nAChR

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  1. nAChR Agonist

    Spinosyn L is a selective agonist of nicotinic acetylcholine receptors (nAChR). It induces sustained neural excitation and paralysis in insects, demonstrating effective activity against various agricultural pests, including Lepidoptera and Diptera. This compound is valuable for research applications focused on developing novel pesticides and understanding insect physiology.
  2. Insecticide Agent

    nAChR modulator-2 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChRs). This compound functions as an effective insecticide by influencing neurotransmission in target insects, leading to neurotoxic effects. It is particularly useful in research applications aimed at understanding insect physiology and the development of novel pest control strategies.
  3. nAChR Inhibitor

    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.
  4. α7 nAChR Agonist

    Bradanicline tosylate is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR) with significant oral bioavailability and moderate blood-brain barrier penetration. It demonstrates high affinity and subtype specificity for human α7 nAChR, exerting antitussive effects through prolonged receptor activation. Bradanicline tosylate effectively inhibits cough responses induced by citric acid, bradykinin, and inhaled nicotine in a dose-dependent manner. This compound is well tolerated in preclinical studies, making it a valuable tool in research focused on chronic refractory cough and related therapeutic areas.
  5. Insecticide Agent

    nAChR modulator-1 is an orthosteric modulator of insect nicotinic acetylcholine receptors (nAChR), functioning as a targeted insecticide agent. This compound demonstrates significant biological activity by disrupting neurotransmission in insects, leading to paralysis and death. It is widely utilized in research applications for studying pest control mechanisms and developing novel insecticide strategies.
  6. NF-κB Inhibitor

    (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.
  7. nAChR Agonist

    SIB-1508Y is an orally active and selective agonist of the nicotinic acetylcholine receptor (nAChR). It holds potential for research applications related to parkinsonism and neurodegenerative disorders. Additionally, SIB-1508Y features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
  8. α7 nAChR Agonist

    Nelonicline citrate is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with high affinity, as demonstrated by a Ki value of 12.3 nM in human brain tissue. This compound is primarily utilized in research investigating schizophrenia and Alzheimer's disease, providing insights into the modulation of cognitive processes and synaptic plasticity associated with these neurological disorders. Its oral bioavailability makes it a valuable tool for in vivo studies.
  9. nAChR Agonists

    SIB 1663 is a conformationally restricted analog of nicotine that selectively activates α2β4 and α4β4 human recombinant neuronal nicotinic acetylcholine receptors (nAChRs). This compound has been shown to enhance the release of dopamine (DA) and norepinephrine (NE), making it a valuable tool in the study of neurotransmitter dynamics. SIB 1663 is applicable in neurological disease research, providing insights into the mechanisms underlying various neuropharmacological conditions.
  10. α7nACh Agonist

    Epibatidine is an α7 nicotinic acetylcholine receptor (nAChR) agonist with a Kd of 100 nM. This compound is a valuable tool for investigating neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as psychiatric conditions like schizophrenia. By activating the α7nACh receptors, Epibatidine can provide insights into cholinergic signaling and its implications in these disorders.
  11. α7 nAChR Agonist

    WYE-103914 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting EC50 values of 0.49 µM for rat and 0.57 µM for human receptors. This compound is known to enhance cognitive functions and memory in various experimental models. It is also utilized in research focusing on schizophrenia and can be administered alongside antipsychotic therapies to investigate potential synergistic effects.
  12. α7 nAChR Activator

    IND8 is an activator of the α7 nicotinic acetylcholine receptor (nAChR), known for its cognitive enhancement properties. This compound has demonstrated efficacy in improving spatial working memory, episodic short-term memory, and spatial long-term memory in amnesic mice induced by Scopolamine. IND8 is particularly relevant for research on Alzheimer's disease and can be utilized in studies investigating interventions for cognitive decline.
  13. Antidepressant Agent

    Cypenamine hydrochloride is an antidepressant agent that selectively interacts with human nicotinic acetylcholine receptors (nAchR) subtypes, specifically α2β4, α3β4, and α4β4, exhibiting Ki values of 4.65 μM, 2.69 μM, and 4.11 μM, respectively. This compound is commonly used in research to investigate its potential therapeutic effects in mood disorders and the underlying mechanisms of action related to neurotransmitter regulation.
  14. α7 nAChR PAMs

    GAT107 is a potent positive allosteric modulator (PAM) of the α7 nicotinic acetylcholine receptor (nAChR). It enhances receptor activity, making it useful for research into neuropharmacology and potential treatments for cognitive disorders. Its mechanism allows for modulation of cholinergic signaling, which is crucial in areas such as memory and learning. GAT107 can aid in elucidating the functional properties of α7 nAChR in various biological contexts.
  15. α7 nAChR Agonist

    Bradanicline hydrochloride is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. This compound demonstrates significant biological activity that supports research into cognitive disorders and schizophrenia. Its targeted mechanism makes it a valuable tool for studying therapeutic approaches in neuropsychiatric conditions.
  16. nAChR Antagonist

    SR 16584 is a selective antagonist of the α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting an IC50 value of 10.2 μM. This compound is utilized in research investigating the role of nAChRs in neurological disorders and potential therapeutic applications. Its specific inhibition of α3β4 nAChR makes it valuable for studying the receptor's involvement in neurotransmission and related signaling pathways.
  17. nAChRs Agonist

    SIB-1553A free base is an orally bioavailable agonist of nicotinic acetylcholine receptors (nAChRs), exhibiting selective activity towards receptors containing the β4 subunit. This compound serves as a selective ligand for neuronal nAChRs and demonstrates significant cognitive-enhancing properties. SIB-1553A free base shows therapeutic potential for addressing symptoms associated with Alzheimer's disease and other cognitive disorders in research applications.
  18. α7 nAChR Partial Agonist

    AZD0328 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). It is known to enhance midbrain dopaminergic neuronal activity and increase cortical dopamine levels, contributing to improved cognitive performance. This compound is primarily used in research related to cognitive disorders and neurological modeling.
  19. α7 nACh Receptor Partial Agonist

    BMS-933043 is a selective partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). This compound has been shown to mitigate cognitive impairment in murine models, making it a valuable tool for research focused on cognitive dysfunction, particularly in the context of schizophrenia. Its unique mechanism facilitates the exploration of neuropsychological pathways and potential therapeutic interventions.
  20. α7 nAChR Agonist

    CP-810123 is a brain-permeable agonist of the α7 nicotinic acetylcholine receptor (nAChR). It demonstrates significant potential in enhancing cognitive function and is valuable for investigating cognitive impairments associated with psychiatric and neurological disorders, including schizophrenia and Alzheimer's disease. This compound serves as an important tool for researchers exploring therapeutic strategies aimed at modulating cholinergic systems in the context of cognitive deficits.
  21. α4β2 Agonist

    RJR-2429 is a potent agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 59 nM and a binding affinity (Ki) of 1 nM. This compound is known to induce contraction in the ileum, making it relevant for studies examining gastrointestinal motility and nAChR-mediated signaling pathways. RJR-2429 serves as a valuable tool in pharmacological research focused on neuropharmacology and cholinergic function.
  22. nAChR Agonist

    1,1-Dimethyl-4-acetylpiperazinium iodide is a potent agonist of nicotinic acetylcholine receptors (nAChRs), facilitating the opening of ion channels and leading to cell membrane depolarization. This compound is instrumental in studying synaptic transmission and has applications in neuropharmacology and neuromuscular research, providing insights into cholinergic signaling pathways and potential therapeutic interventions for related disorders.
  23. nAChR Ligand

    Hepzidine is a novel ligand for nicotinic acetylcholine receptors (nAChRs). It demonstrates binding affinity for acetylcholine binding protein (AChBP), making it a valuable tool in the study of cholinergic signaling. This compound is particularly relevant for neurobiological research, providing insights into the roles of nAChRs in various neurological conditions and processes.
  24. Stable Isotope

    Mecamylamine-d3 hydrochloride is a deuterium-labeled derivative of Mecamylamine hydrochloride, functioning as a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). This stable isotope is employed in research applications focused on neuropsychiatric disorders and the pharmacological assessment of nAChR activity. Its ability to cross the blood-brain barrier facilitates investigations into central nervous system functions and disorders, as well as potential therapeutic interventions.
  25. nAChR Modulator

    Bensultap is a nicotinic acetylcholine receptor (nAChR) modulator known for its insecticidal properties against the Colorado beetle and other insect pests. This compound exhibits mild and temporary neuromodulatory effects on the rat nervous system, making it relevant for research into nAChR function and insect neurobiology. Its applications extend to studies in pest management and the exploration of neural signaling pathways impacted by nAChR modulation.
  26. Alkaloid

    (±)-Coniine is a piperidine alkaloid known for its function as an nAChR agonist, demonstrating an EC50 of 0.3 mM. This compound exhibits acute toxicity in murine models, with an LD50 value of 7.7 mg/kg. Its unique properties make it valuable for research applications focused on neuromuscular transmission and toxicity studies.
  27. nAChR Agonist

    Hydroxy Varenicline is a metabolite of varenicline, functioning as a nicotinic acetylcholine receptor (nAChR) agonist. This compound exhibits key biological activity by modulating nAChR signaling, making it relevant for research on nicotine addiction and its neuropharmacological effects. Hydroxy Varenicline serves as a valuable tool in studies aimed at understanding receptor dynamics and developing therapeutic strategies for smoking cessation and related disorders.
  28. α4β2 nAChR Partial Agonist

    3-Pyr-Cytisine is a cytisine derivative that functions as a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR). This compound exhibits weak agonistic properties, making it of interest in antidepressant research. Its modulation of α4β2 nAChR may provide insights into therapeutic strategies for mood disorders and further understanding of cholinergic signaling pathways.
  29. nAChR Agonist

    Sofinicline benzenesulfonate is a potent agonist of the nicotinic acetylcholine receptor, specifically targeting the α4β2 subtype with an IC50 of 0.1 nM. This compound has demonstrated potential to enhance cognitive functions, including attention and memory, making it a valuable tool in the investigation of cognitive impairments. Its applications extend to research on attention deficit hyperactivity disorder (ADHD) and other cognitive disorders.
  30. nAChR Antagonist

    Microgrewiapine A is a selective antagonist of nicotinic acetylcholine receptors (nAChR), specifically inhibiting human α4β2 and α3β4 subtypes with 60% and 70% efficacy, respectively. This compound demonstrates cytotoxic effects in HT-29 human colon cancer cells, exhibiting an IC50 value of 6.8 μM. Microgrewiapine A holds potential for research applications in cancer biology and neuropharmacology.
  31. AChE/nAChR Inhibitor

    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.
  32. Stable Isotope

    Varenicline-13C,15N is a stable isotope-labeled variant of Varenicline, a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), with an IC50 of 250 nM. This compound also interacts with α6β2 nAChR as a partial agonist and activates α7β2 nAChR as a full agonist. Varenicline-13C,15N is utilized in research to study nicotine dependence and the pharmacodynamics of smoking cessation therapies, providing valuable insights into receptor interactions and metabolic pathways.
  33. nAChR Antagonist

    Dexmecamylamine is a selective antagonist of the nicotinic acetylcholine receptors (nAChR), specifically targeting the α3β4, α4β2, α7, and α1β1γδ subtypes with IC50 values in the micromolar range. This compound demonstrates notable anxiolytic and antidepressant-like effects, making it a valuable tool in neurological research and the study of mood disorders. Its ability to modulate nAChR activity positions it as a potential lead for therapeutic development in psychiatric conditions.
  34. nAChR Agonist

    TC-2216 is an agonist of the α4β2 neuronal nicotinic acetylcholine receptors (nAChRs). This compound demonstrates significant antidepressant and anxiolytic properties, validated by multiple animal models. TC-2216's modulation of nAChR activity represents its potential utility in neuropharmacological research and the development of therapeutic strategies for mood disorders.
  35. Calmodulin Inhibitor

    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.
  36. nAChR antagonist

    Waglerin-1 is a 22-amino acid peptide that acts as a competitive antagonist of the muscle nicotinic acetylcholine receptor (nAChR). It effectively inhibits nAChR-mediated signaling, making it a valuable tool for studying neuromuscular transmission and muscle physiology. This peptide is utilized in various research applications, including the investigation of synaptic mechanisms and the development of therapeutic strategies for neuromuscular disorders.
  37. nAChR/GABA Receptor Modulator

    Spinosyn J functions as a non-competitive modulator of nicotinic acetylcholine receptors (nAChR) and γ-aminobutyric acid (GABA) receptors. It exhibits significant insecticidal activity, making it a valuable compound for the study of agricultural pests. This property positions Spinosyn J as a useful tool in entomological research and pest management strategies.
  38. Insecticide

    Insecticidal agent 21 is a potent insecticide primarily targeting Culex pipiens larvae with an LC50 of 0.4 μg/mL. This compound exerts multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and affecting multiple neural receptors, including nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR). Insecticidal agent 21 demonstrates a strong insecticidal effect and is suitable for research applications focused on developing novel insecticides to combat resistance in mosquito populations.
  39. Stable Isotope

    Acetylcholine-d4 chloride is a deuterium-labeled form of the neurotransmitter acetylcholine. It functions as a potent cholinergic agonist and effectively crosses the blood-brain barrier (BBB). This reagent modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs) and has also been shown to inhibit the aggregation of p53 mutant peptides in vitro. Its unique isotopic labeling makes it a valuable tool for chemical and biological research applications.
  40. Stable Isotope

    Acetylcholine-d9 chloride is a deuterium-labeled form of acetylcholine chloride, a potent cholinergic agonist that effectively crosses the blood-brain barrier. This compound modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs). Additionally, it has been shown to inhibit p53 mutant peptide aggregation in vitro, making it valuable for research focused on neurobiology, receptor pharmacology, and protein aggregation studies.
  41. α7 nAChR Allosteric Modulator

    PAM-2 is a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR). Exhibiting potent anti-nociceptive and anti-inflammatory properties, PAM-2 enhances receptor activity, demonstrating efficacy in animal models of neuropathic pain induced by Streptozotocin and Oxaliplatin. It shows selectivity for α7 nAChR over α9α10 nAChR and CaV2.2 channels, making it a valuable tool for research into pain mechanisms and potential therapeutic applications in neuropathic pain.
  42. α9α10 nAChR/CaV2.2 Antagonist

    GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels.
  43. Racemate of Anabasine

    (±) Anabasine hydrochloride is a racemic mixture of the alkaloid Anabasine, functioning primarily as an agonist of the alpha-7 nicotinic acetylcholine receptor (α7nAChR). This compound demonstrates notable anti-inflammatory properties, making it useful in studies related to inflammation and neuropathology. Additionally, it exhibits insecticidal activity, proving beneficial in entomological research.
  44. Isotope-Labeled Compounds

    (±) Anabasine-d4 is a deuterated analog of (±) Anabasine, serving as a useful isotope-labeled compound. This racemic mixture acts as an agonist of the α7 nicotinic acetylcholine receptor (α7nAChR), demonstrating notable anti-inflammatory properties and insecticidal activity. It is suitable for applications in pharmacological research, particularly studies involving receptor activation and inflammatory responses.
  45. Racemate of Anabasine

    (±) Anabasine is the racemic mixture of Anabasine, acting as an agonist of the alpha-7 nicotinic acetylcholine receptor (α7nAChR). This compound has demonstrated anti-inflammatory properties and insecticidal activity, making it relevant for research in neuropharmacology and pest control studies. Its biological activities encourage further investigations into its therapeutic potential and applications.
  46. nAChR Modulator

    JNJ-1930942 is a selective positive allosteric modulator of the α(7) nicotinic acetylcholine receptor (nAChR) that effectively crosses the blood-brain barrier. This compound facilitates heightened intracellular Ca2+ levels and promotes neurotransmission at synapses in the hippocampal dentate gyrus. Additionally, JNJ-1930942 has been shown to reverse sensory gating deficits in DBA/2 mouse models, making it a valuable tool for research in neuropsychiatric disorders and synaptic physiology.
  47. α7 nAChR Agonist

    WAY-361789 is an orally active agonist of the α7 nicotinic acetylcholine receptor (α7 nAChR), with an EC50 of 0.18 μM. This compound enhances cognitive function and shows promise in addressing cognitive deficits associated with Alzheimer's Disease and schizophrenia. It serves as a valuable tool for researchers investigating the role of α7 nAChR in neurodegenerative conditions and psychiatric disorders.
  48. Intermediate

    2-Chloropyridine-4-boronic acid is a versatile chemical intermediate primarily used in the synthesis of nicotinic acetylcholine receptor (nAChR) agonists. Its boronic acid functionality facilitates cross-coupling reactions, making it valuable in the development of various bioactive compounds. Additionally, this reagent has applications in cancer research, contributing to the exploration of novel therapeutic strategies.
  49. Biochemical Assay Reagent

    Decamethonium iodide is a neuromuscular blocking agent that targets nicotinic acetylcholine receptors (nAChRs) at the neuromuscular junction. Its primary mechanism involves binding to nAChRs, leading to depolarization block and resulting in skeletal muscle paralysis, making it essential in anesthesia for inducing muscle relaxation during surgical procedures. Additionally, Decamethonium iodide serves as a valuable reference standard in pharmacological studies focused on nAChRs, facilitating research into neuromuscular transmission and receptor function.
  50. Neuromuscular Blocking Agent

    Vecuronium bromide is a non-depolarizing neuromuscular blocking agent that selectively inhibits nicotinic acetylcholine receptors (nAChRs). This compound induces muscle relaxation and is primarily utilized in the context of anesthesia during surgical procedures. Its rapid onset and intermediate duration of action make it a valuable tool for facilitating intubation and providing muscle relaxation in various clinical settings.

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