ROD-188

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IUPAC_name = (5R)-5- [(1R)-2-(4-methylphenyl)sulfonyl-3,4-dihydro-1H-isoquinolin-1-yl] oxolan-2-one


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PubChem = 9842377
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C = 20 | H = 21 | N = 1 | O = 4 | S = 1
molecular_weight = 371.449 g/mol
smiles = c3cc(C)ccc3S(=O)(=O)N2CCc1ccccc1C2C(CC4)OC4=O
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legal_status = Legal
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ROD-188 is a sedative drug structurally derived from the GABA_A antagonist bicuculline. 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. [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] ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine receptors. [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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