摘要: GABA(A) receptor channels are ubiquitous in the mammalian central nervous system mediating fast inhibitory neurotransmission by becoming permeant to chloride ions response GABA. The emphasis of this review is on rich chemical diversity ligands that influence function. Such provides many avenues for design and development new entities acting receptors. There also a significant subtypes composed different protein subunits. discovery subtype specific agents major challenge continuing pharmacology. Leads receptors come from using recombinant known subunit composition as has been elegantly demonstrated refining benzodiazepine actions with alpha1 preferring showing sedative properties but not anxiolytic properties. most recent advances therapeutic use concern promotion sound sleep. Many herbal medicines used promote sleep their active ingredients include flavonoids terpenoids modulate
eurekaselect.com
sydney.edu.au 参考文章(216)
Barbara A Goldstein, Abraham Shulman, Arnold M Strashun, GABAA-benzodiazepine-chloride receptor-targeted therapy for tinnitus control: preliminary report. International Tinnitus Journal. ,vol. 8, pp. 30- 36 ,(2002)
Se-Eun Choi, Seok Choi, Jun-Ho Lee, Paul J. Whiting, Sang-Mok Lee, Seung-Yeol Nah, Effects of ginsenosides on GABA(A) receptor channels expressed in Xenopus oocytes. Archives of Pharmacal Research. ,vol. 26, pp. 28- 33 ,(2003) , 10.1007/BF03179927
Hson Mou Chang, Kuk Ying Chui, Fan Wah Lau Tan, Yun Yang, Zeng Pei Zhong, Chi Ming Lee, Hing Leung Sham, Henry N. C. Wong, Structure-activity relationship of miltirone, an active central benzodiazepine receptor ligand isolated from Salvia miltiorrhiza Bunge (Danshen). Journal of Medicinal Chemistry. ,vol. 34, pp. 1675- 1692 ,(1991) , 10.1021/JM00109A022
Structure-activity studies with Ginkgo biloba extract constituents as receptor-gated chloride channel blockers and modulators. Pharmacopsychiatry. ,vol. 36, pp. 68- 77 ,(2003) , 10.1055/S-2003-40455
J. J. Lambert, J. A. Peters, S. C. Harney, D. Belelli, Steroid Modulation of GABAA Receptors Handbook of experimental pharmacology. ,vol. 150, pp. 117- 140 ,(2001) , 10.1007/978-3-642-56833-6_4
Rhodri J. Walters, Stephen H. Hadley, Kendall D.W. Morris, Jahanshah Amin, Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms. Nature Neuroscience. ,vol. 3, pp. 1274- 1281 ,(2000) , 10.1038/81800
A. Jones, E. R. Korpi, R. M. McKernan, R. Pelz, Z. Nusser, R. Mäkelä, J. R. Mellor, S. Pollard, S. Bahn, F. A. Stephenson, A. D. Randall, W. Sieghart, P. Somogyi, A. J. H. Smith, W. Wisden, Ligand-gated ion channel subunit partnerships: GABAA receptor alpha6 subunit gene inactivation inhibits delta subunit expression. The Journal of Neuroscience. ,vol. 17, pp. 1350- 1362 ,(1997) , 10.1523/JNEUROSCI.17-04-01350.1997
Susanne K. Hansen, Michael-Robin Witt, Ola Bergendorff, Olov Sterner, Diane M. Rutherford, Mogens P.C. Nielsen, Isolation and identification from Salvia officinalis of two diterpenes which inhibit t-butylbicyclophosphoro[35S]thionate binding to chloride channel of rat cerebrocortical membranes in vitro. Neuroscience Letters. ,vol. 135, pp. 224- 226 ,(1992) , 10.1016/0304-3940(92)90441-9
Matt T. Bianchi, Luyan Song, Helen Zhang, Robert L. Macdonald, Two Different Mechanisms of Disinhibition Produced by GABAA Receptor Mutations Linked to Epilepsy in Humans The Journal of Neuroscience. ,vol. 22, pp. 5321- 5327 ,(2002) , 10.1523/JNEUROSCI.22-13-05321.2002
D Benke, L Scheurer, J A Benson, B J Hamilton, Y Wang, D B Carter, H Mohler, F Knoflach, H Lüddens, Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2. Molecular Pharmacology. ,vol. 50, pp. 1253- 1261 ,(1996)