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nicotinic acetylcholine receptors (nAChRs)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	mAChR (2) nAChR (143) 5-HT Receptor (5) Antibiotic (6) Autophagy (1) Bacterial (1) Biochemical Assay Reagents (1) Calcium Channel (4) Cholinesterase (ChE) (7) Dengue Virus (1) Dopamine Transporter (1) Drug Isomer (2) Drug Metabolite (1) Endogenous Metabolite (5) Environmental Pollutants (6) ERK (2) Flavivirus (1) GABA Receptor (3) Histone Methyltransferase (1) HIV (1) HSV (1) iGluR (1) Insecticide (3) Isotope-Labeled Compounds (8) Liposome (4) Mitophagy (1) mTOR (1) Opioid Receptor (1) p38 MAPK (2) Parasite (14) Potassium Channel (1) Reference Standards (16) SARS-CoV (2) Serotonin Transporter (1) Sodium Channel (1) STAT (1) TNF Receptor (2)
By Research Areas:	Cancer (22) Cardiovascular Disease (4) Infection (21) Inflammation/Immunology (23) Metabolic Disease (2) Neurological Disease (110)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	Pegylated Lipids (3)

148

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

Targets Recommended: nAChR mAChR

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-B0282

Acetylcholine chloride 20+ Cited Publications ACh chloride	nAChR Calcium Channel Endogenous Metabolite	Infection Neurological Disease Cancer
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-10019

Varenicline 1 Publications Verification 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 α7β2 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-12560A

PNU-282987 10+ Cited Publications	nAChR 5-HT Receptor	Neurological Disease
PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC₅₀ of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT₃ receptor with an IC₅₀ of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems .

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-10021

Varenicline Tartrate 1 Publications Verification CP 526555-18	nAChR ERK p38 MAPK	Others Neurological Disease 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-B0282S

Acetylcholine-d4 chloride ACh-d4 chloride	nAChR Calcium Channel Endogenous Metabolite	Neurological Disease Cancer
Acetylcholine-d₄ (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-B0118A

Vecuronium bromide ORG NC 45	nAChR	Neurological Disease Cancer
Vecuronium (ORG NC 45) bromide is a non-depolarizing neuromuscular blocking agent that also acts as a nicotinic acetylcholine receptor (nAChR) inhibitor, a muscle relaxant, and can be used for pre-surgical anesthesia .

HY-145298

Dicloromezotiaz	nAChR	Infection
Dicloromezotiaz is a potent insecticide acting on **nicotinic acetylcholine receptors (nAChRs)**. Dicloromezotiaz can be used to control a broad range of lepidoptera .

HY-B0823

Acetamiprid 2 Publications Verification	Environmental Pollutants nAChR	Neurological Disease
Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a **nicotinic acetylcholine receptor (nAChR)** agonist, and is shown to be associated with neuromuscular and reproductive disorders .

HY-B0820

Nitenpyram	nAChR Parasite	Neurological Disease
Nitenpyram is a calss of neonicotinoid and an insect **nicotinic acetylcholine receptor (nAChR) agonist with an IC₅₀** of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals .

HY-P1264F

α-Bungarotoxin, FITC labeled	nAChR	Neurological Disease
FITC-labeled α-Bungarotoxin is FITC-conjugated α-Bungarotoxin (HY-P1264). α-Bungarotoxin acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) .

HY-118504

Sulfoxaflor 1 Publications Verification	Environmental Pollutants nAChR	Neurological Disease
Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive *nAChR1* and *nAChR2* subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .

HY-15430A

Encenicline hydrochloride 5 Publications Verification EVP-6124 hydrochloride	nAChR	Neurological Disease
Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

HY-101347

Chlorisondamine diiodide	nAChR	Neurological Disease
Chlorisondamine (diiodide) is a potent **nicotinic acetylcholine receptor (nAChR)** antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way .

HY-B1532

Anabasine (S)-Anabasine; (+)-Anabasine	Environmental Pollutants nAChR	Neurological Disease
Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC₅₀=0.7 μM) .

HY-10020

Varenicline Hydrochloride CP 526555 hydrochloride	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-N0443

N-Methylcytisine 2 Publications Verification Caulophylline	nAChR	Inflammation/Immunology
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (K_d = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .

HY-B0282S1

Acetylcholine-d9 chloride ACh-d9 chloride	nAChR Calcium Channel Endogenous Metabolite	Neurological Disease Cancer
Acetylcholine-d₉ (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-14824

Sofiniclin ABT 894	nAChR	Neurological Disease
Sofiniclin (ABT 894), an agonist of **nicotinic acetylcholine receptor (nAChR)**, is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD) .

HY-14840

Phenylpiracetam Carphedon	nAChR Dopamine Transporter GABA Receptor iGluR	Neurological Disease
Phenylpiracetam (Carphedon) is a positive allosteric modulator of nicotinic acetylcholine receptors (nAChR) with an IC₅₀ of 5.86 μM. Phenylpiracetam is applicable to studies on scopolamine (Scopolamine) (HY-N0296)-induced amnesia, depression and immune stress .

HY-145296

Triflumezopyrim 2 Publications Verification	Environmental Pollutants nAChR	Infection
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor *(nAChR)* inhibition, which is very highly efficient, rapidly effective, and nearly nontoxic to nontarget arthropods .

HY-19490

VQW-765 AQW-051	nAChR	Neurological Disease
VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pK_D value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety .

HY-101955

(2S,6S)-Hydroxynorketamine hydrochloride (2S,6S)-HNK hydrochloride	mTOR nAChR	Neurological Disease
(2S,6S)-Hydroxynorketamine hydrochloride is a neurorelaxant with potential antidepressant and analgesic effects. (2S,6S)-Hydroxynorketamine hydrochloride can activate the mTOR pathway, increase the phosphorylation level of downstream targets, and antagonize α7-nicotinic acetylcholine receptor (nAChR) to exert neuroactive properties .

HY-172706

DSPE-PEG5000-RVG29	Liposome nAChR	Neurological Disease
DSPE-PEG5000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB .

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-107682

TQS	nAChR	Neurological Disease Inflammation/Immunology
TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain .

HY-B0282R

Acetylcholine chloride (Standard) ACh chloride (Standard)	Reference Standards nAChR Calcium Channel Endogenous Metabolite	Neurological Disease Cancer
Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-10019A

Varenicline dihydrochloride CP 526555 dihydrochloride	nAChR	Neurological Disease Inflammation/Immunology Cancer
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 α7β2 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-P1271

Catestatin Catestatin (cattle)	nAChR	Cardiovascular Disease
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive *nicotinic* antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .

HY-147360

Tribendimidine 2 Publications Verification	nAChR	Infection
Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type **nicotinic acetylcholine receptor (nAChR)** agonist .

HY-121027

Anagyrine (-)-Anagyrine; Monolupine; Rhombinine	mAChR nAChR	Neurological Disease
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of *nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR* .

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-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-W705106

(-)-Coclaurine hydrochloride 1 Publications Verification (-)-(S)-Coclaurine hydrochloride; L-Coclaurine hydrochloride	nAChR	Neurological Disease
(-)-Coclaurine hydrochloride (compound I) is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. (-)-Coclaurine hydrochloride is a **nicotinic acetylcholine receptor (nAChRs)** antagonist .

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-14774S1

(Rac)-Monepantel sulfone-d5	nAChR	Cancer
(Rac)-Monepantel sulfone-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-12149

A-867744	nAChR	Neurological Disease
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC₅₀ of 1.0 μM .

HY-14774R

Monepantel (Standard) AAD1566 (Standard); NUZ-001 (Standard)	Reference Standards nAChR	Cancer
Monepantel (Standard) is the analytical standard of Monepantel. This product is intended for research and analytical applications. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-139582

Simpinicline OC-02	nAChR SARS-CoV	Infection
Simpinicline (OC-02), a highly selective **nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC₅₀** of 0.04 µM .

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-15430

Encenicline EVP-6124	nAChR	Neurological Disease
Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

HY-14774S

(Rac)-Monepantel-d5	nAChR	Cancer
(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-129674

PHA 568487 free base 1 Publications Verification	nAChR	Neurological Disease
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation .

HY-12560

PNU-282987 free base	nAChR 5-HT Receptor	Neurological Disease
PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC₅₀ of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT₃ receptor with an IC₅₀ of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems .

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-P5823

Azemiopsin	nAChR	Neurological Disease
Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC₅₀s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .

HY-145297

Flupyrimin	nAChR Insecticide	Neurological Disease
Flupyrimin is the antagonist for insect nicotinic acetylcholine receptor (nAChR) that exhibits insecticidal effect by targeting insect nervous system .

HY-12560D

PNU-282987 S enantiomer free base	nAChR	Others
PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.

HY-P1271A

Catestatin TFA	nAChR	Cardiovascular Disease
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive *nicotinic* antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .

HY-107676

SIB-1553A	nAChR	Neurological Disease
SIB-1553A is an orally bioavailable **nicotinic acetylcholine receptors (nAChRs)** agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders .

Art. -Nr.	Produktname	Type

HY-172706

DSPE-PEG5000-RVG29	Biochemical Assay Reagents
DSPE-PEG5000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB .

HY-172705

DSPE-PEG2000-RVG29

Biochemical Assay Reagents

DSPE-PEG2000-RVG29 is a PEG conjugate composed of DSPE and rabies virus glycoprotein 29 (RVG29). RVG29 specifically binds to nicotinic acetylcholine receptors (nAChR) at the blood-brain barrier (BBB), crosses the BBB, and mediates receptor-dependent transcytosis. DSPE-PEG2000-RVG29 can be used for brain-targeted drug delivery, surface modification of nanocarriers, as well as gene and nucleic acid delivery. DSPE-PEG2000-RVG29 is applicable to research related to hypoxic-ischemic brain injury, Parkinson's disease, and other conditions .

HY-W127670

Decamethonium iodide

Biochemical Assay Reagents

Decamethonium (iodide) is an organic compound containing ammonium and iodide ions. It is commonly used as a neuromuscular blocking agent in anesthesia to induce muscle relaxation during surgery. Decamethonium Iodide acts by binding to nicotinic acetylcholine receptors (nAChRs) in the neuromuscular junction, causing depolarization block and subsequent skeletal muscle paralysis. In addition, it can also serve as a reference standard for pharmacological studies of nAChRs.

HY-172704

DSPE-PEG1000-RVG29	Biochemical Assay Reagents
DSPE-PEG1000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB .

HY-172705A

DSPE-PEG3400-RVG29

Biochemical Assay Reagents

DSPE-PEG3400-RVG29 is a PEG conjugate composed of DSPE and rabies virus glycoprotein 29 (RVG29). RVG29 specifically binds to nicotinic acetylcholine receptors (nAChR) at the blood-brain barrier (BBB), crosses the BBB, and mediates receptor-dependent transcytosis. DSPE-PEG3400-RVG29 can be used for brain-targeted drug delivery, surface modification of nanocarriers, as well as gene and nucleic acid delivery. DSPE-PEG3400-RVG29 is applicable to research related to hypoxic-ischemic brain injury, Parkinson's disease, and other conditions

Art. -Nr.	Produktname	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-P0102

Dipeptide diaminobutyroyl benzylamide diacetate	nAChR	Neurological Disease Metabolic Disease
Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a *nAChR* antagonist. Dipeptide diaminobutyroyl benzylamide diacetate mimics Waglerin-1 to block neuromuscular junction **nicotinic acetylcholine receptors**, partially inhibits neuronal signal transduction, and relaxes muscles. Dipeptide diaminobutyroyl benzylamide diacetate reduces appearance of facial wrinkles linked to repeated muscle movement.Dipeptide diaminobutyroyl benzylamide diacetate can be used for the research of mild-to-moderate fine and coarse periocular and perioral wrinkles and periorbital ageing .

HY-P1264F

α-Bungarotoxin, FITC labeled	nAChR	Neurological Disease
FITC-labeled α-Bungarotoxin is FITC-conjugated α-Bungarotoxin (HY-P1264). α-Bungarotoxin acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs) .

HY-P1271

Catestatin Catestatin (cattle)	nAChR	Cardiovascular Disease
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive *nicotinic* antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .

HY-P0099

Pentapeptide-3	nAChR	Others
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of **nicotinic acetylcholine receptors (nAChRs)**, it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .

HY-P5823

Azemiopsin	nAChR	Neurological Disease
Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC₅₀s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR .

HY-P1271A

Catestatin TFA	nAChR	Cardiovascular Disease
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive *nicotinic* antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .

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 .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-B0282

Acetylcholine chloride 20+ Cited Publications ACh chloride	Structural Classification Natürliche Produkte Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification Cancer	nAChR Calcium Channel Endogenous Metabolite
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-15310

Ivermectin Maximum Cited Publications 48 Publications Verification MK-933; CD-5024; K-237	Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Antiviral Anti-parasitic Disease Research Disease Research Fields Source Classification Cancer	Environmental Pollutants Antibiotic Mitophagy Bacterial Parasite Autophagy Flavivirus HSV HIV SARS-CoV Dengue Virus
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X₄ and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .

HY-B1178

Cotinine 3 Publications Verification (-)-Cotinine; (S)-Cotinine; NIH-10498	Alkaloids Pyrrole Alkaloids Nicotiana tabacum L. Classification of Application Fields Other Diseases Pyridine Alkaloids Solanaceae Plants Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite nAChR
Cotinine ((-)-Cotinine) is an orally active alkaloid found in tobacco and is the primary metabolite of nicotine. Cotinine is metabolized by CYP2A13 into trans-3'-hydroxycotinine. Cotinine is used as a biomarker to measure exposure to tobacco smoke components. Cotinine has vasodepressor activity. The mixture of cotinine and nicotine (Nicotine) has antiproliferative activity against pterygium. (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, leading to the release of dopamine (Dopamine, HY-B0451). Cotinine ((-)-Cotinine) is used in research related to cardiovascular and inflammatory diseases .

HY-138800

Spinosad 4 Publications Verification	Natürliche Produkte Microorganisms Neurological Disease Classification of Application Fields Disease Research Fields Biological Pesticide Research Source Classification Agricultural Research	nAChR
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor *(nAChRs)* of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .

HY-N3610

Coclaurine 1 Publications Verification	Alkaloids Structural Classification Phenols Polyphenols Plants Lauraceae Isoquinoline Alkaloids Lindera aggregata (Sims) Kosterm. Source Classification	nAChR
Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum with anticancer activity. Coclaurine is a **nicotinic acetylcholine receptor** (nAChRs) antagonist. Coclaurine is a key molecule in S. tetrandra responsible for EFHD2 inhibition. Coclaurine can downregulate EFHD2-related NOX4-ABCC1 signaling and enhanced Cisplatin (HY-17394) sensitivity. Coclaurine suppresses the stemness and metastatic properties of NSCLC cells. Coclaurine disrupts the interaction between the transcription factor FOXG1 and the EFHD2 promoter, leading to a reduction in EFHD2 transcription .

HY-B1532

Anabasine (S)-Anabasine; (+)-Anabasine	Alkaloids Piperidine Alkaloids Structural Classification Nicotiana tabacum L. Pyridine Alkaloids Solanaceae Plants Source Classification	Environmental Pollutants nAChR
Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC₅₀=0.7 μM) .

HY-N0443

N-Methylcytisine 2 Publications Verification Caulophylline	Alkaloids Piperidine Alkaloids Classification of Application Fields Leguminosae Pyridine Alkaloids Sophora flavescens Aiton Plants Inflammation/Immunology Disease Research Fields Source Classification	nAChR
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (K_d = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .

HY-B0282R

Acetylcholine chloride (Standard) ACh chloride (Standard)	Structural Classification Natürliche Produkte Endogenous metabolite Source Classification	Reference Standards nAChR Calcium Channel Endogenous Metabolite
Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-121027

Anagyrine (-)-Anagyrine; Monolupine; Rhombinine	Alkaloids Piperidine Alkaloids Classification of Application Fields Leguminosae Plants Disease Research Fields Lupinus albus Linn. Cancer Source Classification	mAChR nAChR
Anagyrine ((-)-Anagyrine) is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine is a potent and effective desensitizer of *nAChR, and Anagyrine can directly, without metabolism, desensitize nAChR* .

HY-W705106

(-)-Coclaurine hydrochloride 1 Publications Verification (-)-(S)-Coclaurine hydrochloride; L-Coclaurine hydrochloride	Alkaloids Piperidine Alkaloids Cocculus laurifolius DC. Plants Menispermaceae Source Classification	nAChR
(-)-Coclaurine hydrochloride (compound I) is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. (-)-Coclaurine hydrochloride is a **nicotinic acetylcholine receptor (nAChRs)** antagonist .

HY-N16475

Spinosyn L	Structural Classification Microorganisms Antibiotics Source Classification	nAChR
Spinosyn L is a selective nicotinic acetylcholine receptors (nAChR) agonist. Spinosyn L causes sustained neural excitation and paralysis in insects. Spinosyn L is promising for research of pesticides for controlling Lepidoptera, Diptera, and other agricultural pests .

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 .

HY-N16476

Spinosyn J	Structural Classification Natürliche Produkte Microorganisms Source Classification	GABA Receptor nAChR
Spinosyn J is a non-competitive insect nicotinic acetylcholine receptor (nAChR) and γ-aminobutyric acid (GABA) receptor modulator with insecticidal activity. Spinosyn J is promising for research of agricultural pests .

HY-N0443R

N-Methylcytisine (Standard) Caulophylline (Standard)	Alkaloids Piperidine Alkaloids Structural Classification Leguminosae Pyridine Alkaloids Sophora flavescens Aiton Plants Source Classification	Reference Standards nAChR
N-Methylcytisine (Standard) is the analytical standard of N-Methylcytisine. This product is intended for research and analytical applications. N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .

HY-121027A

Anagyrine hydrochloride (-)-Anagyrine hydrochloride; Monolupine hydrochloride; Rhombinine hydrochloride	Alkaloids Piperidine Alkaloids Leguminosae Plants Sophora flavescens Aiton Source Classification	mAChR nAChR
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC₅₀ values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of *nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR* .

HY-B1532R

Anabasine (Standard) (S)-Anabasine (Standard); (+)-Anabasine (Standard)	Alkaloids Piperidine Alkaloids Structural Classification Nicotiana tabacum L. Pyridine Alkaloids Solanaceae Plants Source Classification	Reference Standards nAChR
Anabasine (Standard) is the analytical standard of Anabasine. This product is intended for research and analytical applications. Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC₅₀=0.7 μM) .

HY-126638

Marcfortine A NSC 324645	Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Source Classification	Parasite
Marcfortine A is an indole alkaloid originally isolated from P. roqueforti. It has nematocidal activity against the parasitic nematode H. contortus (LD99=0.06 μg/mL) and inhibits motility of adult worms (EC₅₀=2 μM). Marcfortine A eliminates H. contortus, T. colubriformis, and O. ostertagi from experimentally infected jirds (ED95s=0.33, 0.11, and 2.5 mg/animal, respectively). It dose-dependently inhibits nicotine-induced calcium mobilization in SH-SY5Y and TE-671 cells expressing α3 subunit-containing human nicotinic acetylcholine receptors (nAChRs) and muscle-type nAChRs, respectively.

Art. -Nr.	Produktname	Chemical Structure

HY-B0282S

Acetylcholine-d4 chloride

Acetylcholine-d₄ (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-B0282S1

Acetylcholine-d9 chloride

Acetylcholine-d₉ (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .

HY-14774S1

(Rac)-Monepantel sulfone-d5
(Rac)-Monepantel sulfone-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-14774S

(Rac)-Monepantel-d5
(Rac)-Monepantel-d₅ is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

HY-106901AS

Asoxime-d4 dichloride

1 Publications Verification

Asoxime-d₄ dichloride (HI-6-d₄) is the deuterium labeled Asoxime dichloride. Asoxime dichloride is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system.

HY-10019S2

Varenicline-13C15N

Varenicline- ¹³C ¹⁵N (CP 526555- ¹³C ¹⁵N) is ¹³C and ¹⁵N labeled Varenicline. 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 α7β2 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-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 α7β2 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 . 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 .

HY-118504S

Sulfoxaflor-d3

Sulfoxaflor-d₃ is the deuterium labeled Sulfoxaflor (HY-118504). Sulfoxaflor is an orally active full agonist of insect nicotinic acetylcholine receptors (nAChRs), targeting the α-bungarotoxin-insensitive nAChR1 and nAChR2 subtypes. Sulfoxaflor binding to nACh is not inhibited by d-Tubocurarine (HY-125901), but is partially inhibited by Mecamylamine (HY-B1395A). Sulfoxaflor induces inward currents by activating nAChRs, leading to insect neurotoxicity. Sulfoxaflor can be used in the research of agricultural pest control, pesticide toxicology, insect neural receptor pharmacology, etc .

HY-B0820S1

Nitenpyram-d3-1
Nitenpyram-d₃-1 is the deuterium labeled Nitenpyram (HY-B0820). Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC₅₀ of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals .

Art. -Nr.	Produktname		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 .

Art. -Nr.	Produktname		Classification

HY-172706

DSPE-PEG5000-RVG29		Pegylated Lipids
DSPE-PEG5000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB .

HY-172705

DSPE-PEG2000-RVG29		Pegylated Lipids
DSPE-PEG2000-RVG29 is a PEG conjugate composed of DSPE and rabies virus glycoprotein 29 (RVG29). RVG29 specifically binds to nicotinic acetylcholine receptors (nAChR) at the blood-brain barrier (BBB), crosses the BBB, and mediates receptor-dependent transcytosis. DSPE-PEG2000-RVG29 can be used for brain-targeted drug delivery, surface modification of nanocarriers, as well as gene and nucleic acid delivery. DSPE-PEG2000-RVG29 is applicable to research related to hypoxic-ischemic brain injury, Parkinson's disease, and other conditions .

HY-172704

DSPE-PEG1000-RVG29		Pegylated Lipids
DSPE-PEG1000-RVG29 is a PEG compound which composed of DSPE and a Rabies virus glycoprotein 29 (RVG29). RVG29 can bind specifically to the nicotinic acetylcholine receptor (nAChR) at the blood-brain barrier (BBB) and cross over the BBB .

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