insomnia use drug therapy, with benzodiazepines being the most commonly used medications, such as diazepam, eszopiclone, and alprazolam. However, the unclear pathogenesis of insomnia complicates the development of hypnotic drugs that effectively target its underlying mechanisms. Consequent...
Benzodiazepine receptors mediate many of the pharmacological actions of the benzodiazepines and related minor tranquillisers, including their anxiolytic, hypnotic and muscle-relaxant properties (see Tallman et al., 1980; Skolnick and Paul 1982 for review). The benzodiazepine receptor or recognition site...
16 Basile AS, Hughes RD, Harrison PM, Nurou Y. Elevated brain concentrations of 1,4-benzodiazepines in fluminant hepatic failure. N Engl J Med, 1991;19(2):112-116 17 Anthony S, Basile S, Jones EJ, Fisher C, Smith K, Liner GW et al. The pathogenesis and treatment of hepatic enceph...
The molecular mechanisms of coevolution between plants and insects remain elusive. GABA receptors are targets of many neurotoxic terpenoids, which represent the most diverse array of natural products known. Over deep evolutionary time, as plant terpene synthases diversified in plants, so did plant terp...
We also show that benzodiazepines and GABA act at apparently distinct sites to protect benzodiazepine receptors from heat and iodoacetamide.doi:10.1038/287651a0Gavish, MosheSnyder, Solomon HNatureGavish, M., Snyder, S.H.: Benzodiazepine recognition sites on GABA receptors. Nature 287 , 651–652 (...
For example,benzodiazepines, a class of drugs used to treat anxiety, bind to GABA-A receptor and facilitate its binding to GABA, thus potentiating GABA inhibitory effect. 例如,一类治疗焦虑症的药物-苯二氮卓类与GABA-a受体结合,促进其与GABA的结合,从而增强GABA的抑制作用。01:46 ...
Journal of Receptors and Signal TransductionSchoch, P., Häring, P., Takacs, B., Stähli, C., and Mohler, H. 1984. A GABA/benzodiazepine receptor from bovine brain: Purification, reconstitution and immunological characterization. J. Recept. Res. 4:189–200....
benzodiazepines that bind to the GABA-A receptor. GABA-A receptors are pentameric, consisting of proteins from several subunit classes: alpha, beta, gamma, delta and rho. Mutations in this gene cause juvenile myoclonic epilepsy and childhood absence epilepsy type 4. Multiple transcript variants ...
Blanchard, J. C. and Julou, L. (1983) Suriclone: a new cyclopyrrolone derivative recognizing receptors labeled by benzodiazepines in rat hippocampus and cerebellum.J. Neurochem.40 Bloom F. E. and Iversen L. L. (1971) Localizing3H-GABA in nerve terminals of rat cerebral cortex by electron...