- mAChR
- nAChR
- AChE
nAChR 选择性抑制剂 | 激动剂 | 拮抗剂 | 调节剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| S0702 | α-Conotoxin GI | α-Conotoxin GI, a 13-residue peptide originally isolated from the venom of the fish-hunting cone snail Conus geographus, acts as a competitive antagonist for the muscle-type nicotinic acetylcholine receptor (nAChR) with excellent selectivity for α/δ receptor subunit binding over α/γ. | Selective | |
| S6985 | Varenicline | Varenicline(CP 526555) is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. | Selective | |
| S2957 | Encenicline (EVP-6124) hydrochloride | Encenicline (EVP-6124) hydrochloride is a selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. | Selective | |
| S5022 | Varenicline Hydrochloride | Varenicline (CP 526555) Hydrochloride is a partial agonist of α4β2 nicotine acetylcholine receptor (nAChR) and α6β2 nicotine acetylcholine receptor (nAChR), with a Ki value of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively, in the striatum of rats. | Selective | α6β2 nAChR, Ki: 0.12 nM; α4β2 nAChR, Ki: 0.14 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 |
| S5930 | PNU 282987 HCl | PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors with Ki value of 26 nM for the rat receptor. | Selective | rat α7 nAChR, Ki: 26 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 | α4β2 nAChRs, IC50: 49 nM; α7 nAChRs, IC50: 122 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(NSC 129224) is a nicotinic receptor inhibitor, used as an antispasmodic drug. | Selective | α1 nAChR, IC50: 1.9 μM; α3β4 nAChR, IC50: 1.8 μM; α4β2 nAChR, IC50: 3.7 μM; α4β4 nAChR, IC50: 6.3 μM |
| S0717 | Varenicline (CP 526555) dihydrochloride | Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) 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 | α4β2 nAChR, EC50: 2.3 μM; α3β4 nAChR, EC50: 55 μM; α7 nAChRs, EC50: 18 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 |
| S0518 | NS 1738 | NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor (α7 nAChR), with respect to positive modulation of Xenopus laevis oocyte α7 nAChR with EC50 of 3.4 μM, as well as a comparable efficacy at the rat α7 nAChR with EC50 of 3.9 μM. | Selective | rat α7 nAChR, EC50: 3.9 μM |
| S4505 | Vinblastine sulfate | Vinblastine sulfate 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 |
| S4072 | Decamethonium Bromide | Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent. | Selective | |
| S0552 | BNC210 | BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). | 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 | |
| S3202 | Catharanthine | Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM. | Selective |
