nAChR

Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug

Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.

Vinblastine sulfate inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer.

EVP-6124 is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs); shows selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.

EVP-6124 hydrochloride is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs). EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.

Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.

NS-6740 hydrochloride is a potent partial agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), exhibiting an IC50 of 3 nM. It functions as a modulator of the cholinergic anti-inflammatory pathway and alters α7 signaling in an ion channel-independent manner, which diminishes synaptic function and promotes receptor desensitization. NS-6740 hydrochloride has been shown to significantly reduce LPS-induced TNF-α release from microglia, making it a valuable tool in the study of neuroinflammation and neuropathic pain mechanisms.

Conofurin-Delta is a potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 of 177 nM. Additionally, it demonstrates inhibitory activity against the α9α10 nAChR with an IC50 of 98.1 nM. This compound is relevant for research applications in the study of SARS-CoV-2 infection and its impact on cholinergic signaling pathways.

Dinotefuran is a competitive inhibitor targeting insect nicotinic acetylcholine receptors (nAChRs). This compound effectively disrupts neural signaling in insects, leading to dysfunction. With an IC50 of 890 nM for [3H]epibatidine and 36.1 μM for [3H]α-bungarotoxin in American cockroach neural membranes, Dinotefuran demonstrates significant knockdown (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Its primary applications include agricultural pest control, specifically targeting piercing-sucking and chewing insects like aphids and planthoppers, and it also serves as a tool for studying environmental toxicological impacts such as oxidative stress and reproductive neurotoxicity in earthworms.

Meclofenoxate, a nAChR inhibitor, is an ester derived from dimethylaminoethanol (DMAE) and para-chlorophenylalanine (pCPA). It is known for its potential to enhance memory and cognitive function. Meclofenoxate is commonly utilized in neurological research to investigate mechanisms underlying cognitive enhancement and memory improvement.

Asoxime dichloride is a reversible inhibitor of acetylcholinesterase (AChE) that functions as a thiosemicarbazone-based antidote. Its primary mechanism involves reactivating AChE that has been inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dichloride enhances muscle function in the presence of poisoning without reactivating AChE and acts as an antagonist to acetylcholine receptors, including nicotinic and α7 nAChRs. Due to its immunomodulatory properties, Asoxime dichloride can also enhance the immune response of the nervous system, making it valuable in neuropharmacological research.

Lupanine is a natural ketonic derivative of Sparteine that acts as an inhibitor of nicotinic acetylcholine receptors (nAChR). It exhibits binding affinity to these receptors with a Ki value of 500 nM, demonstrating its potential as a ganglioplegic agent. Lupanine is utilized in research applications related to neuromodulation and the study of cholinergic signaling pathways.

CVN417 is an orally active antagonist of the α6 subunit-containing nicotinic acetylcholine receptors (nAChRs). This inhibitor modulates phasic dopaminergic neurotransmission in an impulse-dependent manner and exhibits inhibitory effects on Ca(2+) efflux through various nAChR subunits, with IC50 values of 0.086 μM for α6, 2.56 μM for α3, and 0.657 μM for α4. CVN417 has demonstrated efficacy in reducing resting tremors in rodent models and may offer therapeutic potential for improving movement dysfunction associated with Parkinson's disease.

Triflumezopyrim is a selective inhibitor of the nicotinic acetylcholine receptor (nAChR), exhibiting potent insecticidal activity at low dosages. Its primary application is in the control of hopper species, where it demonstrates rapid efficacy while maintaining low toxicity to non-target arthropods. This compound is particularly valuable in agricultural research and pest management studies focused on sustainable and selective insect control strategies.

nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a selective inhibitor of nicotinic acetylcholine receptors (nAChRs) that specifically targets receptors lacking α5, α6, or β3 subunits. This compound demonstrates significant potential in alleviating nerve disorders and is valuable for research focused on nAChR dysfunction and various neurological conditions. Its mechanism of action makes it an essential tool for studying the role of nAChRs in neurological signaling pathways.

Azemiopsin is a potent inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 0.18 μM against the T. californica nAChR and 22 μM against the human α7 nAChR. This compound effectively blocks acetylcholine-induced currents in Xenopus oocytes that are heterologously expressing human muscle-type nAChR. Azemiopsin serves as a valuable tool for investigating nAChR-mediated signaling pathways and contributes to studies on neuropharmacology and synaptic transmission.

nAChR-IN-2 is an inhibitor of insect nicotinic acetylcholine receptors (nAChR), targeting the acetylcholine binding site and the NCB/PCP binding site. It demonstrates an IC50 of 360 μM for α-bungarotoxin binding and 84 μM for Phencyclidine binding in honeybee head preparations. This compound is valuable for studying nAChR-mediated signaling pathways and their role in insect neurobiology. Research applications include investigating insecticide mechanisms and assessing the neurophysiological effects of nAChR modulation.

bPiDI is a selective antagonist of the α6β2 nicotinic acetylcholine receptors (nAChRs). It effectively inhibits nicotine-evoked dopamine release in the striatum, making it a valuable tool for studying dopaminergic signaling pathways. This compound is particularly useful in research pertaining to nicotine addiction and dopamine-related disorders.

Asoxime dimesylate is a reversible inhibitor of acetylcholinesterase (AChE) that serves as a thiosemicarbazone-based antidote. Its primary mechanism of action involves reactivating AChE inhibited by nerve agents, thus restoring cholinergic nerve function. Additionally, Asoxime dimesylate has been shown to significantly restore muscle function compromised by poisoning without the reactivation of AChE. It also acts as an antagonist at acetylcholine receptors, including nicotinic receptors and α7 nAChR, and demonstrates potential as an immunomodulator, enhancing immune responses in the nervous system. This compound is valuable for research in neuropharmacology and toxicology.

Lupanine perchlorate is a natural ketonic derivative of sparteine that functions as an nAChR inhibitor. It exhibits significant ganglioplegic activity and demonstrates a binding affinity for nicotinic receptors with a Ki value of 500 nM. This compound is commonly utilized in research focused on studying neuronal signaling and the effects of cholinergic modulation.

Ferulamide is a derivative of ferulic acid that acts as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). It exhibits significant anticholinesterase activity, making it a valuable tool for studying cholinergic signaling pathways. This compound is useful in research related to neurodegenerative diseases and the modulation of synaptic transmission.

QND8 is a selective and potent inhibitor of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant biological activity by alleviating thermal and mechanical hyperalgesia in carrageenan-induced inflammatory pain models. QND8 effectively reduces swelling, inhibits the release of pro-inflammatory cytokines, and prevents leukocyte infiltration at the inflammatory site. This compound is valuable for research applications focused on inflammation and neurological disorders, including arthritis.

Aristoquinoline is a naturally occurring alkaloid derived from Aristotelia chilensis, functioning primarily as an inhibitor of the α3β4 nicotinic acetylcholine receptor (nAChR). This compound demonstrates significant biological activity by modulating neurotransmitter signaling, making it a valuable tool for research in neuropharmacology, particularly in studies related to addiction, cognitive function, and neurodegenerative diseases. Its specific inhibitory effect on nAChR presents opportunities for investigating the receptor's role in various physiological processes.

nAChR-IN-1 hydrochloride is a selective nicotinic acetylcholine receptor (nAChR) inhibitor that specifically targets nAChRs lacking the α5, α6, or β3 subunits. This compound is particularly useful in studying the roles of nAChRs in neurological disorders and offers potential insights into therapeutic strategies for conditions involving nicotinic acetylcholine receptor dysfunction. Its effectiveness in modulating nAChR activity makes it a valuable tool for chemical biology and pharmacological research.

Lupanine hydrochloride is a natural ketonic derivative of Sparteine, functioning as a nicotinic acetylcholine receptor (nAChR) inhibitor. It demonstrates binding affinity for the nAChR with a Ki value of 500 nM, indicating its potential role in modulating cholinergic signaling. This compound is suitable for research applications related to neuromuscular transmission and ganglioplegic activity.

Xanthoplanine is an nAChR inhibitor derived from the root of Xylopia parviflora. It effectively inhibits the EC50 acetylcholine responses of both alpha7 and alpha4beta2 nicotinic acetylcholine receptors, demonstrating estimated IC50 values of 9 μM for alpha7 and 5 μM for alpha4beta2. Its potent inhibitory activity makes it a valuable tool for studying cholinergic signaling and related neurological pathways in research applications.

(R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders.

AChE/nAChR-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and nicotinic acetylcholine receptors (nAChR). This compound exhibits potent toxicity and larvicidal activity against Culex pipiens larvae, with an LC50 of 4 ng/mL. AChE/nAChR-IN-1 is utilized in research focused on controlling mosquito populations and studying mosquito-borne diseases.

Zaldaride is a selective calmodulin inhibitor that effectively inhibits CaM-stimulated cAMP phosphodiesterase activity, exhibiting an IC50 of 3.3 nM. This compound demonstrates significant biological activity by preventing estrogen-induced transcription activation mediated by estrogen receptors. Additionally, Zaldaride reversibly blocks voltage-activated sodium, calcium, and potassium currents in PC12 cells, and also inhibits nicotinic acetylcholine receptors (nAChR), making it a valuable tool for research into calcium signaling pathways and their related physiological processes.

(+)-Sparteine is a natural alkaloid that functions as a competitive inhibitor of nicotinic acetylcholine receptors (nAChRs). By blocking these receptors in neurons, it serves as a ganglionic blocking agent, impacting neurotransmission. This compound is utilized in research applications related to neurotransmitter signaling and the study of ganglionic transmission.

Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptors (nAChR), exhibiting IC50 values of 1.9 μM for α1, 1.8 μM for α3β4, 3.7 μM for α4β2, and 6.3 μM for α4β4. This compound demonstrates significant anticonvulsant properties, making it valuable for studies related to seizure disorders and neuropharmacology. Its selective action on various nAChR subtypes positions Adiphenine as a useful tool for exploring the role of these receptors in different biological contexts.