rel-SB-612111 hydrochloride

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CAS NO:

371980-94-8

rel-SB-612111 hydrochloride 是一种新型高效的人阿片受体孤儿受体 (ORL-1) 拮抗剂，对 hORL-1 具有较高的亲和力 (K_i=0.33 nM)。rel-SB-612111 hydrochloride 对 μ-，κ- 和 δ-receptor 的K_i值分别为 57.6 nM，160.5 nM 和 2109 nM。rel-SB-612111 hydrochloride 能有效拮抗 Nociceptin (HY-P0183) 在急性疼痛模型中的造成的痛觉作用。

生物活性

rel-SB-612111 hydrochloride is a novel and potenthuman opiate receptor-like orphan receptor (ORL-1)antagonist with a high affinity for hORL-1 (K_i=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors withK_ivalues 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^[1].

IC₅₀& Target

Ki: 0.33 nM (hORL-1)
Ki: 57.6 nM (μ-receptor); 160.5 nM (κ-receptor); 2109 nM (δ-receptor)^[1]

体内研究
(In Vivo)

rel-SB-612111 hydrochloride (intravenous injection; 0.6-10 nmol/mouse) antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED₅₀of 0.62 mg/kg^[1].
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^[1].

Animal Model:	Male rats^[1]
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.

分子量

454.86

Formula

C₂₄H₃₀Cl₃NO

CAS 号

371980-94-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.