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Oliceridine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Oliceridine hydrochloride图片
CAS NO:1401031-39-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
TRV130 (hydrochloride)
产品介绍
Oliceridine hydrochloride 是 G 蛋白偏向 μ 阿片受体 (pEC50: 8.1) 的激动剂。

产品描述

Oliceridine hydrochloride is an agonist of G protein biased μ opioid receptor (pEC50: 8.1).

体外活性

Oliceridine elicits robust G protein signaling, with potency and efficacy similar to morphine [2].

体内活性

In mice, Robust antinociception, complete inhibition of gastrointestinal function produced by Oliceridine treatment, and weak abuse-related effects [1]. In an analgesic assay, Oliceridine displays an ED50 of 0.9 mg/kg. Oliceridine analgesia is reversible in mice by administration of 3 mg/kg naloxone s.c. 15 minutes after Oliceridine dosing. In the rat 52°C hot plate, Oliceridine is 10-fold more potent than morphine with ED50 of 0.32 and 3.2 mg/kg, respectively. Oliceridine (0.3 mg/kg, s.c.) possesses an improved therapeutic index of analgesia to constipation relative to morphine in mice [2]. Oliceridine (1.2 mg/kg, s.c.) significantly depresses the respiration of mice [3].

Cas No.

1401031-39-7

分子式

C22H31ClN2O2S

分子量

423.01

别名

TRV130 (hydrochloride)

储存和溶解度

DMSO:38 mg/mL (89.83 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years