Rauwolscine hydrochloride (Synonyms: 萝芙素盐酸盐; α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride)

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Rauwolscine hydrochloride是高效，选择性的 α2 adrenergic 受体拮抗剂，K_i 值为12 nM。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Rauwolscine 通常具有更好的水溶性和稳定性。

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Rauwolscine hydrochloride Chemical Structure

CAS No. : 6211-32-1

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Rauwolscine hydrochloride 的其他形式现货产品:

Rauwolscine

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生物活性
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参考文献

生物活性	Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a K_i of 12 nM.
IC₅₀ & Target	Ki: 12 nM (α2 adrenergic receptor)^[1]
体外研究 (In Vitro)	[³H]Rauwolscine binding to 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 and this conclusion is compatible with earlier functional studies, 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 relatively high affinity for the human receptor (K_i human=14.3 nM, K_i rat=35.8 nM)^[3]. Saturation studies shows that the affinity of [³H]Rauwolscine is similar in mouse, rat, rabbit, dog (2.33-3.03 nM) except man where it is significantly higher (0.98 nM) ^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Rauwolscine hydrochloride 相关抗体:
分子量	390.90
Formula	C₂₁H₂₇ClN₂O₃
CAS 号	6211-32-1
性状	固体
颜色	White to off-white
中文名称	萝芙素；育亨宾碱；洛芙素盐酸盐；萝芙素盐酸盐
结构分类	Alkaloids Indole Alkaloids
初始来源	植物其他科
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
纯度 & 产品资料	纯度: 99.92% 选择批次： Data Sheet (532 KB) SDS (480 KB) COA (294 KB) HNMR (267 KB) CNMR (286 KB) LCMS (268 KB) 元素分析报告 (218 KB) 产品使用指南 (1538 KB)
参考文献	[1]. Perry BD, et al. [3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. 1981 Dec 17;76(4):461-4. [Content Brief] [2]. De Vos H, et al. [3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes. Eur J Pharmacol. 1991 May 25;207(1):1-8. [Content Brief] [3]. Wainscott DB, et al. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24. [Content Brief] [4]. Neylon CB, et al. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349-59. [Content Brief]

Kinase Assay ^[1]	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 minivials containing 3.0 mL of a 95% Econofluor/5% Protosol 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Perry BD, et al. [3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. 1981 Dec 17;76(4):461-4. [Content Brief] [2]. De Vos H, et al. [3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes. Eur J Pharmacol. 1991 May 25;207(1):1-8. [Content Brief] [3]. Wainscott DB, et al. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24. [Content Brief] [4]. Neylon CB, et al. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349-59. [Content Brief]

Kinase Assay
^[1]

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 minivials containing 3.0 mL of a 95% Econofluor/5% Protosol 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Perry BD, et al. [3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. 1981 Dec 17;76(4):461-4. [Content Brief]

[2]. De Vos H, et al. [3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes. Eur J Pharmacol. 1991 May 25;207(1):1-8. [Content Brief]

[3]. Wainscott DB, et al. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24. [Content Brief]

[4]. Neylon CB, et al. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349-59. [Content Brief]

Rauwolscine hydrochloride 相关分类

Neurological Disease Endocrinology

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Keywords:

Rauwolscine6211-32-1α-YohimbineCorynanthidineIsoyohimbine萝芙素育亨宾碱洛芙素盐酸盐萝芙素盐酸盐Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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Rauwolscine hydrochloride (Synonyms: 萝芙素盐酸盐; α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride)

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Rauwolscine hydrochloride (Synonyms: 萝芙素盐酸盐; α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride)

Customer Review

Other Forms of Rauwolscine hydrochloride:

Rauwolscine hydrochloride 相关抗体

Rauwolscine hydrochloride 相关产品

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Rauwolscine hydrochloride 相关抗体:

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