nachr agonist 1

nAChR agonist 1 (DUN71755) is a brain-permeable and orally efficacious positive allosteric α7 nicotinic acetylcholine receptor (α7 nAChR)modulator.

α7 nAchR-JAK2-STAT3 agonist 1 is a potent inhibitor of the α7 nAchR-JAK2-STAT3 pathway that acts on nitric oxide (NO) (IC50: 0.32 μM). It has demonstrated positive effects on iNOS, IL-1β, and IL-1β in murine macrophages RAW264.7, and inhibited the expression of iNOS, IL-1β, and IL-6 in mouse macrophages. Additionally, α7 nAchR-JAK2-STAT3 agonist 1 suppressed LPS-induced NO release, NF-κB activation, and cytokine production, making it useful for studying sepsis.

Pozanicline hydrochloride is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [3H]cytisine sites[1]. Pozanicline hydrochloride is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant[2].

Rivanicline hemioxalate, also known as RJR-2403 hemioxalate or (E)-Metanicotine hemioxalate, is a chemical compound acting as a neuronal nicotinic receptor agonist with pronounced selectivity for the α4β2 receptor subtype, showing over 1,000-fold greater selectivity for this subtype (Ki=26 nM) compared to α7 receptors (Ki=3.6 μM). Its in vitro studies demonstrate no significant activation of nAChRs in PC12 cells, muscle type nAChRs, or muscarinic receptors at concentrations up to 1 mM. Furthermore, Rivanicline displayed less than one-tenth the potency of nicotine in inducing ileum contraction, with substantially lower efficacy, and failed to antagonize nicotine-induced stimulation of muscle or ganglionic nAChR functions, with an IC50 value greater than 1 mM. Chronic exposure to Rivanicline at 10 microM led to up-regulation of high-affinity nAChRs in M10 cells, mimicking effects observed with nicotine. In vivo studies revealed that Rivanicline significantly reversed scopolamine-induced amnesia and improved working and reference memory in a rat model, while being 15 to 30 times less potent than nicotine in affecting body temperature, respiration, and other physiological responses. Metanicitone's potency was approximately five times lower than nicotine in tail-flick tests following subcutaneous administration, yet slightly more potent upon central administration.

AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

PNU-282987 (free base) is a potent agonist of α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 154 nM and a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. It can be used for central and peripheral nervous system studies[1].

Bradanicline is a potent and highly selective agonist of the α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 17 nM and a Ki of 1.4 nM for the human α7 nAChR. It is primarily employed in research pertaining to cognitive disorders [1] [2].

5-AMAM-2-CP, a significant metabolite of Acetamiprid, serves as a global insecticide within the neonicotinoid class and acts as an nAChR agonist [1] [2].

Epiboxidine, a methylisoxazole analog of the alkaloid Epibatidine and analog of the nAChR agonist ABT 418 [1], serves as a potent and selective agonist for neural nicotinic acetylcholine receptors (nAChR), exhibiting Ki values of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively.

Epiboxidine hydrochloride, a methylisoxazole analog of the alkaloid Epibatidine and an analog of the nAChR agonist ABT 418 [1], serves as a potent and selective agonist of neural nAChRs, demonstrating K i values of 0.46 nM and 1.2 nM for α4β2 nAChRs in rats and humans, respectively.

Flupyradifurone (flupyradifurone) is a systemic insecticide and nicotinic acetylcholine receptor (nAChR) agonist that acts by interfering with the nervous system of insects.

α-Conotoxin MrIC is a biased agonist selective for the α7 nicotinic acetylcholine receptor (nAChR), with activation contingent upon the presence of type II positive allosteric modulators, such as PNU120596. It is utilized to investigate neurological disorders and delineate the pharmacological characteristics of the α7nAChR [1].

NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs), acting as a partial agonist at α3β4 nAChR and binding with high affinity to heteromeric α3β4 nAChR, with binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1].

Anatoxin-a (ATX-a), a neurotoxic alkaloid, functions as an agonist for the nicotinic acetylcholine receptor (nAChR) and as an inhibitor of Acetylcholinesterase (AChE) [1] [2].