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Nicotinic acetylcholine receptor (nAChR) agonists, antagonists and modulators act on ligand-gated cation channels. Each receptor is a pentamer of subunits arranged around a central pore that opens when acetylcholine binds. A refined structure of the Torpedo receptor at 4 Å resolution, published in 2005, resolved its ligand-binding, membrane and cytoplasmic regions. Muscle-type receptors mediate neuromuscular transmission, while neuronal subtypes such as α7 and α4β2 are studied in attention, memory and nicotine dependence. Agonists include PNU 282987, which is selective for α7, and the partial agonist varenicline. PNU-120596, described in 2005, is a positive allosteric modulator of α7 that enhances acetylcholine-evoked currents. Vecuronium bromide, a neuromuscular blocking agent, acts on the muscle-type receptor.
Synonyms: OC-02
Simpinicline (OC-02) is a highly selective agonist of the nicotinic acetylcholine receptor (nAChR). This compound exhibits potent antiviral activity against SARS-CoV-2 variants in cell culture, with an IC50 value of 0.04 µM. Its unique selectivity and efficacy make it a valuable tool for research in virology and neuropharmacology.
Synonyms: CMI 545 dihydrochloride
(±)-Epibatidine dihydrochloride is a potent nicotinic agonist known for its strong analgesic effects. This alkaloid, initially isolated from frog skin, exhibits selectivity, showing minimal or no activity at various central receptors such as opioid, muscarinic, adrenergic, dopamine, serotonin, and gamma-aminobutyric acid receptors. Its unique pharmacological profile makes it a valuable tool for investigating nicotinic receptor functions and developing analgesic therapies in research applications.
α-Nicotine is the α-isomer of nicotine and functions as an agonist of nicotinic acetylcholine receptors (nAChRs). This compound exhibits notable biological activity that may be beneficial for understanding neuropsychiatric disorders, including schizophrenia and attention deficit hyperactivity disorder (ADHD). Its potential applications in research make it a valuable tool for exploring the pharmacological effects of nAChR activation.
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Spinosad is an acetylcholine agonist that acts primarily on the nicotinic acetylcholine receptors (nAChRs) in the insect nervous system. Derived from the fermentation products of the soil actinomycete Saccharopolyspora spinosa, Spinosad exhibits potent biological neurotoxic activity, making it effective as a broad-spectrum insecticide. Its favorable environmental and mammalian safety profile, along with its larvicidal properties, supports its use in various pest control applications.
Acetamiprid is a neonicotinoid insecticide that acts as a selective agonist of nicotinic acetylcholine receptors (nAChRs). It disrupts normal synaptic transmission, leading to paralysis and death in target pests. Research applications include studies on neuromuscular function, insect behavior, and potential reproductive impacts in non-target organisms.
PHA-543613 is a selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting a Ki value of 8.8 nM. This compound demonstrates significant selectivity for the α7 nAChR compared to other nicotinic and serotonergic receptors, including α3β4, α1β1γδ, α4β2, and 5-HT3. PHA-543613 is applicable in research focused on cognitive deficits associated with Alzheimer's disease and schizophrenia, making it a valuable tool for neuropharmacological studies.
Flupyradifurone is a systemic agonist of nicotinic acetylcholine receptors (nAChRs) that disrupts signal transduction in the central nervous system of sap-sucking insects. It functions as a butenolide insecticide, effectively targeting pest populations while offering low toxicity to non-target organisms. Research applications include studying insect neurobiology and developing pest management strategies.
Synonyms: Ebanicline dihydrochloride; ABT-594 dihydrochloride
Tebanicline dihydrochloride is a selective agonist of nicotinic acetylcholine receptors (nAChRs), particularly targeting the α4β2 subtype. It exhibits strong analgesic properties and demonstrates oral bioavailability. This compound is valuable for research into pain management and the modulation of cholinergic signaling in neurological studies.
Synonyms: ABT-089 dihydrochloride
Pozanicline dihydrochloride is a selective agonist for nicotinic acetylcholine receptors (nAChRs), specifically targeting the α4β2 subtype with a binding affinity (Ki) of 17 nM at rat brain nAChR sites. It exhibits an affinity of 16.7 nM for [3H]cytisine binding sites, demonstrating its potential in modulating cholinergic signaling. This compound is instrumental in research focused on neurological disorders, cognition enhancement, and the exploration of nAChR-related pathways. Its oral bioavailability further supports its utility in in vivo studies.
PHA 568487 free base is a selective agonist of the α-7 nicotinic acetylcholine receptor (nAchR). This compound has been shown to reduce neuroinflammation, making it a valuable tool for research in neurodegenerative diseases and disorders associated with inflammation. Its ability to modulate α-7 nAchR activity provides insights into cholinergic signaling and potential therapeutic strategies targeting these pathways.
NS3861 is a selective agonist of the heteromeric α3β4 nicotinic acetylcholine receptor (nAChR), exhibiting high-affinity binding with a Ki value of 0.62 nM. This compound also demonstrates varied affinities for other nAChR subtypes, with Ki values of 25 nM for α3β2, 7.8 nM for α4β4, and 55 nM for α4β2. NS3861 is valuable for research focused on synaptic transmission and neuropharmacology, facilitating studies of cholinergic signaling in conditions such as neurodegeneration and addiction.
Synonyms: AQW-051
VQW-765 is a selective agonist for the alpha-7 nicotinic acetylcholine receptor (α7-nAChR), exhibiting a pKD value of 7.56 in recombinant human α7-nAChR assays. This compound demonstrates anxiolytic-like effects in vivo, making it a valuable tool for the study of anxiety disorders and acute performance anxiety. Researchers can utilize VQW-765 to investigate the role of α7-nAChR modulation in neuropsychiatric conditions.
ABT-107 is a selective agonist of the α7 neuronal nicotinic receptor (nAChR), known for its neuroprotective properties. This compound has demonstrated effectiveness in protecting against nigrostriatal damage in rodent models, specifically in rats with unilateral 6-hydroxydopamine lesions. ABT-107 is a valuable tool for research applications focusing on neurodegenerative diseases and the role of nicotinic receptors in neurological function.
Anabaseine is a potent agonist of various nicotinic acetylcholine receptors (AChRs), including the neuromuscular α12β1γδ or α12β1γɛ and α7 subtypes. This brain-penetrant alkaloid toxin exhibits key biological activity as a stimulator of these receptors, making it valuable for research into neuromuscular transmission and neurobiology. Additionally, Anabaseine acts as a weak partial agonist at α4β2 nAChRs, further broadening its applications in studying cholinergic signaling pathways.
Synonyms: TC-5619
Bradanicline is a highly selective agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 17 nM and a Ki of 1.4 nM in human α7 nAChR assays. This compound is primarily utilized in research focused on cognitive disorders, providing insights into mechanisms of action and potential therapeutic applications for enhancing cognitive function.
Sulfoxaflor is an orally active agonist that specifically targets insect nicotinic acetylcholine receptors (nAChRs), including the α-bungarotoxin-insensitive subtypes nAChR1 and nAChR2. By binding to these receptors, Sulfoxaflor induces inward currents that result in neurotoxicity in insects. This compound is valuable for research applications in agricultural pest control, pesticide toxicology, and the pharmacology of insect neural receptors.
AR-R17779 hydrochloride is a potent and selective full agonist of the nicotinic acetylcholine receptor (nAChR), demonstrating Ki values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. This compound has been shown to enhance cognitive functions, such as learning and memory, in rodent models. Additionally, AR-R17779 hydrochloride exhibits anxiolytic properties and is capable of reducing inflammation through the activation of anti-inflammatory cholinergic pathways. Its diverse biological activities make it a valuable tool for research in neurobiology and inflammation.
A 85380 hydrochloride is a high-affinity agonist for neuronal nicotinic acetylcholine receptors (nAChRs), specifically exhibiting selectivity for the α4β2 subtypes. This compound demonstrates a broad-spectrum analgesic profile, making it valuable for research in pain mechanisms and therapeutic applications. Its unique properties facilitate investigations into the roles of nAChRs in various biological processes.
AN317 is a selective agonist for the α6β2-containing nicotinic acetylcholine receptor (nAChR), exhibiting Ki values of 6.2 nM for the α6/α3β2β3 receptor and 4.1 nM for the α4β2 receptor. This compound effectively induces dopamine release in rat striatum synaptosomes and enhances dopaminergic neuronal activity in the substantia nigra. Additionally, AN317 demonstrates neuroprotective effects against dopamine neurotoxin MPP+ and possesses favorable pharmacokinetic properties, including the ability to cross the blood-brain barrier. Research applications include studies in neuropharmacology and the exploration of mechanisms underlying dopaminergic signaling.
α7 Nicotinic receptor agonist-1 is a selective agonist for the α7 nicotinic acetylcholine receptor (nAChR). This compound plays a crucial role in the modulation of neurotransmitter release and is significant in studies investigating various psychiatric and neurocognitive disorders. Its applications include research on conditions such as schizophrenia, anxiety disorders, Alzheimer's disease, cognitive deficits, and attention deficit hyperactivity disorder, providing insights into the therapeutic potential for these ailments.
Synonyms: 2-Propylpiperidine hydrochloride
(±)-Coniine hydrochloride is a potent agonist of the nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 value of 0.3 mM. It serves as an important tool in research focused on neurobiology and the modulation of cholinergic signaling. Due to its acute toxicity, characterized by an LD50 value of 7.7 mg/kg, careful handling is advised in laboratory settings.
(Rac)-CP-601927 hydrochloride is a racemic mixture of CP-601927, functioning as a nicotinic acetylcholine receptor (nAChR) agonist. It exhibits high affinity with Ki values of 1.2 nM for the α4β2 receptor and 102 nM for the α3β4 receptor. This compound is utilized in research applications focused on neurological studies and the modulation of synaptic transmission involving nAChRs.
Synonyms: 3-Br-cytisine
3-Bromocytisine is a potent agonist of nicotinic acetylcholine receptors (nAChRs), exhibiting IC50 values of 0.28 nM, 0.30 nM, and 31.6 nM for human α4β4, α4β2, and α7 nAChRs, respectively. It demonstrates differential effects on high sensitivity (HS) and low sensitivity (LS) α4β2 nAChRs, with EC50 values of 8 nM and 50 nM, respectively. This compound is valuable for research in neuropharmacology and studies related to nicotine addiction and receptor pharmacodynamics.
5-AAM-2-CP is a potent nAChR agonist, primarily functioning as a significant metabolite of the neonicotinoid insecticide Acetamiprid. Its primary biological activity includes the modulation of nicotinic acetylcholine receptors, which plays a critical role in neurotransmission. This compound is essential for research applications focused on neurobiology and insect neurophysiology, offering insights into the mechanisms of insecticides and synaptic transmission.
5-AMAM-2-CP is a potent agonist of nicotinic acetylcholine receptors (nAChRs). As a key metabolite of the neonicotinoid insecticide Acetamiprid, it plays a significant role in understanding the neurotoxic effects of neonicotinoids on non-target species. This compound is valuable for research into nAChR-mediated pathways and their implications in both insect physiology and environmental science.
