ROD-188
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ROD-188
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| Systematic (IUPAC) name | |
| (5R)-5-{(1R)-2-[(4-methylphenyl)sulfonyl]-1,2,3,4-tetrahydroisoquinolin-1-yl}dihydrofuran-2(3H)-one | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Uncontrolled |
| Identifiers | |
| ATC code | None |
| PubChem | CID 9842377 |
| Chemical data | |
| Formula | C20H21NO4S |
| Mol. mass | 371.449 g/mol |
| SMILES | eMolecules & PubChem |
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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]
See also
References
- ^ 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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