nAChR Antagonist

nAChR Antagonists (77):

Cat. No.	Product Name	Effect	Purity

HY-N2332A

Methyllycaconitine citrate	Antagonist	99.58%
Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .

HY-180559

nAChR antagonist 2	Antagonist
nAChR antagonist 2 is a selective nAChR antagonist. nAChR antagonist 2 inhibits nAChR subtype including hα9α10, hα9, and hα7 with IC₅₀ values of 16.0 nM, 26.2 nM, and 336.3 nM, respectively, in Xenopus oocytes. nAChR antagonist 2 suppresses ATP-induced IL-1β release at nanomolar concentrations. nAChR antagonist 2 can be used for nonopioid analgesics and immunomodulators research.

HY-B1395

Mecamylamine hydrochloride	Antagonist	98.0%
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.

HY-P1264F

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

HY-P1050A

COG 133 TFA	Antagonist	99.89%
COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC₅₀ of 445 nM.

HY-P1264

α-Bungarotoxin	Antagonist	99.11%
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-13596

Cisatracurium besylate	Antagonist	98.0%
Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.

HY-B0567

Dequalinium Chloride	Antagonist	99.72%
Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity.

HY-B0569

Hexamethonium Bromide	Antagonist	99.75%
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.

HY-107670

Dihydro-β-erythroidine hydrobromide	Antagonist	99.96%
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-100637

Hydroxybupropion	Antagonist	99.91%
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC₅₀ value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .

HY-B0429

Pancuronium dibromide	Antagonist	98.0%
Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action.

HY-P1050

COG 133	Antagonist	98.04%
COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC₅₀ of 445 nM.

HY-P0102

Dipeptide diaminobutyroyl benzylamide diacetate	Antagonist	99.72%
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-N3610

Coclaurine	Antagonist	98.97%
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-106901A

Asoxime dichloride	Antagonist	98.47%
Asoxime dichloride (HI-6) 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-135783

AT 1001	Antagonist	99.94%
AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a K_i value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease.

HY-101955

(2S,6S)-Hydroxynorketamine hydrochloride	Antagonist	99.30%
(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-101347

Chlorisondamine diiodide	Antagonist	99.6%
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-P1831

Proadrenomedullin (1-20), human	Antagonist	99.67%
Proadrenomedullin (1-20), human is a potent hypotensive and catecholamine release–inhibitory peptide released from chromaffin cells. Proadrenomedullin (1-20) inhibits catecholamine secretion in PC12 pheochromocytoma cells (IC₅₀ ≈ 350 nM) by suppressing Na⁺/Ca²⁺ influx and blocking desensitization. Proadrenomedullin (1-20), human specifically acts on nicotinic cholinergic receptors in a non competitive manner. Proadrenomedullin (1-20), human can be used for research on conditions such as hypertension.

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