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Results for "

alpha4beta2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Amyloid-β (2) Bacterial (2) Cholinesterase (ChE) (4) Endogenous Metabolite (1) ERK (1) Isotope-Labeled Compounds (5) nAChR (60) NF-κB (2) p38 MAPK (1) Potassium Channel (1)
By Research Areas:	Cancer (3) Infection (1) Inflammation/Immunology (9) Metabolic Disease (1) Neurological Disease (58)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-115764

nAChR agonist 2

nAChR Neurological Disease

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

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

HY-N1064

Xanthoplanine
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-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-107673

RJR-2429 dihydrochloride

nAChR Neurological Disease

RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist .

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

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-B0942

Benzethonium chloride	nAChR Bacterial	Neurological Disease
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.

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-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-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-N2326

(±)-Anatoxin A fumarate
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits K_i values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ ³H]-dopamine release from rat striatal synaptosomes (EC₅₀=134 nM) .

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-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-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-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-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-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-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-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-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-P5147

α-Conotoxin GID	nAChR	Neurological Disease
α-Conotoxin GID is a paralytic peptide neurotoxin and a selective antagonist of nAChR, with IC₅₀s of 5 nM (α7), 3 nM (α3β2)， 150 nM (α4β2), respectively. α-Conotoxin GID is small disulfide-rich peptide, with potential to inhibit chronic pain. α-Conotoxin GID contains a C-terminal carboxylate, thus substitution with a C-terminal carboxamide results in loss of α4β2 nAChR. α-Conotoxin GID can be isolated from the Conus species .

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-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-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-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-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 .

HY-10019S1

Varenicline-15N,13C,d2 CP 526555-15N,13C,d2	nAChR Isotope-Labeled Compounds	Neurological Disease Inflammation/Immunology Cancer
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-N10132

Microgrewiapine A	nAChR	Infection Neurological Disease
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-107670

Dihydro-β-erythroidine hydrobromide 1 Publications Verification DHβE hydrobromide	nAChR	Neurological Disease
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-B0379A

Adiphenine hydrochloride	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-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-110121

NS3861 fumarate	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-110121A

NS3861	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-105670A

PHA-543613 hydrochloride	nAChR	Neurological Disease
PHA-543613 hydrochloride is an oral or active α7 nAChR agonist with brain permeability, For *α3β4, α1β1γδ, α4β2* and 5-HT3 receptors selective. PHA-543613 hydrochloride affects sensory gating and memory in an in vivo model of schizophrenia .

HY-P5189A

*His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA*	Endogenous Metabolite Cholinesterase (ChE)	Others
His-D-beta-Nal-Ala-Trp-D-Phe-Lys-NH2 TFA, is a growth hormone releasing peptide, as well as a metabolite of GHRP-1. GHRP-1, or Ala-His-D-beta Nal-Ala-Trp-D-Phe-Lys-NH2, has the effect of promoting the release of growth hormone (GH). GHRP-1 increases GH release and increases [Ca2+]i levels in static monolayer cells of rat pituitary gland, but does not affect cAMP levels .

HY-12152

PNU-120596 NSC 216666	nAChR	Neurological Disease Inflammation/Immunology
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC₅₀ of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0175

Cytisinicline 1 Publications Verification Cytisine; Sophorine; Baptitoxine	Alkaloids 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 12 Publications Verification Galantamine hydrobromide	Structural Classification Alkaloids Other Alkaloids Source classification 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-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-A0009R

Galanthamine hydrobromide (Standard) Galantamine hydrobromide (Standard)	Structural Classification 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) .

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-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 .

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-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].

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