Drug intelligence / Profile preview

r-propranolol

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous, Rectal, Enteral, Sublingual, Buccal
01

Overview

r-propranolol is the R(+)-enantiomer of propranolol, a nonselective beta-adrenergic receptor antagonist, isolated from the usual racemic mixture in which the S(–)-enantiomer is primarily responsible for beta-blocking activity. As a single enantiomer, r-propranolol has markedly lower affinity for β1- and β2-adrenergic receptors than s-propranolol and is mainly of interest as a pharmacological tool and research compound to study stereoselective pharmacokinetics and pharmacodynamics of propranolol rather than as a therapeutic agent. It is a small-molecule synthetic beta-blocker derivative and shares the general physicochemical properties and metabolic pathways of propranolol, but with substantially reduced beta-adrenergic antagonism.

02

Targets

ADRB1 (β1)ADRB2 (β2)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))NaV (Voltage-gated sodium channels)

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