neuronal nicotinic receptors

DMAB-anabaseine dihydrochloride (N,N-dimethyl-4-[(E)-(6-pyridin-3-yl-3,4-dihydro-2H-pyridin-5-ylidene)methyl]aniline;dihydrochloride) is an α7-containing neuronal nicotinic receptor partial agonist and an antagonist at α4β2 and other nicotinic receptors.

α-Conotoxin MII acetate is a 16-amino acid peptide from the venom of the marine snail Conus magus. α-Conotoxin MII acetate potently blocks nicotinic acetylcholine receptors composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII acetate potently blocks β3-containing neuronal nicotinic acetylcholine receptors.

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

suvn-911 is a potent and selective antagonist of neuronal nicotinic acetylcholine α4β2 receptor (Ki = 1.5 nM) with antidepressant activity.

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays >

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

RVG29, a peptide originating from Rabies Virus Glycoprotein, specifically targets the α-7 subunit of nicotinic acetylcholine receptors (AchR) on neuronal cells, thereby facilitating the transport of Mycobacterium tuberculosis antigens to antigen-presenting cells [1].

Alpha-Conotoxin EIIB is a peptide toxin derived from Conus ermineus that selectively binds to neuronal nicotinic acetylcholine receptors (nAChR) with a dissociation constant (Ki) of 2.2 nM. This compound is utilized in neurological research, including the study of schizophrenia, drug addiction, Alzheimer's disease, and Parkinson's disease [1].

Altinicline can bine with neuronal nicotinic acetylcholine receptors; SIB-1765F - fumarate.

α-Conotoxin MII TFA (α-CTxMII TFA), a peptide consisting of 16 amino acids derived from the venom of Conus magus, selectively inhibits nicotinic acetylcholine receptors (nAChRs) that are composed of α3β2 subunits, demonstrating an inhibitory concentration half-maximal (IC50) value of 0.5 nM. Additionally, it effectively targets β3-containing neuronal nicotinic receptors. [1] [2] [3]

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.

(S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU 282987, a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor, has negligible activity against α1β1γδ and α3β4 nAC

Spinosad is a naturally-occurring insecticide found in the the soil bacterium S. spinosa. It is a mixture of the macrocyclic lactones spinosyn A and spinosyn D, which act as agonists of insect nicotinic acetylcholinesterase receptors (nAChRs).

κ-Bungarotoxin (κ-Bgt) is a selective and potent antagonist of α3β2 neuronal nicotinic acetylcholine receptors, exhibiting slow reversibility and an IC50 of 2.30 nM [1].

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

NS 1738 (NSC-213859) is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nAChRs)

High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinic receptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronal nicotinic receptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695

Carbachol (Carbamoylcholine chloride), an analog of acetylcholine, serves as a valuable tool in the investigation of various physiological responses mediated by nicotinic (nAChR) and muscarinic (mAChR) acetylcholine receptors. These responses include smooth muscle contraction, gut motility, and neuronal signaling. Known for its agonistic properties, Carbachol activates both nAChR and mAChR, with reported Ki values ranging from 10 to 10,000 nM for different receptor types and experimental preparations.

α-Conotoxin Bt1.8 is a potent inhibitor of both rat α6/α3β2β3 and α3β2 neuronal nicotinic acetylcholine receptors (nAChRs), exhibiting half-maximal inhibitory concentrations (IC50s) of 2.1 nM for α6/α3β2β3 and 9.4 nM for α3β2, respectively [1].

Nelonicline is a selective agonist of neuronal nicotinic receptors.

Dihydro-β-erythroidine hydrobromide(DHβE) is a potent, oral active and competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs). Dihydro-β-carotene hydrobromide showed selectivity to α4β4 and α4β2nAChR, with IC50 of 0.19 and 0.37 μM,

Rivanicline is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM). It show > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM and IC50 : 26 nM).

Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat

neuronal nicotinic ACh receptors (nAChRs) antagonist

Encenicline hydrochloride (EVP-6124 hydrochloride) is a new-type partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).