Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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Purity: ≥ 98%
Yohimbine HCl (Antagonil; Corynine; Quebrachin; Quebrachine; Yohimex; Yocon; APHRODINE; Aphrodyne; Aphrosol; Johimbin), the hydrochloride salt of Yohimbine, is a potent alpha 2-adrenoreceptor antagonist used as a mydriatic for the treatment of impotence. It is an indole alkaloid derived from the bark of the Pausinystalia yohimbe tree in Central Africa. Yohimbine is also alleged to be an aphrodisiac. Yohimbine may exert its beneficial effect on erectile ability through blockade of central alpha 2-adrenergic receptors producing an increase in sympathetic drive secondary to an increase in norepinephrine release and in firing rate of cells in the brain noradrenergic nuclei.
Targets |
alpha 2-adrenergic receptor
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ln Vitro |
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ln Vivo |
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Animal Protocol |
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ADME/Pharmacokinetics |
Absorption
Rapidly absorbed following oral administration. Bioavailability is highly variable, ranging from 7 to 87% (mean 33%). Metabolism / Metabolites Yohimbine appears to undergo extensive metabolism in an organ of high flow such as the liver or kidney, however, the precise metabolic fate of yohimbine has not been fully determined. Biological Half-Life Elimination half-life is approximately 36 minutes. |
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Toxicity/Toxicokinetics |
rat LD50 intraperitoneal 55 mg/kg
Hepatotoxicity In small clinical trials and case series, yohimbine therapy has not been linked to serum enzyme elevations or clinical liver disease. Although yohimbine is often found in weight loss and muscle building herbal combinations, it has not been associated with cases of clinically apparent acute liver injury.br> Likelihood score: E (unlikely cause of clinically apparent liver injury). |
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References | |||
Additional Infomation |
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
See also: Yohimbine (has active moiety). |
Molecular Formula |
C21H26N2O3.HCL
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Molecular Weight |
390.9
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Exact Mass |
390.171
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Elemental Analysis |
C, 64.52; H, 6.96; Cl, 9.07; N, 7.17; O, 12.28
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CAS # |
65-19-0
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Related CAS # |
Rauwolscine hydrochloride; 6211-32-1; Yohimbine; 146-48-5; Rauwolscine; 131-03-3
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PubChem CID |
6169
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Appearance |
White to light yellow solid powder
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Boiling Point |
542.979ºC at 760 mmHg
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Melting Point |
288-290 °C (dec.)(lit.)
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Flash Point |
282.184ºC
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Index of Refraction |
103 ° (C=1, H2O)
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LogP |
3.387
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Hydrogen Bond Donor Count |
3
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Hydrogen Bond Acceptor Count |
4
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Rotatable Bond Count |
2
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Heavy Atom Count |
27
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Complexity |
555
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Defined Atom Stereocenter Count |
5
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SMILES |
Cl[H].O([H])[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])C([H])([H])N3C([H])([H])C([H])([H])C4C5=C([H])C([H])=C([H])C([H])=C5N([H])C=4[C@]3([H])C([H])([H])[C@]2([H])[C@@]1([H])C(=O)OC([H])([H])[H]
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InChi Key |
PIPZGJSEDRMUAW-VJDCAHTMSA-N
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InChi Code |
InChI=1S/C21H26N2O3.ClH/c1-26-21(25)19-15-10-17-20-14(13-4-2-3-5-16(13)22-20)8-9-23(17)11-12(15)6-7-18(19)24;/h2-5,12,15,17-19,22,24H,6-11H2,1H3;1H/t12-,15-,17-,18-,19+;/m0./s1
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Chemical Name |
methyl (1S,15R,18S,19R,20S)-18-hydroxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate;hydrochloride
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5582 mL | 12.7910 mL | 25.5820 mL | |
5 mM | 0.5116 mL | 2.5582 mL | 5.1164 mL | |
10 mM | 0.2558 mL | 1.2791 mL | 2.5582 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06018727 | Not yet recruiting | Dietary Supplement: Yohimbine Drug: Hydrocortisone |
Borderline Personality Disorder | University of North Carolina, Chapel Hill |
March 2024 | Phase 4 |
NCT00958880 | Completed | Drug: Yohimbine Hydrochloride Drug: Sugar Pill |
Social Anxiety Disorder | Southern Methodist University | March 2009 | Phase 3 |
NCT00078715 | Completed | Drug: Yohimbine hydrochloride Drug: Placebo |
Depression, Involutional Major Depresssion |
National Institute of Mental Health (NIMH) |
March 2004 | Phase 2 |