Yohimbine
(Synonyms: 育亨宾) 目录号 : GC37952
An α2-adrenoceptor antagonist
Cas No.:146-48-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Yohimbine is a natural alkaloid that has highest affinity for α2-adrenergic receptors (pKis = 8.2, 8.7, and 9.6 for human α2A, α2B, and α2C, respectively), with antagonist activity at these receptors.1,2 It less potently antagonizes serotonin 5-HT1 receptors (pKis = 7.3, 6.8, and 7.6 for human HT1A, HT1B, and HT1D, respectively) and α1-adrenergic receptors (pKis = 6.7, 6.8, and 6.8 for human α1A, α1B, and α1D, respectively).1 Yohimbine is used in veterinary medicine to reverse the sedative effects of α2-agonists.
1.Millan, M.J., Newman-Tancredi, A., Audinot, V., et al.Agonist and antagonist actions of yohimbine as compared to fluparoxan at α2-adrenergic receptors (AR)s, serotonin (5-HT)1A, 5-HT1B, 5-HT1D and dopamine D2 and D3 receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive statesSynapse35(2)79-95(2000) 2.Schwartz, D.D., and Clark, T.P.Selectivity of atipamezole, yohimbine and tolazoline for alpha-2 adrenergic receptor subtypes: Implications for clinical reversal of alpha-2 adrenergic receptor mediated sedation in sheepJ. Vet. Pharmacol. Ther.21(5)342-347(1998)
| Cas No. | 146-48-5 | SDF | |
| 别名 | 育亨宾 | ||
| Canonical SMILES | [H][C@]12C(NC3=C4C=CC=C3)=C4CCN1C[C@@]5(CC[C@H](O)[C@H](C(OC)=O)[C@]5(C2)[H])[H] | ||
| 分子式 | C21H26N2O3 | 分子量 | 354.44 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.8214 mL | 14.1068 mL | 28.2135 mL |
| 5 mM | 0.5643 mL | 2.8214 mL | 5.6427 mL |
| 10 mM | 0.2821 mL | 1.4107 mL | 2.8214 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。
A literature perspective on the pharmacological applications of Yohimbine
Ann Med 2022 Dec;54(1):2861-2875.PMID:36263866DOI:10.1080/07853890.2022.2131330.
Introduction: Phytochemicals have garnered much attention because they are useful in managing several human diseases. Yohimbine is one such phytochemical with significant pharmacological potential and could be exploited for research by medicinal chemists. It is an indole alkaloid obtained from various natural/synthetic sources.Aims and Results: The research on Yohimbine started early, and its use as a stimulant and aphrodisiac by humans has been reported for a long time. The pharmacological activity of Yohimbine is mediated by the combined action of the central and peripheral nervous systems. It selectively blocks the pre and postsynaptic α2-adrenergic receptors and has a moderate affinity for α1 and α2 subtypes. Yohimbine also binds to other behaviourally relevant monoaminergic receptors in the following order: α-2 NE > 5HT-1A>, 5HT-1B > 1-D > D3 > D2 receptors.Conclusion: The current review highlights some significant findings that contribute to developing yohimbine-based drugs. It also highlights the therapeutic potential of Yohimbine against selected human diseases. However, further research is recommended on the pharmacokinetics, molecular mechanisms, and drug safety requirements using well-designed randomized clinical trials to produce Yohimbine as a pharmaceutical agent for human use.Key MessagesYohimbine is a natural indole alkaloid with significant pharmacological potential.Humans have used it as a stimulant and aphrodisiac from a relatively early time.It blocks the pre- and postsynaptic α2-adrenergic receptors that could be exploited for managing erectile dysfunction, myocardial dysfunction, inflammatory disorders, and cancer.
Yohimbine: a clinical review
Pharmacol Ther 2001 Sep;91(3):215-43.PMID:11744068DOI:10.1016/s0163-7258(01)00156-5.
Although Yohimbine (YOH) has been available for the treatment of male erectile dysfunction (ED) for longer than Viagra, there is a perception that little is known about the clinical performance of the drug. This review attempts, by comprehensive analysis of the literature, to cover the clinical, pharmacological, and therapeutic profiles of YOH, relevant to its potential utility in the management of patients with ED. Relatively few well-designed studies have been completed. From these, however, it can be concluded that YOH as monotherapy possesses only modest efficacy in ED patients. In acute and chronic (long-term) studies, YOH has been found to be relatively free of side effects over the dose range predicted to be effective in ED. At much higher doses, the most frequently observed effects, consistent with the primary pharmacological action of the drug, are elevation of blood pressure, a slight anxiogenic action, and increased frequency of urination. These side effects are all easily reversible on termination of YOH therapy. There is increasing evidence that the erectogenic action of YOH can be augmented by concomitant administration of agents that augment the release and/or action of nitric oxide in the corpus cavernosum. YOH has yet to be studied in female sexual dysfunction. Overall, the benefit risk profile of YOH would indicate that it has potential, more probably as part of a combination strategy, e.g., with a drug that enhances the nitric oxide pathway, in the treatment of ED.
Yohimbine: the effects on body composition and exercise performance in soccer players
Res Sports Med 2006 Oct-Dec;14(4):289-99.PMID:17214405DOI:10.1080/15438620600987106.
The main aim of this study was to determine the effects of Yohimbine supplementation on body composition and exercise performance in professional soccer players. The athletes (20 top-level male soccer players) were allocated to two randomly assigned trials. Subjects in the Yohimbine group orally ingested tablets that contains Yohimbine at a dose of 20 milligrams per day in two equal doses for 21 days. Subjects in the placebo group ingested an equal number of identical-looking pills that contained cellulose. There were no statistically significant changes in body mass and muscle mass within or between trials (p > 0.05) after the supplementation protocol. Percentage of body fat significantly decreased in the Yohimbine group after the supplementation protocol (9.3 +/- 1.1 vs. 7.1 +/- 2.2%; p < 0.05). Furthermore, fat mass was significantly lower in the Yohimbine versus placebo trial at postsupplementation assessment (7.1 +/- 2.2 vs. 9.2 +/- 1.9%; p < 0.05). There were no changes in exercise performance indicators (bench and leg press, vertical jump, dribble and power test results, shuttle run) within or between. trials (p > 0.05). No subject reported any side effects from Yohimbine. The results of the current study indicate that supplementation with Yohimbine combined with resistance training does not significantly alter the body mass, muscle mass, or performance indicators in professional soccer players. Nonetheless, Yohimbine supplementation appears to be suitable as a fat loss strategy in elite athletes.
Yohimbine use for physical enhancement and its potential toxicity
J Diet Suppl 2011 Dec;8(4):346-54.PMID:22432773DOI:10.3109/19390211.2011.615806.
Yohimbine is a naturally sourced pharmacological agent, which produces hyperadrenergic physiological effects. In excess doses, it may typically cause agitation, anxiety, hypertension, and tachycardia. There is no conclusive evidence for this drug to be of benefit in bodybuilding, exercise tolerance, physical performance, or desirable alterations of body mass. Although tolerated generally well in low doses, the potential for dose-dependent toxicity should be recognized.
Yohimbine in the treatment of erectile disorder
Br J Clin Pract 1994 May-Jun;48(3):133-6.PMID:8031688doi
Yohimbine is an alkaloid derived mainly from the bark of the African tree, Pausinystalia yohimbe. Although many pharmacological properties of Yohimbine have been described, at the plasma concentration attained at recommended dosages in man the predominant activity is antagonism of alpha 2-adrenoceptors. For more than 70 years Yohimbine has been used as a treatment for male and female sexual difficulties. It has enjoyed a reputation as an aphrodisiac although no effect on sexual drive in humans has been adequately demonstrated. Yohimbine has been evaluated in the management of erectile disorder by means of placebo-controlled but often poorly designed trials. It does appear to have a modest therapeutic benefit over placebo, particularly in essentially psychogenic erectile disorder, and is generally well tolerated. Yohimbine is not licensed in the UK.