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ROD-188
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ROD-188 : ウィキペディア英語版
ROD-188

ROD-188 is a sedative drug that was structurally derived from the GABAA antagonist bicuculline by a team at Roche.〔US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders〕 Unlike bicuculline, ROD-188 acts as an agonist at GABAA receptors, being a positive allosteric modulator acting at a novel binding site distinct from those of benzodiazepines, barbiturates or muscimol, with its strongest effect produced at the α6β2γ2 subtype of the GABAA receptor.〔Thomet U, Baur R, Razet R, Dodd RH, Furtmüller R, Sieghart W, Sigel E. A novel positive allosteric modulator of the GABA(A) receptor: the action of (+)-ROD188. ''British Journal of Pharmacology''. 2000 Oct;131(4):843-50. PMID 11030736〕 ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.〔Sigel E, Baur R, Furtmueller R, Razet R, Dodd RH, Sieghart W. Differential cross talk of ROD compounds with the benzodiazepine binding site. ''Molecular Pharmacology''. 2001 Jun;59(6):1470-7. PMID 11353808〕
== See also ==

* Bicuculline

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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