Lobeline sulfate  (Synonyms: α-Lobeline sulfate; L-Lobeline sulfate)

Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation^[1][2].

IC50: endogenous metabolite^[1]

Lobeline (0.1-100 μM) sulfate evokes [³H]DA overflow calcium-independently^[1].
Lobeline sulfate inhibits [³H]DA uptake into synaptosomes (IC₅₀=80 μM) and vesicles (IC₅₀=0.88 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lobeline (0.3-3.0 mg/kg; s.c.; single dose) sulfate decreases d-methamphetamine self-administration in rats model^[3].
Lobeline (3 mg/kg; s.c.; 7 times during 7 sessions) sulfate specifically decreases responding for d-Methamphetamine in a noncompetitive manner, and increases tolerance development^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

772.99

C₄₄H₅₆N₂O₈S

134-64-5

CN1[C@@H](CC(C2=CC=CC=C2)=O)CCC[C@H]1C[C@H](O)C3=CC=CC=C3.CN4[C@@H](CC(C5=CC=CC=C5)=O)CCC[C@H]4C[C@H](O)C6=CC=CC=C6.O=S(O)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Teng L, et al. Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake. J Pharmacol Exp Ther. 1997 Mar;280(3):1432-44.  [Content Brief]

  [2]. https://mayoclinic.pure.elsevier.com/en/publications/a-smoking-cessation-trial-with-lobeline-sulfate-a-pilot-st

  [3]. Monzurul Amin Roni, et al. Lobeline attenuates ethanol abstinence-induced depression-like behavior in mice. Alcohol. 2017 Jun:61:63-70.  [Content Brief]