Lobeline has been sold, in tablet form, for use as a smoking cessation aid, and may have application in the treatment of other drug addictions such as addiction to amphetamines, cocaine, or alcohol. However, there is limited clinical evidence of any efficacy.
Ingestion of lobeline may cause nausea, vomiting, diarrhea, coughing, dizziness, visual disturbances, hearing disturbances, mental confusion, weakness, slowed heart rate, increased blood pressure, increased breathing rate, tremors, and seizures. Lobeline has a narrow therapeutic index; the potentially beneficial dose of lobeline is very close to the toxic dose.
Analogous compounds, such as lobelane (a minor alkaloid found in the same plants) and its synthetic derivatives have similar biological effects with somewhat different relative affinities to VMAT and other proteins. A related alkaloid sedamine, with only one 2-phenylethyl group on the piperidine ring and found in plants of genus sedum, is known to be an inhibitor of pea seedlings amine oxidase, but its affinity to proteins such as the dopamine transporter has apparently not been tested.
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^Miller, D. K.; Harrod, S. B.; Green, T. A.; Wong, M. Y.; Bardo, M. T.; Dwoskin, L. P. (2003). "Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats". Pharmacology Biochemistry and Behavior. 74 (2): 279–86. doi:10.1016/s0091-3057(02)00996-6. PMID12479946.
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^National Center for Biotechnology Information. PubChem Database. (-)-Sedamine, CID=442657, [pubchem.ncbi.nlm.nih.gov] (accessed on July 7, 2019)
^Ŝárka Adámková, Ivo Frébort, Marek Ŝebela & Pavel Peĉ, "Probing the Active Site of Pea Seedlings Amine Oxidase with Optical Antipodes of Sedamine Alkaloids", Journal of Enzyme Inhibition Volume 16, 2001 - Issue 4