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α3β4 nicotinic acetylcholine receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	nAChR (18) Interleukin Related (1) Isotope-Labeled Compounds (2) NF-κB (1) Reference Standards (1) STAT (1) TNF Receptor (1)
By Research Areas:	Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (17)
Click Chemistry:	Alkynes (1)

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Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: nAChR mAChR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P1264

α-Bungarotoxin 5+ Cited Publications	nAChR	Neurological Disease
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC₅₀ of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .

HY-B0379A

Adiphenine hydrochloride 3 Publications Verification	nAChR	Neurological Disease
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC₅₀s of 1.9, 1.8, 3.7, and 6.3 μM for α1, *α3β4, α4β2, and α4β4*, respectively. Adiphenine hydrochloride has anticonvulsant effects .

HY-135783

AT 1001 1 Publications Verification	nAChR	Neurological Disease Metabolic Disease Inflammation/Immunology
AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a K_i value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .

HY-110121A

NS3861 1 Publications Verification	nAChR	Neurological Disease
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .

HY-10063

Ispronicline TC-1734; ACD3480	nAChR	Neurological Disease
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (K_i=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .

HY-136207

TC-2559 difumarate	nAChR	Neurological Disease
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC₅₀=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. Antinociceptive effect .

HY-110121

NS3861 fumarate 1 Publications Verification	nAChR	Neurological Disease
NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K_i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .

HY-171746

F4-Trp 4,5,6,7-Tetrafluoro-L-tryptophan	nAChR	Neurological Disease
F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .

HY-114791

Lobelanidine	nAChR	Neurological Disease
Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC₅₀ of 2.8 and 8.2 μM .

HY-169870

Dexmecamylamine (+)-Mecamylamine; TC-5214	nAChR	Neurological Disease
Dexmecamylamine ((+)-Mecamylamine) is the antagonist for **nicotinic acetylcholine receptor (nAChR*), that antagonises the α3β4/α4β2/α7/α1β1γδ* receptor with IC₅₀ of micromolare levels. Dexmecamylamine exhibits anxiolytic and antidepressant-like activities .

HY-171807

TC-2559 free base	nAChR STAT	Neurological Disease Inflammation/Immunology
TC-2559 free base is a *α4β2 nicotinic* acetylcholine receptor (nAChR) agonists with an EC₅₀** of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .

HY-W680961

Hydrohydrastinine	nAChR	Neurological Disease
Hydrohydrastinine is a selective α4β2 **nicotinic acetylcholine receptor antagonist with an IC₅₀ of 2.6 μM and a K_i of 17 μM. Hydrohydrastinine exhibits weak activity at α4β4 and α3β4** nicotinic acetylcholine receptors. Hydrohydrastinine can be used for the research of depression .

HY-121141

Adiphenine	nAChR	Neurological Disease
Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC₅₀s of 1.9, 1.8, 3.7, and 6.3 μM for α1, *α3β4, α4β2, and α4β4*, respectively. Adiphenine has anticonvulsant effects .

HY-10019S

Varenicline-d4 CP 526555-d₄	Isotope-Labeled Compounds nAChR	Neurological Disease
Varenicline-d₄ is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .

HY-14318

Altinicline SIB-1508Y free base	nAChR	Neurological Disease
Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against *α3β4* nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .

HY-10019AS1

Varenicline-d4 hydrochloride	Isotope-Labeled Compounds nAChR	Inflammation/Immunology
Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for *α4β2 nicotinic* acetylcholine receptor (nAChR) with an EC₅₀** value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .

HY-B0379AR

Adiphenine hydrochloride (Standard)	Reference Standards nAChR	Neurological Disease
Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .

HY-182707

JWX-A0108	nAChR Interleukin Related TNF Receptor NF-κB	Neurological Disease
JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC₅₀ of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .

Cat. No.	Product Name	Target	Research Area

HY-P1264

α-Bungarotoxin 5+ Cited Publications	nAChR	Neurological Disease
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC₅₀ of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .

HY-171746

F4-Trp 4,5,6,7-Tetrafluoro-L-tryptophan	nAChR	Neurological Disease
F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-114791

Lobelanidine	Structural Classification Alkaloids Lobelia tupa L. Other Alkaloids Campanulaceae Plants Source Classification	nAChR
Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC₅₀ of 2.8 and 8.2 μM .

Cat. No.	Product Name	Chemical Structure

HY-10019S

Varenicline-d4
Varenicline-d₄ is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .

Varenicline-d4

Varenicline-d₄ is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment .

HY-10019AS1

Varenicline-d4 hydrochloride
Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for *α4β2 nicotinic* acetylcholine receptor (nAChR) with an EC₅₀** value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .

Varenicline-d4 hydrochloride

Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .

Cat. No.	Product Name		Classification

HY-14318

Altinicline SIB-1508Y free base		Alkynes
Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against *α3β4* nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .

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