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definition - ROD-188

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ROD-188

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ROD-188
Systematic (IUPAC) name
(5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one
Identifiers
CAS number ?
ATC code ?
PubChem9842377
Chemical data
FormulaC20H21NO4S 
Mol. mass371.449 g/mol
SMILESeMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life ?
Excretion ?
Therapeutic considerations
Pregnancy cat. ?
Legal statusLegal
Routes ?


ROD-188 is a sedative drug structurally derived from the GABAA antagonist bicuculline. 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.[1] ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors.[2]

References

  1. ^ 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
  2. ^ 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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