Drug intelligence / Profile preview

yohimbine

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral
01

Overview

Yohimbine is a naturally occurring indole alkaloid derived from the bark of the African tree Pausinystalia johimbe and also found in Rauwolfia serpentina. It acts primarily as a selective antagonist of pre-synaptic alpha-2-adrenergic receptors, leading to increased release of norepinephrine and enhanced cholinergic activity. This mechanism underlies its use in treating erectile dysfunction (impotence), particularly of vascular, diabetic, or psychogenic origin. Yohimbine has also been used as a mydriatic (to dilate pupils), for weight loss (due to its lipolytic effects), and for conditions such as xerostomia (dry mouth) and orthostatic hypotension, though evidence for these uses is limited or inconclusive. At higher concentrations, yohimbine interacts with other receptors including alpha-1 adrenergic, several serotonin receptor subtypes (notably 5-HT1A as partial agonist; 5-HT1B/1D/2A/2B as antagonist), and dopamine D2/D3 receptors. Yohimbine is available by prescription in some countries but is also present in dietary supplements; however, supplement content can be highly variable[3][4][5][7][8].

Brand names
AphrodyneYocon
Other names
quebrachine
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR1B (5-Hydroxytryptamine Receptor 1B)HTR1D (5-hydroxytryptamine receptor 1D)HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)ADRA1A (α1A)ADRA2A (α2A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)

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