Rauwolscine hydrochloride
(Synonyms: 萝芙素盐酸盐; α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride) 目录号 : GC16250
A reversible α2-adrenergic receptor antagonist
Cas No.:6211-32-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Kinase experiment: |
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]. |
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References: [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. |
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Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM.
[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 (Ki human=14.3 nM, Ki 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].
References:
[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.
[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.
[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.
[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.
| Cas No. | 6211-32-1 | SDF | |
| 别名 | 萝芙素盐酸盐; α-Yohimbine hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride | ||
| 化学名 | (1S,2S,4aS,13bS,14aS)-methyl 2-hydroxy-1,2,3,4,4a,5,7,8,13,13b,14,14a-dodecahydroindolo[2',3':3,4]pyrido[1,2-b]isoquinoline-1-carboxylate hydrochloride | ||
| Canonical SMILES | O[C@@H]1[C@@H](C(OC)=O)[C@@H]2[C@H](CC1)CN3[C@H](C(NC4=CC=CC=C54)=C5CC3)C2.Cl | ||
| 分子式 | C21H26N2O3.HCl | 分子量 | 390.91 |
| 溶解度 | DMF: 0.1 mg/ml,DMSO: 2 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5581 mL | 12.7907 mL | 25.5813 mL |
| 5 mM | 0.5116 mL | 2.5581 mL | 5.1163 mL |
| 10 mM | 0.2558 mL | 1.2791 mL | 2.5581 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。