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ROD-188
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| Systematic (IUPAC) name | |
| (5R)-5-[(1R)-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinolin-1-yl]oxolan-2-one | |
| Identifiers | |
| CAS number | ? |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C20H21NO4S |
| Mol. mass | 371.449 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Legal |
| 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]
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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
Wikipedia content modification information:
- This page was last modified on 16 July 2008, at 03:34.
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