ROD-188

ROD-188

Clinical data
ATC code	none
Legal status
Legal status	In general: uncontrolled
Identifiers
IUPAC name (5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one
CAS Number	309267-40-1  Y
PubChem CID	9842377
ChemSpider	8018092
ChEMBL	ChEMBL136324
CompTox Dashboard (EPA)	DTXSID001027550
Chemical and physical data
Formula	C20H21NO4S
Molar mass	371.45 g·mol−1
3D model (JSmol)	Interactive image
SMILES Cc1ccc(cc1)S(=O)(=O)N2CCc4ccccc4[C@@H]2[C@@H]3CCC(=O)O3
(verify)

ROD-188 is a sedative drug that was structurally derived from the GABA_A antagonist bicuculline by a team at Roche. ^[1] Unlike bicuculline, ROD-188 acts as an agonist at GABA_A 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 GABA_A 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]}

See also

• Bicuculline

References

1. US 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): 843–850. 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): 1470–1477. doi:10.1124/mol.59.6.1470. PMID   11353808.
4. Ramerstorfer J, Furtmüller R, Sarto-Jackson I, Varagic Z, Sieghart W, Ernst M (January 2011). "The GABAA receptor α+β-interface: a novel target for subtype selective drugs". The Journal of Neuroscience. 31 (3): 870–877. doi:10.1523/JNEUROSCI.5012-10.2011. PMC   3182524 . PMID   21248110. S2CID   1989995.