Drug intelligence / Profile preview

rauwolscine

Development stage
Preclinical
Modality
Small Molecules
Administration
Transdermal, Oral, Intravenous
01

Overview

Rauwolscine is a monoterpene indole alkaloid and a stereoisomer of yohimbine (specifically alpha-yohimbine) found in plants of the genus *Rauvolfia*. It is a potent and selective antagonist of alpha-2 adrenergic receptors, with high affinity for the alpha-2A, alpha-2B, and alpha-2C subtypes. Due to its pharmacological profile, it is widely utilized as a research tool and radioligand in studies of adrenergic signaling. Beyond its primary adrenergic activity, rauwolscine has demonstrated antagonistic effects at the adenosine A2b receptor, agonistic activity at the 5-HT4 receptor, and potential inhibitory properties against PARP-1 and VEGFR-2. It is also commonly encountered as a dietary supplement ingredient, often marketed for weight loss and athletic performance. Research has explored its potential roles in managing conditions such as arterial thrombosis, neuropathic pain, and cancer, as well as its association with metabolic traits like type 2 diabetes.

Other names
alpha-yohimbinecorynanthidine17-alpha-hydroxy-20-alpha-yohimban-16-beta-carboxylic acid methyl ester
02

Targets

5-HT2 (5-HT2 receptor family)ADRA2B (α2B)VEGFR2 (Vascular endothelial growth factor receptor 2)ADRA2C (α2C)ADRA2A (α2A)

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