ROD-188

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ROD-188
File:ROD-188.png
Systematic (IUPAC) name
(5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one
Clinical data
Legal status
  • Uncontrolled
Identifiers
ATC code none
PubChem CID: 9842377
Chemical data
Formula C20H21NO4S
Molecular mass 371.449 g/mol
  • CC1=CC=C(S(=O)(N2CCC3=CC=CC=C3[C@@H]2[C@@H](O4)CCC4=O)=O)C=C1
  (verify)

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

References

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  1. ↑ US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders
  2. ↑ 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
  3. ↑ 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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