产品
编 号：F339496
分子式：C24H30Cl3NO
分子量：454.86
分子式：C24H30Cl3NO
分子量：454.86
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CAS No: 371980-94-8
产品详情
生物活性：
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with Ki values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
体内研究：
rel-SB-612111 hydrochloride (intravenous?injection; 0.6-10 nmol/mouse)antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg.rel-SB-612111 hydrochloride (intravenous?injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected.Animal Model:Male rats
Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration:Intravenous?injection; single dose
Result:Had antihyperalgesic effects on carrageenan-induced rat paw.
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with Ki values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
体内研究：
rel-SB-612111 hydrochloride (intravenous?injection; 0.6-10 nmol/mouse)antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg.rel-SB-612111 hydrochloride (intravenous?injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected.Animal Model:Male rats
Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg
Administration:Intravenous?injection; single dose
Result:Had antihyperalgesic effects on carrageenan-induced rat paw.
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