Puneet Varma (Editor)

Yohimbine

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Routes of administration
  
Oral

PubChem CID
  
8969

DrugBank
  
DB01392

Biological half-life
  
0.25-2.5 hours

Bioavailability
  
7-86% (mean 33%)

CAS Number
  
146-48-5

IUPHAR/BPS
  
102

CAS ID
  
146-48-5

Formula
  
C21H26N2O3

Excretion
  
Urine (as metabolites)

Yohimbine Yohimbine NOOTRIMENTcom

Legal status
  
AU: S4 (Prescription only) US: Dietary supplement

Molar mass
  
354.44 g/mol (base); 390.90 g/mol (hydrochloride)

ATC code
  
G04BE04 (WHO) QV03AB93 (WHO)

Yohimbine (/jˈhɪmbn/) is an indole alkaloid derived from the bark of the Pausinystalia yohimbe tree in Central Africa. It is a veterinary drug used to reverse sedation in dogs and deer. Yohimbine has been studied as a potential treatment for erectile dysfunction but there is insufficient evidence to rate its effectiveness. Extracts from yohimbe have been marketed as dietary supplements for improving sexual function.

Contents

Yohimbine Yohimbine YHCL Updated 16Jan2016

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Uses

Yohimbine is a drug used in veterinary medicine to reverse the effects of xylazine in dogs and deer.

Yohimbe extracts, which contain yohimbine, have been used in traditional medicine and marketed as dietary supplements.

Toxicity

Yohimbine Yohimbine HCL Review

Depending on dosage, yohimbine can either increase or decrease systemic blood pressure (through vasoconstriction or vasodilation, respectively). Because yohimbine has highest affinity for the α2 receptor, small doses can increase blood pressure by causing a relatively selective α2 blockade. Yohimbine also, however, interacts with α1 receptors, albeit with lower affinity; therefore, at higher doses an α1 blockade can occur and supersede the effects of the α2 blockade, leading to a potentially dangerous drop in blood pressure. Higher doses of oral yohimbine may create numerous side effects, such as rapid heart rate, overstimulation, anomalous blood pressure, cold sweating, and insomnia.

Extracts and chemistry

Yohimbine The What And Why Of Yohimbe And Yohimbine

Yohimbe (Pausinystalia johimbe) is a tree that grows in western and central Africa; yohimbine was originally extracted from the bark of yohimbe in 1896 by Adolph Spiegel. In 1943 the correct constitution of yohimbine was proposed by Witkop. Fifteen years later, Van Tamelen used a 23-step synthesis to become the first person to achieve the synthesis of yohimbine.

Pharmacology

Yohimbine Yohimbine Wikipedia

Yohimbine has high affinity for the α2-adrenergic receptor, moderate affinity for the α1 receptor, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, 5-HT2B, and D2 receptors, and weak affinity for the 5-HT1E, 5-HT2A, 5-HT5A, 5-HT7, and D3 receptors. It behaves as an antagonist at α1-adrenergic, α2-adrenergic, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, and D2, and as a partial agonist at 5-HT1A. Yohimbine interacts with serotonin and dopamine receptors in high concentrations.

Sexual dysfunction

Yohimbine has been studied as a potential treatment for erectile dysfunction but there is insufficient evidence to rate its effectiveness. It is illegal in the United States to market an over the counter product containing yohimbine as a treatment for erectile dysfunction without getting FDA approval to do so.

Yohimbine Yohimbine HCL Yohimbe Bark Extract Nootropic Effects and Benefits

Yohimbine blocks the pre- and post-synaptic α2 receptors. Blockade of post-synaptic α2 receptors causes only minor corpus cavernosum smooth muscle relaxation, due to the fact that the majority of adrenoceptors in the corpus cavernosum are of the α1 type. Blockade of pre-synaptic α2 receptors facilitates the release of several neurotransmitters in the central and peripheral nervous system — thus in the corpus cavernosum — such as nitric oxide and norepinephrine. Whereas nitric oxide released in the corpus cavernosum is the major vasodilator contributing to the erectile process, norepinephrine is the major vasoconstrictor through stimulation of α1 receptors on the corpus cavernosum smooth muscle. Under physiologic conditions, however, nitric oxide attenuates norepinephrine vasoconstriction.

Yohimbine Yohimbe Or Yohimbine HCL

References

Yohimbine Wikipedia