nAChR Inhibitor

Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

Vinblastine (sulfate) (Standard) is the analytical standard of Vinblastine (sulfate). This product is intended for research and analytical applications. Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC₅₀ of 8.9 μM.

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.

Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC₅₀ of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.

Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities.

Harman-¹³C₂,¹⁵N is ¹³C and ¹⁵N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research.

(+)-sparteine (sulfate pentahydrate) is a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.

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.

Meclofenoxate (hydrochloride) (Standard) is the analytical standard of Meclofenoxate (hydrochloride). This product is intended for research and analytical applications. Meclofenoxate hydrochloride is an ester synthesized from DMAE and pCPA, which has the activity of stimulating memory and improving cognition.

nAChR-IN-2 (Compound 2) is an inhibitor of insect nicotinic acetylcholine receptors (nAChR). nAChR-IN-2 inhibits the binding of α-bungarotoxin (HY-P1264) to the ACh site of insect nAChR in honeybee heads, with an IC₅₀ of 360 μM. nAChR-IN-2 also inhibits the binding of Phencyclidine to the NCB/PCP site of insect nAChR in honeybee heads, with an IC₅₀ of 84 μM.

Hydrodolasetron is a metabolite of Dolasetron (HY-B0750). Hydrodolasetron is more potent than Dolasetron in inhibiting nAChR. Hydrodolasetron is a 5-HT(3A)R blocker with an IC₅₀ of 0.29 nM. Hydrodolasetron has antiemetic activity.

Ganglefene is a blocker for n-choline receptor, which leads to the sexual dysfunction in the offspring in adulthood, when administrated to pregnant rats.

Lupanine (D-Lupanine) perchlorate is a natural ketonic derivative of Sparteine (HY-W008350)with a ganglioplegic activity. Lupanine perchlorate shows binding affinity for nicotinic receptor with a K_i value of 500 nM.

Meclofenoxate (Centrophenoxine) is an ester synthesized from DMAE and pCPA, which has the activity of stimulating memory and improving cognition.

Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities.

Adiphenine 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 has anticonvulsant effects.

BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC₅₀ = 18.00 pM, human BChE IC₅₀ = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ_1-42-induced injury model and inhibitory effects on Aβ_1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD).

Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

Sparteine (Lupinidine) is an alkaloid compound derived from leguminous plants and can act as a ganglionic blocker. Sparteine competitively inhibits the activity of the neuronal nicotinic acetylcholine receptor (nACh receptor).