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Results for "

α4β2 nAChRs

" in MedChemExpress (MCE) Product Catalog:

By Targets:	nAChR (50) 5-HT Receptor (1) Amyloid-β (2) Cholinesterase (ChE) (3) ERK (1) Isotope-Labeled Compounds (4) NF-κB (2) p38 MAPK (1) Potassium Channel (1)
By Research Areas:	Cancer (3) Infection (1) Inflammation/Immunology (9) Metabolic Disease (1) Neurological Disease (48)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: nAChR

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-137231B

(S)-UFR2709 hydrochloride	nAChR	Neurological Disease
(S)-UFR2709 (hydrochloride) is a competitive *nAChR* antagonist and displays higher affinity for α₄β₂ nAChRs than for α₇ nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .

HY-137231A

(S)-UFR2709	nAChR	Neurological Disease
(S)-UFR2709 is a competitive *nAChR* antagonist and displays higher affinity for α₄β₂ nAChRs than for α₇ nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction .

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-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-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-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-131001

DPNB-ABT594	nAChR	Neurological Disease
DPNB-ABT594 is a nitrobenzyl-caged ABT594 (HY-14316A) and activates *nAChRs* containing the *α4β2* subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca ²⁺ signalling in the MHb .

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-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 .

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-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-105670

PHA-543613	nAChR	Neurological Disease
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .

HY-105670B

PHA-543613 dihydrochloride	nAChR	Neurological Disease
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors . PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research .

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

HY-10019AS1

Varenicline-d4 hydrochloride	Isotope-Labeled Compounds	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-A0009

Galanthamine hydrobromide Maximum Cited Publications 12 Publications Verification Galantamine hydrobromide	Cholinesterase (ChE) nAChR	Neurological Disease
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-14565

Pozanicline ABT-089	nAChR	Neurological Disease
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (K_i=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (K_i, rat) for Pozanicline to [ ³H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .

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-135483A

AR-R17779 hydrochloride	nAChR	Neurological Disease
AR-R17779 hydrochloride is a potent and selective full agonist of *nAChR, with K_is of 92 and 16000 nM for α7 and α4β2* subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .

HY-A0009S

Galanthamine-d3 hydrobromide Galantamine-d₃ hydrobromide	Isotope-Labeled Compounds Cholinesterase (ChE) nAChR	Neurological Disease
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].

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-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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