nAChR Antagonist
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Methyllycaconitine citrate
0 ImagesSynonyms: MLA citrateMethyllycaconitine (MLA) citrate is a blood-brain barrier-permeable antagonist of α7 nicotinic acetylcholine receptor (α7nAChR) with an IC50 of 2 nM. Methyllycaconitine citrate inhibits Aβ25-35-induced autophagy by restoring the mTOR pathway, and prevents reactive oxygen species (ROS) production, microglial activation, reduced dopamine uptake, loss of dopaminergic terminals and catecholamine secretion. Methyllycaconitine citrate induces hippocampal glutamate efflux, enhances long-term potentiation, and improves memory acquisition. Methyllycaconitine citrate can be used in research related to Alzheimer's disease, cerebral palsy, Parkinson's disease and schizophrenia.
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Mecamylamine hydrochloride
0 ImagesMecamylamine 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.
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α-Bungarotoxin, FITC labeled
0 ImagesArt. -Nr.: HY-P1264FFITC-labeled α-Bungarotoxin is FITC-conjugated α-Bungarotoxin (HY-P1264). α-Bungarotoxin acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChRs).
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COG 133 TFA
0 ImagesCOG 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.
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α-Bungarotoxin
0 Imagesα-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.
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Cisatracurium besylate
0 ImagesSynonyms: 51W89 besylate; Cisatracurium besilateCisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
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Dequalinium Chloride
0 ImagesDequalinium 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.
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Hexamethonium Bromide
0 ImagesHexamethonium 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.
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Dihydro-β-erythroidine hydrobromide
0 ImagesSynonyms: DHβE hydrobromideDihydro-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.
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Hydroxybupropion
0 ImagesHydroxybupropion 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 .
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Pancuronium dibromide
0 ImagesPancuronium 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.
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COG 133
0 ImagesCOG 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.
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Dipeptide diaminobutyroyl benzylamide diacetate
0 ImagesDipeptide 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.
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Coclaurine
0 ImagesCoclaurine 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.
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Asoxime dichloride
0 ImagesSynonyms: HI-6Asoxime 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.
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AT 1001
0 ImagesAT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki 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.
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(2S,6S)-Hydroxynorketamine hydrochloride
0 ImagesSynonyms: (2S,6S)-HNK hydrochloride(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.
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Proadrenomedullin (1-20), human
0 ImagesSynonyms: ProAM N20, Human; PAMP-20, humanProadrenomedullin (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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Anagyrine
0 ImagesSynonyms: (-)-Anagyrine; Monolupine; RhombinineAnagyrine ((-)-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.
