Extrasynaptic GABAA receptors are critical targets for sedative-hypnotic drugs.
DOI: 10.5664/JCSM.26526
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摘要: The gamma-aminobutyric acid subtype A (GABAA) receptor is widely considered to be an important target for most clinically effective sedative-hypnotic compounds, including general anesthetics, benzodiazepines, barbiturates, and gaboxadol or THIP (4,5,6,7-tetrahydroisoxazolo (5,4-c)pyridin-3-ol). GABAA receptors are highly expressed in anatomical regions that implicated sleep processes, notably the thalamus. Furthermore, concentrations of these drugs modify behavior vivo also increase GABA-induced inhibitory conductances vitro. This review will summarize functional, regional distribution, pharmacologic properties various classes receptors. Particular emphasis placed on subpopulations extrasynaptic neurons, as exquisitely sensitive several compounds. Evidence date suggests can broadly classified into two groups; those containing delta subunit non-delta subunit-containing Finally, probable contribution modulation considered.
sci-hub.st 参考文章(8)
Gintautas Grabauskas, Time course of GABA in the synaptic clefts of inhibitory synapses in the rostral nucleus of the solitary tract. Neuroscience Letters. ,vol. 373, pp. 10- 15 ,(2004) , 10.1016/J.NEULET.2004.09.051
S Pirker, C Schwarzer, A Wieselthaler, W Sieghart, G Sperk, GABAA receptors : Immunocytochemical distribution of 13 subunits in the adult rat brain Neuroscience. ,vol. 101, pp. 815- 850 ,(2000) , 10.1016/S0306-4522(00)00442-5
S G Brickley, S G Cull-Candy, M Farrant, Development of a tonic form of synaptic inhibition in rat cerebellar granule cells resulting from persistent activation of GABAA receptors. The Journal of Physiology. ,vol. 497, pp. 753- 759 ,(1996) , 10.1113/JPHYSIOL.1996.SP021806
B. M. Stell, S. G. Brickley, C. Y. Tang, M. Farrant, I. Mody, Neuroactive steroids reduce neuronal excitability by selectively enhancing tonic inhibition mediated by δ subunit-containing GABAA receptors Proceedings of the National Academy of Sciences of the United States of America. ,vol. 100, pp. 14439- 14444 ,(2003) , 10.1073/PNAS.2435457100
Fan Jia, Leonardo Pignataro, Claude M. Schofield, Minerva Yue, Neil L. Harrison, Peter A. Goldstein, An extrasynaptic GABAA receptor mediates tonic inhibition in thalamic VB neurons. Journal of Neurophysiology. ,vol. 94, pp. 4491- 4501 ,(2005) , 10.1152/JN.00421.2005
V. B. Caraiscos, E. M. Elliott, K. E. You-Ten, V. Y. Cheng, D. Belelli, J. G. Newell, M. F. Jackson, J. J. Lambert, T. W. Rosahl, K. A. Wafford, J. F. MacDonald, B. A. Orser, Tonic inhibition in mouse hippocampal CA1 pyramidal neurons is mediated by α5 subunit-containing γ-aminobutyric acid type A receptors Proceedings of the National Academy of Sciences of the United States of America. ,vol. 101, pp. 3662- 3667 ,(2004) , 10.1073/PNAS.0307231101
DJ Laurie, W Wisden, PH Seeburg, The distribution of thirteen GABAA receptor subunit mRNAs in the rat brain. III. Embryonic and postnatal development The Journal of Neuroscience. ,vol. 12, pp. 4151- 4172 ,(1992) , 10.1523/JNEUROSCI.12-11-04151.1992
I. Mody, Y. De Koninck, T.S. Otis, I. Soltesz, Bridging the cleft at GABA synapses in the brain Trends in Neurosciences. ,vol. 17, pp. 517- 525 ,(1994) , 10.1016/0166-2236(94)90155-4