Drug intelligence / Profile preview

Bietaserpine

Development stage
Discontinued
Lead developer
Sandoz
Modality
Small Molecules
01

Overview

Bietaserpine is a small molecule drug and a derivative of reserpine, identified by code names such as DL 152 and N-diethylaminoethyl reserpine. It was investigated as an antihypertensive agent and also exhibited sedative effects. Its mechanism of action involves the inhibition of vesicular monoamine transporters (VMAT1 and VMAT2), similar to its parent compound reserpine. This inhibition leads to the depletion of monoamine neurotransmitters, including norepinephrine, dopamine, and serotonin, from synaptic vesicles. The resulting reduction in sympathetic nervous system activity contributes to its hypotensive effects.

Other names
N-diethylaminoethyl reserpine1-[2-(diethylamino)ethyl]reserpine
02

Targets

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

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