α6 nachr

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

α-Conotoxin PIA TFA, targeting nicotinic acetylcholine receptor (nAChR) subtypes with α6 and α3 subunits, acts as an antagonist. This compound shows promise for research into Parkinson's disease and schizophrenia [1].

CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].

α-Conotoxin BuIA is a paralytic peptide neurotoxin that acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChR), with inhibitory concentration 50 (IC50) values of 0.258 nM for α6 α3β2, 1.54 nM for α6 α3β4, and 5.72 nM for α3β2. It serves to differentiate between nAChRs containing the β2- and β4-subunits and selectively inhibits αxβ2 nAChRs, exhibiting a potency hierarchy of α6>α3>α2>α4 [1].

α-Conotoxin TxID is a potent antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR) with an inhibitory half-maximal inhibitory concentration (IC50) of 12.5 nM. Its inhibitory activity is weaker against the closely related α6 α3β4 nAChR, with an IC50 of 94 nM. This compound holds potential for the development of novel smoking cessation drugs [1].

AN317 is a selective agonist for the nicotinic acetylcholine receptor (nAChR) containing α6β2, with dissociation constants (Ki) of 6.2 nM and 4.1 nM for the α6 α3β2β3 and α4β2 receptor subtypes, respectively. It induces dopamine release in rat striatal synaptosomes, enhances the activity of dopaminergic neurons in the substantia nigra, and exhibits protective effects against the dopaminergic neurotoxin MPP+ in rat neurons. AN317 also demonstrates favorable pharmacokinetic properties in rats and permeability across the blood-brain barrier (BB).

α-Conotoxin PIA acetate is an antagonist of nicotinic acetylcholine receptor (nAChR) mainly targeting α6 and α3 subunits.