Every lot is tried & tested in a relevant biological assay.
It also acts on the α4/β2 combination2.
- Alomone Labs (-)-Lobeline hydrochloride inhibits the muscle α1/β1/γ/δ nAChR currents expressed in Xenopus oocytes.A. Time course of current reversible inhibition by increasing concentrations of (-)-Lobeline hydrochloride (#L-120). Currents were elicited by application of 100 µM Acetylcholine every 100 seconds from a holding potential of -80 mV B. Superimposed example traces of current response to acetylcholine before (Cont) and during 1, 5 and 10 µM (-)-Lobeline hydrochloride application.
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.