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Rauwolscine 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。
Rauwolscine hydrochloride图片
CAS NO:6211-32-1
包装与价格:
包装价格(元)
50 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
盐酸育亨宾碱
萝芙素盐酸盐
α-Yohimbine hydrochloride
Isoyohimbine hydrochloride
Corynanthidine hydrochloride
产品介绍
Rauwolscine hydrochloride 是一种高选择性的 α2 adrenergic 受体拮抗剂,Ki=12 nM。

产品描述

Rauwolscine, a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

体外活性

[3H]Rauwolscine binding to the α2 adrenergic receptor is reversible, stcreospccific, and saturable. [3H]Rauwolscine specifically labels both the high and low-affinity states of the α2 adrenergic receptor in brain membranes[1]. [3H]Rauwolscine also behaves as a 5-HT1A receptor agonist, indicating that rauwolscine (as well as yohimbine) has agonistic properties at the level of 5-HT autoreceptors[2]. When using [3H]5-HT as a radioligand, rauwolscine is determined to have a relatively high affinity for the human receptor (Ki: 14.3/35.8 nM, for human and rat)[3]. Saturation studies show that the affinity of [3H]Rauwolscine is similar in mouse, rabbit, rat, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) [4].

激酶实验

Fresh bovine frontal cortex is incubated in triplicate with [3H]Rauwolscine (82 Ci/mM, diluted). Incubation is terminated by filtration under reduced pressure over filters, which are then rinsed with ice-cold Tris-HCl buffer, dried overnight and added to disposable glass mini vials containing 3.0 mL of a 95% Econofluor/5% Protocol solution. Samples are counted by liquid scintillation spectrometry with an efficiency of 32%. (-)- [3H]Epinephrine binding to bovine cortex membranes is conducted at 25°C[1].

Cas No.

6211-32-1

分子式

C21H27ClN2O3

分子量

390.91

别名

盐酸育亨宾碱;萝芙素盐酸盐;α-Yohimbine hydrochloride;Isoyohimbine hydrochloride;Corynanthidine hydrochloride

储存和溶解度

H2O:5 mM,warmed
DMSO:25 mM,warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years