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Search Results for " α3β4 nachr "

17

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9542	NS3861	AChR	Neuroscience
	NS3861 是烟碱型乙酰胆碱受体的激动剂，对α3β4 nAChR 具有高亲和力。能够分别与α3β4 (Ki:0.62 nM)、α3β2 (Ki:25 nM)、α4β4 (Ki:7.8 nM)、α4β2 (Ki:55 nM) 结合。
T2422	PNU-282987	AChR	Neuroscience
	PNU 282987 是一种选择性 α7 烟碱型乙酰胆碱受体 (α7 nAChR) 激动剂，Ki 为 26 nM。
TP2063	α-Conotoxin MII	AChR	Neuroscience
	α-Conotoxin MII 是可从僧袍芋螺中分离得到的一种天然产物，有效抑制 nAChR 受体的α3β2亚基，IC50值为 0.5 nM。它还可有效抑制 β3-containing 神经尼古丁受体。
T9450	NS3861 fumarate
	NS3861 fumarate 是烟碱型乙酰胆碱受体 (nAChRs) 的激动剂。NS3861 fumarate 是α3β4 nAChR 的部分激动剂。与α3β4、α3β2、α4β4、α4β2 的结合Ki 值分别为 0.62、25、7.8、55 nM。
T23388	SR 16584	Others	Others
	α3β4 nAChR antagonist
T80219	α-Conotoxin TxID
	α-Conotoxin TxID 为一种有效的α3β4nAChR拮抗剂，IC50为12.5 nM。相对于密切相关的α6/α3β4nAChR，其抑制活性较弱（IC50=94 nM）。此化合物在开发新型戒烟药物方面具有潜力。
T70987	AT-1001
	AT-1001 is an α3β4 nAChR partial agonist. AT-1001 attenuates stress-induced reinstatement of nicotine seeking in a rat model of relapse and induces minimal withdrawal in dependent rats. AT-1001 also potently and reversibly blocks epibatidine-induced inward currents in HEK cells transfected with α3β4 nAChR. Importantly, AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding. When tested in a nucleus accumbens (NAcs) synaptosomal prepar...
T39833	(Rac)-CP-601927 hydrochloride
	(Rac)-CP-601927 hydrochloride is the racemate form of CP-601927, which is a nicotinic acetylcholine receptor (nAChR) agonist. It exhibits Ki values of 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively.
T40119	TC-2559 difumarate
	TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist with an EC 50 of 0.18 μM. It exhibits selectivity for α4β2 receptors over α2β4, α4β4, and α3β4 receptors, with EC 50 s ranging from 10 to 30 μM. TC-2559 difumarate also demonstrates antinociceptive effects.
T75877	α-Conotoxin AuIB TFA
	α-Conotoxin AuIB TFA，一种选择性α3β4烟碱乙酰胆碱受体(nAChR)的有效拮抗剂，能阻断在非洲爪蟾卵母细胞中表达的α3β4 nAChRs，其IC50值为0.75 μM。
T0072	Adiphenine hydrochloride Adiphenine HCl,盐酸阿地芬宁,Spasnil,Patrovina,Sentiv	AChR	Neuroscience
	Adiphenine hydrochloride (Patrovina) 是一种烟碱样受体抑制剂，可用作解痉药，对α1、α3β4、α4β2和α4β4的IC50值分别为 1.9、1.8、3.7 和 6.3 µM。
T73894	α-Conotoxin Vc1.1 TFA
	α-Conotoxin Vc1.1 TFA 是一种分离自Conus victoriae 的二硫键肽，也是一种选择性的nAChR 拮抗剂。α-Conotoxin Vc1.1 TFA 抑制α3α5β2，α3β2和α3β4的IC50分别为 7.2 μM，7.3 μM 和 4.2 μM，对其他nAChR 亚型的抑制作用较小，可用于神经性疼痛的研究。
T80475	α-Conotoxin AuIA
	α-Conotoxin AuIA为高效的α3β4 nAChR选择性抑制剂，源自Conus aulicus的分离提取。
T4246L	Varenicline
	Varenicline (CP 526555) 是一种有效的α4β2 nAChR 烟碱乙酰胆碱受体的部分激动剂，EC50值为2.3 μM。Varenicline 是 α3β4 nAChR 和 α7 nAChR 乙酰胆碱受体的完全激动剂，EC50值分别为 55 μM 和 18 μM。Varenicline 是一种基于胞嘧啶结构的烟碱配体，具有戒烟治疗的潜力。
T80166	α-Conotoxin BuIA
	α-Conotoxin BuIA 是一种麻痹性肽类神经毒素，同时也是竞争性nAChR拮抗剂。它对nAChR亚型表现出不同的IC50值：0.258 nM（α6/α3β2）、1.54 nM（α6/α3β4）、5.72 nM（α3β2）。该化合物可用于鉴别包含β2与β4亚单位的nAChR亚型。此外，α-Conotoxin BuIA 对αxβ2nAChR的区分能力按照α6>α3>α2>α4的顺序减弱。
T37202	CC4 CC4
	High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 ...
T35432	α-Conotoxin ImI (trifluoroacetate salt)
	α-Conotoxin ImI is a conotoxin that has been found inC. imperialisand has receptor antagonist and anticancer activities.1It is a peptide antagonist of homomeric α7 nicotinic acetylcholine receptors (nAChRs; IC50= 220 nM). α-Conotoxin ImI is selective for α7 nAChRs over α2β2, α3β2, α4β2, α2β4, α3β4, α4β4, and α1β1γδ subunit-containing nAChRs at 5 μM but does inhibit homomeric α9 nAChRs (IC50= 1,800 nM). Administration of paclitaxel in micelles containing α-conotoxin ImI decreases tumor growth in ...

化合物

Cat.No: T9542

Target: AChR

Cat.No: T2422

Target: AChR

α-Conotoxin MII

Cat.No: TP2063

Target: AChR

NS3861 fumarate

Cat.No: T9450

Cat.No: T23388

Target: Others

α-Conotoxin TxID

Cat.No: T80219

Cat.No: T70987

(Rac)-CP-601927 hydrochloride

Cat.No: T39833

TC-2559 difumarate

Cat.No: T40119

α-Conotoxin AuIB TFA

Cat.No: T75877

Adiphenine hydrochloride

Cat.No: T0072

Synonym: Adiphenine HCl,盐酸阿地芬宁,Spasnil,Patrovina,Sentiv

Target: AChR

α-Conotoxin Vc1.1 TFA

Cat.No: T73894

α-Conotoxin AuIA

Cat.No: T80475

Cat.No: T4246L

α-Conotoxin BuIA

Cat.No: T80166

Cat.No: T37202

Synonym: CC4

α-Conotoxin ImI (trifluoroacetate salt)

Cat.No: T35432

Cat. No.	Product Name	Target	Signaling Pathways
T37609	(rel)-Asperparaline A
	Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces...

天然产物

(rel)-Asperparaline A

Cat.No: T37609

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