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Lobeline

Introduction

Overview

Overview

Lobeline is an alkaloid found in “Indian tobacco” (Lobelia inflata), “Devil’s tobacco” (Lobelia tupa), “cardinal flower” (Lobelia cardinalis), “great lobelia” (Lobelia siphilitica), and Hippobroma longiflora. Additionally, it is also found in Lobelia chinensis. In its pure form it is a white amorphous powder which is freely soluble in water.

Potential uses

Potential uses

Lobeline has been studied for its potential use as a smoking cessation aid,[1][2][3] and may have application in the treatment of other drug addictions such as addiction to amphetamines,[4][5] cocaine,[6] or alcohol.[7]

Pharmacology

Pharmacology

Lobeline has multiple mechanisms of action, acting as a VMAT2 ligand,[8][9][10] which stimulates dopamine release to a moderate extent when administered alone, but reduces the dopamine release caused by methamphetamine.[11][12] It also inhibits the reuptake of dopamine and serotonin,[13] and acts as a mixed agonist–antagonist at nicotinic acetylcholine receptors[14][15] to which it binds at the subunit interfaces of the extracellular domain.[16] It is also an antagonist at ΞΌ-opioid receptors.[17]

References

References

  1. ↑ Stead LF, Hughes JR; Hughes (2012). “Lobeline for smoking cessation”. Cochrane Database Syst Rev. 2: CD000124. doi:10.1002/14651858.CD000124.pub2. PMIDΒ 22336780.
  2. ↑ Marlow, S. P.; Stoller, J. K. (2003). “Smoking cessation”. Respiratory care. 48 (12): 1238–54, discussion 1254–6. PMIDΒ 14651764.
  3. ↑ Buchhalter, A. R.; Fant, R. V.; Henningfield, J. E. (2008). “Novel pharmacological approaches for treating tobacco dependence and withdrawal: Current status”. Drugs. 68 (8): 1067–88. PMIDΒ 18484799.
  4. ↑ Neugebauer, N. M.; Harrod, S. B.; Stairs, D. J.; Crooks, P. A.; Dwoskin, L. P.; Bardo, M. T. (2007). “Lobelane decreases methamphetamine self-administration in rats”. European Journal of Pharmacology. 571 (1): 33–8. doi:10.1016/j.ejphar.2007.06.003. PMCΒ 2104779. PMIDΒ 17612524.
  5. ↑ Eyerman, D. J.; Yamamoto, B. K. (2005). “Lobeline attenuates methamphetamine-induced changes in vesicular monoamine transporter 2 immunoreactivity and monoamine depletions in the striatum”. Journal of Pharmacology and Experimental Therapeutics. 312 (1): 160–9. doi:10.1124/jpet.104.072264. PMIDΒ 15331654.
  6. ↑ Polston, J. E.; Cunningham, C. S.; Rodvelt, K. R.; Miller, D. K. (2006). “Lobeline augments and inhibits cocaine-induced hyperactivity in rats”. Life Sciences. 79 (10): 981–90. doi:10.1016/j.lfs.2006.05.006. PMIDΒ 16765386.
  7. ↑ Farook, J. M.; Lewis, B; Gaddis, J. G.; Littleton, J. M.; Barron, S (2009). “Lobeline, a nicotinic partial agonist attenuates alcohol consumption and preference in male C57BL/6J mice”. Physiology & Behavior. 97 (3–4): 503–6. doi:10.1016/j.physbeh.2009.02.031. PMIDΒ 19268674.
  8. ↑ Zheng, G; Dwoskin, L. P.; Crooks, P. A. (2006). “Vesicular monoamine transporter 2: Role as a novel target for drug development”. The AAPS Journal. 8 (4): E682–92. doi:10.1208/aapsj080478. PMCΒ 2751365. PMIDΒ 17233532.
  9. ↑ Zheng, F; Zheng, G; Deaciuc, A. G.; Zhan, C. G.; Dwoskin, L. P.; Crooks, P. A. (2007). “Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2”. Bioorganic & Medicinal Chemistry. 15 (8): 2975–92. doi:10.1016/j.bmc.2007.02.013. PMCΒ 2001191. PMIDΒ 17331733.
  10. ↑ Zheng, G; Dwoskin, L. P.; Deaciuc, A. G.; Norrholm, S. D.; Crooks, P. A. (2005). “Defunctionalized lobeline analogues: Structure-activity of novel ligands for the vesicular monoamine transporter”. Journal of Medicinal Chemistry. 48 (17): 5551–60. doi:10.1021/jm0501228. PMCΒ 3617589. PMIDΒ 16107155.
  11. ↑ Wilhelm, C. J.; Johnson, R. A.; Eshleman, A. J.; Janowsky, A (2008). “Lobeline effects on tonic and methamphetamine-induced dopamine release”. Biochemical Pharmacology. 75 (6): 1411–5. doi:10.1016/j.bcp.2007.11.019. PMCΒ 2435375. PMIDΒ 18191815.
  12. ↑ Wilhelm, C. J.; Johnson, R. A.; Lysko, P. G.; Eshleman, A. J.; Janowsky, A (2004). “Effects of methamphetamine and lobeline on vesicular monoamine and dopamine transporter-mediated dopamine release in a cotransfected model system”. Journal of Pharmacology and Experimental Therapeutics. 310 (3): 1142–51. doi:10.1124/jpet.104.067314. PMIDΒ 15102929.
  13. ↑ Zheng, G; Horton, D. B.; Deaciuc, A. G.; Dwoskin, L. P.; Crooks, P. A. (2006). “Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters”. Bioorganic & Medicinal Chemistry Letters. 16 (19): 5018–21. doi:10.1016/j.bmcl.2006.07.070. PMCΒ 3934794. PMIDΒ 16905316.
  14. ↑ Damaj, M. I.; Patrick, G. S.; Creasy, K. R.; Martin, B. R. (1997). “Pharmacology of lobeline, a nicotinic receptor ligand”. The Journal of pharmacology and experimental therapeutics. 282 (1): 410–9. PMIDΒ 9223582.
  15. ↑ 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. PMIDΒ 12479946.
  16. ↑ PDB entry 2bys. Hansen, S. B.; Sulzenbacher, G; Huxford, T; Marchot, P; Taylor, P; Bourne, Y (2005). “Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations”. The EMBO Journal. 24 (20): 3635–46. doi:10.1038/sj.emboj.7600828. PMCΒ 1276711. PMIDΒ 16193063.
  17. ↑ Miller, D. K.; Lever, J. R.; Rodvelt, K. R.; Baskett, J. A.; Will, M. J.; Kracke, G. R. (2007). “Lobeline, a potential pharmacotherapy for drug addiction, binds to mu opioid receptors and diminishes the effects of opioid receptor agonists”. Drug and Alcohol Dependence. 89 (2–3): 282–91. doi:10.1016/j.drugalcdep.2007.02.003. PMIDΒ 17368966.


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