| 词条 | ROD-188 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 448134172 | IUPAC_name = (5R)-5- | image = ROD-188.png | tradename = | pregnancy_category = | legal_status = Uncontrolled | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = none | ATC_suffix = | PubChem = 9842377 | C=20 | H=21 | N=1 | O=4 | S=1 | molecular_weight = 371.449 g/mol | smiles = Cc1ccc(cc1)S(=O)(=O)N2CCc4ccccc4[C@@H]2[C@@H]3CCC(=O)O3 }}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] See also
References1. ^US Patent 6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders {{Hypnotics}}{{GABAAR PAMs}}{{GABAergics}}{{sedative-stub}}2. ^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}} 3. ^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}} 6 : Sedatives|Tetrahydroisoquinolines|Tetrahydrofurans|Lactones|GABAA receptor positive allosteric modulators|GABAA-rho receptor negative allosteric modulators |
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