Drug intelligence / Profile preview

lobeline hydrochloride

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Parenteral
01

Overview

Lobeline hydrochloride is a small molecule piperidine alkaloid derived from plants of the genus *Lobelia*, such as *Lobelia chinensis*. It acts as a nicotinic acetylcholine receptor (nAChR) agonist and mixed agonist-antagonist, specifically targeting the α3β2 and α4β2 neuronal subtypes. Beyond its cholinergic activity, lobeline hydrochloride functions as a ligand for the vesicular monoamine transporter 2 (VMAT2) and inhibits the reuptake of dopamine and serotonin. It also exhibits antagonist activity at μ-opioid receptors. Historically, the drug has been utilized as a respiratory stimulant in emergency medicine. It has also been extensively researched for its potential in smoking cessation and the treatment of addictions to substances such as cocaine, amphetamines, and alcohol. Shanghai Hefeng Pharmaceutical manufactures lobeline hydrochloride as a generic injectable product for first-aid and emergency use.

Other names
lobeline HClalpha-lobeline hydrochloride(-)-lobeline hydrochloridelobeline
02

Targets

VMAT2 (Vesicular monoamine transporter 2)SERT (Sodium-dependent serotonin transporter)MOR (Mu opioid receptor)DAT (Dopamine plasma membrane transport protein)CHRNA7 (α7 nicotinic receptor)

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