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
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 是有效的neuronal nicotinic acetylcholine receptors (nAChRs)(神经元烟碱型乙酰胆碱受体)抑制剂,抑制α4β2 nAChRsα7 nAChRsIC50分别为49 nM 和 122 nM。

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是一种有效的α7 nAChR变构调节剂,EC50为216 nM。

Selective α7 nAChR, EC50: 216 nM
S2082 Adiphenine HCl

Adiphenine HCl 是一种烟碱受体抑制剂,IC50为15 µM,用作解痉药。

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

Varenicline dihydrochloride is a partial agonist of α4β2 nicotinic acetylcholine receptor. Varenicline dihydrochloride is a prescription medication used for smoking cessation.

Selective α3β4 nAChR, EC50: 55 μM; α7 nAChRs, EC50: 18 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抑制微管形成nAChR活性,在无细胞实验的测定中,IC50为8.9 μM。

Selective nAChR, IC50: 8.9 μM
S4023 Procaine HCl

Procaine HCl是一种钠离子通道的,NMDA受体以及乙酰胆碱受体抑制剂, IC50分别为60 μM, 0.296 mM何45.5 μM,也是一种,5-HT3抑制剂,KD为1.7 μM。

Selective nAChR, IC50: 45.5 μM
S0552 BNC210

BNC210 is a negative allosteric modulator of α7 nAChR. BNC210 has potent activity in animal models of anxiety and depression.

Selective
S4121 Succinylcholine Chloride Dihydrate

Succinylcholine Chloride Dihydrate是一种烟碱AChR激动剂,同时也是一种去极化神经肌肉阻断剂。

Selective
S4072 Decamethonium Bromide

Decamethonium Bromide是一种烟碱AChR部分激动剂和神经肌肉阻断剂。

Selective
S2287 Cytisine

Cytisine是一种烟碱型乙酰胆碱受体激动剂。

Selective
S3202 Catharanthine

Catharanthine是一种从长春花中分离出来的生物碱,可以抑制烟碱受体介导的隔膜收缩,IC50为59.6µM。

Selective