Drug intelligence / Profile preview

lobeline

Development stage
Phase 2
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Inhalation, Transdermal, Intravenous
01

Overview

Lobeline is a piperidine alkaloid found in several plants of the Lobelia genus, including Indian tobacco (Lobelia inflata). It has been used historically as a smoking cessation aid and for respiratory disorders, though clinical evidence supporting its efficacy is limited. Lobeline acts primarily as a ligand at the vesicular monoamine transporter 2 (VMAT2), inhibiting dopamine uptake and promoting dopamine release from storage vesicles within presynaptic terminals. It also inhibits reuptake of dopamine and serotonin, functions as a mixed agonist–antagonist at nicotinic acetylcholine receptors (notably α3β2 and α4β2 subtypes), antagonizes μ-opioid receptors, and may inhibit P-glycoprotein. These mechanisms underlie its potential to modulate neurochemical pathways involved in addiction and neurodegenerative diseases such as Parkinson's disease. Despite preclinical promise for treating drug dependence (nicotine, amphetamines) and possible neuroprotective effects, there is little robust clinical evidence for approved therapeutic use[1][3][5][6][7][8].

Brand names
bantron
Other names
lobelinelobeline hydrochloride
02

Targets

DAT (Dopamine plasma membrane transport protein)α3β2 nAChR (α3β2 nicotinic receptor)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)SERT (Sodium-dependent serotonin transporter)VMAT2 (Vesicular monoamine transporter 2)MOR (Mu opioid receptor)ABCB1 (P-glycoprotein)

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