ROD-188

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][4]

ROD-188
Clinical data
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • (5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one
PubChem CID
ChemSpider
Chemical and physical data
FormulaC20H21NO4S
Molar mass371.45 g·mol−1
3D model (JSmol)
  • Cc1ccc(cc1)S(=O)(=O)N2CCc4ccccc4[C@@H]2[C@@H]3CCC(=O)O3
  (verify)

See also

References
  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 (October 2000). "A novel positive allosteric modulator of the GABA(A) receptor: the action of (+)-ROD188". British Journal of Pharmacology. 131 (4): 843–50. doi:10.1038/sj.bjp.0703558. PMC 1572371. PMID 11030736.
  3. Sigel E, Baur R, Furtmueller R, Razet R, Dodd RH, Sieghart W (June 2001). "Differential cross talk of ROD compounds with the benzodiazepine binding site". Molecular Pharmacology. 59 (6): 1470–7. doi:10.1124/mol.59.6.1470. PMID 11353808.
  4. Ramerstorfer J, et al. The GABAA Receptor α+β− Interface: A Novel Target for Subtype Selective Drugs. Journal of Neuroscience 2011; 31(3):870-877. doi:10.1523/JNEUROSCI.5012-10.2011
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