(-)-Lobeline hydrochloride

Non Antibodies

nAChR

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

373, 9

A Potent nAChR Antagonist

Ethanol/water. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

(-)-Lobeline hydrochloride is a high affinity modulator of nicotinic acetylcholine receptors. It inhibits α7 nAChRs with IC50 of 8.5 µM1.It also acts on the α4/β2 combination2.

Yes

Nicotinic acetylcholine receptors (nAChRs) are important neuromodulatory cation channels which short-circuit their assimilating membrane by their primary endogenous agonist acetylcholine (ACh)1. nAChRs are highly expressed in myocytes and neurons and are comprised of at least 17 studied subunits, that can be classified into two types: α (α1 - α10) and non-α (β1-4, γ, δ and ε). Various nAChR subunits co-assemble to create muscular (α1β1γδ and α1β1εδ) and neuronal channels which are found in different and more restrictive combinations (α2-6 and β2-4 possible arrangements, e.g. α4β2)2, 3.Lobeline hydrochloride is a lipophylic alkaloid which either agonizes or antagonizes the nicotine-evoked response of nAChRs. Lobeline acts as an anxiolytic, a cognition enhancer and a neurotransmitter-release stimulant in the CNS, whereas it inhibits the response to ACh at the α7 subunit with an IC50 of 8.5 μM, and decreases the endplate potential at the neuromuscular junction - thus attenuates locomotor sensitization4-7. Moreover, its high affinity (Ki = 4-20 nM) to the α4β2, nAChR subtype, along with a nonselective binding to monoamine transporters, renders it capable of preventing the psychostimulatory effects of drugs of abuse8.