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Rauwolscine hydrochloride

Rauwolscine hydrochloride

产品编号 T4429   CAS 6211-32-1
别名: Corynanthidine hydrochloride, 盐酸育亨宾碱, 萝芙素盐酸盐, α-Yohimbine hydrochloride, Isoyohimbine hydrochloride

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) 是一种高选择性的 α2 adrenergic 受体拮抗剂,Ki=12 nM。

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Rauwolscine hydrochloride Chemical Structure
Rauwolscine hydrochloride, CAS 6211-32-1
规格 价格/CNY 货期 数量
50 mg ¥ 415 现货
1 mL * 10 mM (in DMSO) ¥ 456 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Rauwolscine hydrochloride (T4429)
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参考文献
结构类型
产品描述 Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , 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 hydrochloride 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].
靶点活性 α2-adrenoceptor:12 nM (Ki)
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].
别名 Corynanthidine hydrochloride, 盐酸育亨宾碱, 萝芙素盐酸盐, α-Yohimbine hydrochloride, Isoyohimbine hydrochloride
分子量 390.9
分子式 C21H27ClN2O3
CAS No. 6211-32-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 13.75 mg/mL (35.18 mM), Heating is recommended.

H2O: 5 mM, Heating is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.5582 mL 12.791 mL 25.582 mL 63.955 mL
5 mM 0.5116 mL 2.5582 mL 5.1164 mL 12.791 mL
DMSO 10 mM 0.2558 mL 1.2791 mL 2.5582 mL 6.3955 mL
20 mM 0.1279 mL 0.6395 mL 1.2791 mL 3.1977 mL

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TargetMol Library Books参考文献

1. Perry B D, U'Prichard D C. [3H] Rauwolscine (α-yohimbine): a specific antagonist radioligand for brain α2-adrenergic receptors[J]. European journal of pharmacology, 1981, 76(4): 461-464. 2. De Vos H, Czerwiec E, De Backer J P, et al. [3H] Rauwolscine behaves as an agonist for the 5-HTa receptors in human frontal cortex membranes[J]. European Journal of Pharmacology: Molecular Pharmacology, 1991, 207(1): 1-8. 3. Wainscott D B, Sasso D A, Kursar J D, et al. [3H] Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2B (5-HT2B) receptor[J]. Naunyn-Schmiedeberg's archives of pharmacology, 1997, 357(1): 17-24. 4. Neylon C B, Summers R J. [3H]‐rauwolscine binding to α2‐adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species[J]. British journal of pharmacology, 1985, 85(2): 349-359. 5. Cottingham C, Wang Q. α2 adrenergic receptor dysregulation in depressive disorders: Implications for the neurobiology of depression and antidepressant therapy[J]. Neuroscience & Biobehavioral Reviews, 2012, 36(10): 2214-2225.
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相关化合物库

该产品包含在如下化合物库中:
抑制剂库 GPCR靶点分子库 神经退行性疾病化合物库 膜蛋白靶向化合物库 神经信号分子库 已知活性化合物库 生物碱类天然产物库 抗高血压化合物库 抗阿尔茨海默症化合物库 肾上腺素能受体化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

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