nAChR Selective Inhibitors | Agonists | Antagonists | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5022 Varenicline Hydrochloride

Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.

Selective α4β2 nAChR, Ki: 0.14 nM; α6β2 nAChR, Ki: 0.12 nM
S5538 Tropisetron

Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

Selective α7 nAChR, Ki: 6.9 nM
S4162 Benzethonium Chloride

Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.

Selective α7 nAChRs, IC50: 122 nM; α4β2 nAChRs, IC50: 49 nM
S3298 Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.

Selective nAChR, Kd: 50 nM
S2629 PNU-120596

PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

Selective α7 nAChR, EC50: 216 nM
S2082 Adiphenine HCl

Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug.

Selective α4β4 nAChR, IC50: 6.3 μM; α4β2 nAChR, IC50: 3.7 μM; α3β4 nAChR, IC50: 1.8 μM; α1 nAChR, IC50: 1.9 μM
S0717 Varenicline (CP 526555) dihydrochloride

Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.

Selective α7 nAChRs, EC50: 18 μM; α3β4 nAChR, EC50: 55 μM; α4β2 nAChR, EC50: 2.3 μM
S3311 Myosmine

Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.

Selective nAChR, Ki: 3300 nM
S4505 Vinblastine (NSC-49842) sulfate

Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.

Selective nAChR, IC50: 8.9 μM
S4023 Procaine HCl

Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.

Selective nAChR, IC50: 45.5 μM
S0552 BNC210

BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).

Selective
S3202 Catharanthine

Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.

Selective
S4121 Succinylcholine Chloride Dihydrate

Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.

Selective
S2287 Cytisine

Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.

Selective
S4072 Decamethonium Bromide

Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.

Selective