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Results for "

α4β2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Amyloid-β (2) Apoptosis (1) Bacterial (2) Biochemical Assay Reagents (1) Calcium Channel (2) Caspase (1) Cholinesterase (ChE) (3) Dopamine Transporter (1) ERK (2) GABA Receptor (2) Isotope-Labeled Compounds (6) nAChR (76) NF-κB (2) p38 MAPK (2) Potassium Channel (1) Sodium Channel (2)
By Research Areas:	Cancer (6) Infection (2) Inflammation/Immunology (11) Metabolic Disease (4) Neurological Disease (75)

Inhibitors & Agonists

Biochemical Assay Reagents

Natural
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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-110131

A 85380 hydrochloride	nAChR	Neurological Disease
A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .

HY-138879A

(Rac)-CP-601927 hydrochloride	nAChR	Neurological Disease
(Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively .

HY-12766

Bupropion morpholinol	Dopamine Transporter nAChR	Neurological Disease
Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .

HY-107680

3-Pyr-Cytisine 3-Pyr-Cyt	nAChR	Neurological Disease
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant .

HY-107686

5-Iodo-A-85380 dihydrochloride 5-I A-85380 dihydrochloride	nAChR	Neurological Disease
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with K_ds of 12 and 14 pM,respectively .

HY-138953

Epiboxidine	nAChR	Neurological Disease
Epiboxidine is a potent and selective neural nAChR agonist with K_is of 0.46 nM and 1.2 nM for rat and *human α4β2* nAChRs**, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .

HY-138953A

Epiboxidine hydrochloride	nAChR	Neurological Disease
Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with K_is of 0.46 nM and 1.2 nM for rat and *human α4β2* nAChRs**, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .

HY-116149

A-424274	Others	Others
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.

HY-126047B

(R)-(+)-Anatabine	NF-κB Amyloid-β nAChR	Neurological Disease Inflammation/Immunology
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .

HY-107673

RJR-2429 dihydrochloride	nAChR	Neurological Disease
RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist .

HY-115764

nAChR agonist 2	nAChR	Neurological Disease
nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (K_d=26 nM) .

HY-110160

Pozanicline dihydrochloride ABT-089 dihydrochloride	nAChR	Neurological Disease
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K_i of 16.7 nM for binding to [ ³H]cytisine sites . Pozanicline is an *α4β2*-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K_i of 17 nM while binding to α7 nAChR is insignificant .

HY-103066

Br-PBTC	nAChR	Neurological Disease
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)₂α4 and (α4β2)₂β2 EC₅₀ ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .

HY-107675

Desformylflustrabromine hydrochloride Deformylflustrabromine hydrochloride; dFBr hydrochloride	nAChR	Neurological Disease
Desformylflustrabromine hydrochloride is a selective agonist of *α₄β₂* neuronal nicotinic acetylcholine receptor (nAChR) with a pEC₅₀ of 6.48.

HY-108069

Iptakalim hydrochloride	Potassium Channel nAChR	Neurological Disease
Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (K_ATP) opener, as well as an α₄β₂-containing nicotinic acetylcholine receptor (nAChR) antagonist .

HY-14564A

GTS-21 dihydrochloride 5+ Cited Publications DMXB-A; DMBX-anabaseine	nAChR 5-HT Receptor	Inflammation/Immunology
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a *α4β2* (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist .

HY-14316A

Tebanicline dihydrochloride Ebanicline dihydrochloride; ABT-594 dihydrochloride	nAChR	Neurological Disease
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a K_i of 37 pM .

HY-14316B

Tebanicline hydrochloride Ebanicline hydrochloride; ABT-594 hydrochloride	nAChR	Neurological Disease
Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a K_i of 37 pM .

HY-139581

Ropanicant SUVN-911 free base	nAChR	Neurological Disease
Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active *neuronal nicotinic acetylcholine α4β2* receptor** antagonist for the research of depression .

HY-B0942S

Benzethonium-d7 chloride	Isotope-Labeled Compounds nAChR	Neurological Disease
Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

HY-107671

DMAB-anabaseine dihydrochloride	nAChR	Neurological Disease
DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .

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-19918A

Anatabine dicitrate	NF-κB Amyloid-β nAChR	Neurological Disease Inflammation/Immunology
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .

HY-110241

Dianicline dihydrochloride	nAChR	Neurological Disease
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .

HY-W979493

TC-2216	Others	Others
TC-2216 is a compound with antidepressant and anxiolytic activity that has shown activity in multiple animal models and may exert its effects by acting on α4β2 neuronal nicotinic receptors.

HY-B0942

Benzethonium chloride	nAChR Bacterial Apoptosis Caspase	Infection Neurological Disease Cancer
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and *α4β2* neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .

HY-10019

Varenicline CP 526555	nAChR	Neurological Disease Inflammation/Immunology Cancer
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10020

Varenicline Hydrochloride CP 526555 hydrochloride	nAChR	Neurological Disease Inflammation/Immunology
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10021

Varenicline Tartrate CP 526555-18	nAChR ERK p38 MAPK	Others Neurological Disease
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-107684

3-Bromocytisine 3-Br-cytisine	nAChR	Neurological Disease
3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC₅₀s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC₅₀s are 8 and 50 nM, respectively .

HY-10019A

Varenicline dihydrochloride CP 526555 dihydrochloride	nAChR	Neurological Disease Inflammation/Immunology
Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-14564

GTS-21	nAChR 5-HT Receptor	Inflammation/Immunology
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a *α4β2* (K_i=20 nM for humanα4β2) and 5-HT3A receptor (IC₅₀=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .

HY-136146

SUVN-911	nAChR	Neurological Disease
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K_i of 1.5 nM. SUVN-911 has antidepressant activity .

HY-136947

RJR-2429	nAChR	Neurological Disease
RJR-2429 is a nAChR agonist (EC₅₀: 59 nM). RJR-2429 binds with high affinity to α4β2 receptor subtype (K_i = 1 nM). RJR-2429 induces ileum contraction .

HY-14316

Tebanicline Ebanicline; ABT-594	nAChR	Neurological Disease
Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.

HY-B0942R

Benzethonium chloride (Standard)	nAChR Bacterial	Neurological Disease
Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.

HY-14316C

Tebanicline tosylate Ebanicline tosylate; ABT-594 tosylate	nAChR	Neurological Disease
Tebanicline tosylate, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline tosylate exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.

HY-13225D

Rivanicline fumarate RJR-2403 fumarate; (E)-Metanicotine fumarate	nAChR	Neurological Disease
Rivanicline fumarate is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,K_i is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .

HY-120946

VMY-2-95	nAChR	Neurological Disease
VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .

HY-40421

(R)-3-Fluoropyrrolidine hydrochloride	Biochemical Assay Reagents	Others
(R)-3-Fluoropyrrolidine hydrochloride is a derivative of fluorinated pyrrolidines. The amide series of fluorinated pyrrolidines are inhibitors of dipeptidyl peptidase DP-IV. Novel α4β2 receptor ligands characterized by a 3-Fluoropyrrolidine core .

HY-115766

Anabaseine	nAChR	Neurological Disease
Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .

HY-107688A

UB-165 fumarate	nAChR	Neurological Disease
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for [ ³H]-nicotine binding in rat brain .

HY-107688

UB-165	nAChR	Neurological Disease
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for [ ³H]-nicotine binding in rat brain .

HY-10021R

Varenicline Tartrate (Standard)	nAChR ERK p38 MAPK	Others Neurological Disease
Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-13225A

Rivanicline RJR-2403; (E)-Metanicotine	nAChR	Neurological Disease
Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,K_i is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	nAChR	Metabolic Disease Cancer
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-13225

Rivanicline oxalate RJR-2403 oxalate; (E)-Metanicotine oxalate	nAChR	Neurological Disease
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (K_i=26 nM); > 1,000 fold selectivity than α7 receptors(K_i= 3.6 μM).

HY-13225B

Rivanicline hemioxalate 1 Publications Verification RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate	nAChR	Neurological Disease
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (K_i=26 nM); > 1,000 fold selectivity than α7 receptors(K_i= 3.6 μM).

HY-138879

CP-601927	nAChR	Neurological Disease
CP-601927 is a selective *α4β2* nicotinic acetylcholine receptor (nAChR) partial agonist (K_i=1.2 nM; EC₅₀=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .

Cat. No.	Product Name	Type

HY-40421

(R)-3-Fluoropyrrolidine hydrochloride	Biochemical Assay Reagents
(R)-3-Fluoropyrrolidine hydrochloride is a derivative of fluorinated pyrrolidines. The amide series of fluorinated pyrrolidines are inhibitors of dipeptidyl peptidase DP-IV. Novel α4β2 receptor ligands characterized by a 3-Fluoropyrrolidine core .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	Alkaloids Structural Classification Classification of Application Fields Leguminosae Source classification Pyridine Alkaloids Metabolic Disease Plants Thermopsis lanceolala R.Br. Disease Research Fields	nAChR
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-107670

Dihydro-β-erythroidine hydrobromide 1 Publications Verification DHβE hydrobromide	Alkaloids Piperidine Alkaloids Leguminosae Source classification Plants Erythrina	nAChR
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC₅₀s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities .

HY-A0009

Galanthamine hydrobromide Maximum Cited Publications 14 Publications Verification Galantamine hydrobromide	Structural Classification Alkaloids Other Alkaloids Plants Amaryllidaceae	Cholinesterase (ChE) nAChR
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-B1671

(+)-Kavain	Structural Classification Source classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na ⁺ and Ca ²⁺ channels . (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

HY-N10132

Microgrewiapine A	Malvaceae Structural Classification Alkaloids Microcos paniculata L. Other Alkaloids Source classification Plants	nAChR
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC₅₀ of 6.8 μM .

HY-N0175R

Cytisinicline (Standard)	Alkaloids Structural Classification Leguminosae Source classification Pyridine Alkaloids Plants Thermopsis lanceolala R.Br.	nAChR
Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .

HY-A0009R

Galanthamine hydrobromide (Standard) Galantamine hydrobromide (Standard)	Structural Classification Alkaloids Other Alkaloids Source classification Plants Amaryllidaceae	nAChR Cholinesterase (ChE)
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-N1064

Xanthoplanine	Alkaloids Structural Classification Monophenols other families Source classification Phenols Plants Isoquinoline Alkaloids	nAChR
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2) .

HY-B1671R

(+)-Kavain (Standard)	Structural Classification Source classification Other Phenylpropanoids Piper methysticum G.Forst. Piperaceae Phenylpropanoids Plants	GABA Receptor Sodium Channel Calcium Channel
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .

Cat. No.	Product Name	Chemical Structure

HY-B0942S

Benzethonium-d7 chloride
Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

HY-10019S1

Varenicline-15N,13C,d2

Varenicline- ¹⁵N, ¹³C,d₂ is ¹⁵N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

HY-10020S

Varenicline-15N3 hydrochloride

Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the ¹⁵N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .

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[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].

HY-A0009S

Galanthamine-d3 hydrobromide

Galanthamine-d₃ (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].

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 .

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