Drug intelligence / Profile preview

reserpine

Development stage
Phase 3
Lead developer
Sandoz
Modality
Small Molecules
Administration
Oral
01

Overview

Reserpine is a small molecule alkaloid derived from the roots of Rauwolfia serpentina and Rauwolfia vomitoria. It acts as an adrenergic blocking agent primarily used for the treatment of mild to moderate hypertension and has also been used in psychiatric disorders such as schizophrenia and severe agitation. Its mechanism involves irreversible inhibition of the vesicular monoamine transporter 2 (VMAT2), which prevents norepinephrine and other monoamines (dopamine and serotonin) from being stored in synaptic vesicles. This leads to depletion of catecholamines from peripheral sympathetic nerve endings and central nervous system stores. The result is reduced sympathetic tone with lowered heart rate and blood pressure[1][2][4][5]. Due to its side effect profile—including risk of depression—its clinical use has declined but it remains a reference compound in research.

Brand names
SerpasilRenese-R
Other names
(−)-reserpine3,4,5-trimethoxybenzoyl methyl reserpate(3beta,16beta,17alpha,18beta,20alpha)-11,17-Dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic acid methyl esterReserpin
02

Targets

VMAT1 (Vesicular monoamine transporter type 1)VMAT2 (Vesicular monoamine transporter 2)

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