ROD-188
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Systematic (IUPAC) name | |
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(5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one
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Identifiers | |
ATC code | none |
PubChem | CID 9842377 |
Chemical data | |
Formula | C20H21NO4S |
Molar mass | 371.449 g/mol |
3D model (Jmol) | Interactive image |
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ROD-188 is a sedative drug that was structurally derived from the GABAA antagonist bicuculline by a team at Roche.[1] 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.[2] ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.[3]
See also[edit]
References[edit]
- ^ US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders
- ^ 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
- ^ 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
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See also: GABAergics
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