α3 nachr

α7nAChRModulator-3 (Compound 6p) is a positive allosteric modulator of α7nAChR, with an IC50 value of 1.3 μM. This compound is utilized in studies to inhibit auditory gating deficits in mouse models resembling schizophrenia.

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

α-Conotoxin PIA TFA is an nAChR (nicotinic acetylcholine receptor) antagonist that primarily targets nAChR subtypes containing α6 and α3 subunits, exhibiting significantly higher selectivity for α6/α3β2β3 nAChR than α3β2 nAChR, and may be used for Parkinson's disease and schizophrenia.

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