nAChR Inhibitor

Mr1.1[S4Dap, C16Pen] is a highly active and selective nAChR (human α9α10 nAChR IC₅₀ = 4.0 nM, rat α9α10 nAChR IC₅₀ = 2.7 nM) inhibitor. Mr1.1[S4Dap, C16Pen] can significantly relieve pain and has significant stability. Mr1.1[S4Dap, C16Pen] can be used for the study of neuropathic pain.

Aristoquinoline (Compound 1) is an alkaloid can be isolated from Aristotelia chilensis. Aristoquinoline has α3β4 nAChR inhibitory activity.

Migrastatin is a typical Fascin1 inhibitor. Migrastatin is isolated from a cultured broth of Streptomyces sp. MK929-43F1. Migrastatin inhibits tumor cell migration.

Dinotefuran (Standard) is the analytical standard of Dinotefuran. This product is intended for research and analytical applications.

(R)-Dinotefuran ((R)-MTI-446), a neonicotinoid pesticide, exhibits comparative insecticidal activities (1.7-2.4 times) to typical sucking pests Aphis gossypii and Apolygus lucorum compared to racemic mixtures by inhibiting nicotinic acetylcholine receptors. (R)-Dinotefuran has a good efficacy in controlling target pests while minimizing hazard to honeybees.

Isoaminile is an antitussive agent and an anticholinergic compound with antimuscarinic and antinicotinic properties. Isoaminile blocks the effects of acetylcholine and McN-A-343 at ganglionic sites, inhibits responses to preganglionic sympathetic and splanchnic nerve stimulation, and does not affect postganglionic nerve- or adrenergic-mediated responses. Isoaminile inhibits nictitating membrane contraction and induced hypertension, suppresses isolated guinea pig atrial activity, and stimulates central vagal nerve activity to trigger bradycardia. Isoaminile exerts effects of antitussive action, respiratory inhibition, central nervous system excitation, and cardiovascular function regulation.

nAChR-IN-1 (hydrochloride) 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.

Insecticidal agent 12 (Compound F45) has insecticidal activity (LC₅₀: 2.94 μg/mL). Insecticidal agent 12 is an nAChR inhibitor.

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

AChE-IN-117 is an AChE/nAChR inhibitor with larvicidal activity against Culex pipiens third-instar larvae. AChE-IN-117 forms stable catalytic site interactions to disrupt cholinergic signaling. AChE-IN-117 binds to its receptor via hydrogen bonding and π-cation interactions to interfere with cholinergic synaptic transmission. AChE-IN-117 induces neurotoxic symptoms including hyperactivity, erratic movement, tremors, paralysis, and larval mortality. AChE-IN-117 can be used for the research of mosquito-borne infectious diseases.

Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2).

Erysodine is a blood-brain barrier-permeable nicotinic acetylcholine receptor (nAChR) ligand with high affinity for α4β2 nAChR, K_i = 5 nM, and it blocks nicotine-induced dopamine release and behavioral effects through competitive inhibition. Erysodine is useful for studies on alcohol dependence.

WrFr-OCH3 is a competitive nAChR inhibitor, with IC₅₀ values of 291.9 nM, 25.3 nM, 477.5 nM and 36.5 nM against hα1β1εδ nAChR, hα9α10 nAChR, hα7 nAChR and hα9 nAChR, respectively. WrFr-OCH3 exhibits analgesic and muscle relaxant effects, reduces forelimb grip strength in rats, and alleviates Oxaliplatin (HY-17371)-induced cold allodynia in rats. WrFr-OCH3 can be used in studies related to cold allodynia.

(S)-Dinotefuran ((S)-MTI-446), a neonicotinoid pesticide, is toxic by binding to α8 subunit of nAChR of honeybee Apis mellifera (Apis mellifera Linnaeus). (S)-Dinotefuran shows more toxic than R-dinotefuran to honeybee Apis mellifera.

(S)-Norzopiclone ((S)-N-Desmethyl zopiclone; SEP-174559) is a metabolite of Zopiclone with anxiolytic and anticonvulsant effects. (S)-Norzopiclone has benzodiazepine-like actions at γ2-bearing subtypes of the GABA_A receptor and inhibits nACh and NMDA receptors.

NS-6740 hydrochloride is a silent agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC₅₀ of 3 nM. NS-6740 hydrochloride reduces LPS-induced TNF-α release and regulates the cholinergic anti-inflammatory pathway. NS-6740 hydrochloride exerts anti-inflammatory effects. NS-6740 hydrochloride reduces long-term potentiation in hippocampal brain slices. NS-6740 hydrochloride can be used in research related to neuroinflammation and schizophrenia.

(+)-Vesamicol ((+)-AH5183) is an acetylcholine vesicular transport system inhibitor. (+)-Vesamicol blocks acetylcholine storage and uptake by synaptic vesicles, reducing transmitter availability for neuromuscular junction release. (+)-Vesamicol acts as a neuromuscular blocking agent, producing frequency-dependent neuromuscular block in rat hemidiaphragm preparations.

Conofurin-Delta is a potent α7 nAChR inhibitor with an IC₅₀ of 177 nM. Conofurin-Delta also inhibits α9α10 nAChR with an IC₅₀ of 98.1 nM. Conofurin-Delta may be used in SARS-CoV-2 infection research.

Insecticidal agent 25 (Compound WZ18) is an insecticide targeting the nicotinic acetylcholine receptors (nAChRs) in insect nervous systems. Insecticidal agent 25 disrupts neurotransmission by competitively binding to nAChRs, leading to insect paralysis and death.

Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. 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.