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

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

Lobeline (0.1-100 μM) hydrochloride evokes [³H]DA overflow calcium-independently^[1].
Lobeline hydrochloride 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) hydrochloride decreases d-methamphetamine self-administration in rats model^[3].
Lobeline (3 mg/kg; s.c.; 7 times during 7 sessions) hydrochloride 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.

373.92

Solid

C₂₂H₂₈ClNO₂

134-63-4

CN1[C@@H](CC(C2=CC=CC=C2)=O)CCC[C@H]1C[C@H](O)C3=CC=CC=C3.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

  [3]. Harrod SB, et al. Lobeline attenuates d-methamphetamine self-administration in rats. J Pharmacol Exp Ther. 2001 Jul;298(1):172-9.  [Content Brief]