A potent, subtype-selective α3β4 nAChR partial agonist with Ki of 0.62 nM; selectively activates receptors containing β4- but not β2-subunits, shows no efficacy at α4β2 receptors and only marginal efficacy at α4β4 receptors expressed in oocytes; enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment.
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors[1][2][3].
Anagyrine is an alkaloid that has been found in L. albus and has nematocidal and anticancer activities[1].It binds to muscarinic and nicotinic acetylcholine receptors (AChRs) with IC50 values of 132 and 2096 µM respectively[2].
κ-Bungarotoxin (κ-Bgt) is a potent, selective, and slowly reversible antagonist of α3β2 neuronal nicotinic acetylcholine receptors with an IC50 of 2.30 nM[1].
PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR)[1][2].PHA 568487 reduces neuroinflammation and oxidative stress[2]. PHA-568487 has rapid brain penetration[3].
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM[1].
BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression[1].
α-Conotoxin GID is a paralytic peptide neurotoxin and a selective antagonist of nAChR, with IC50s of 5 nM (α7), 3 nM (α3β2)， 150 nM (α4β2), respectively. α-Conotoxin GID is small disulfide-rich peptide, with potential to inhibit chronic pain. α-Conotoxin GID contains a C-terminal carboxylate, thus substitution with a C-terminal carboxamide results in loss of α4β2 nAChR. α-Conotoxin GID can be isolated from the Conus species[1][2][3].
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively[1].
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing[1].
Dihydro-β-erythroidine is a a competitive nicotinic receptor antagonist. Dihydro-β-erythroidine blocks the discriminative stimulus properties of nicotine. Dihydro-β-erythroidine inhibits the anxiolytic effect of nicotine induced[1][2].
Lobeline (α-Lobeline; L-Lobeline), a lipophilic alkaloidal, is a nicotinic receptor agonist. Lobeline inhibits d-methamphetamine self-administration with no dopaminergic toxicity. Lobeline rescues d-amphetamine abuse induced addictive effect. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage[1][2][3].
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant[1].
T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist[1].
(S)-(-)-Levamisole (Levamisole), an anthelmintic agent with immunomodulatory properties. (S)-(-)-Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active[1][2].
Rabies Virus Matrix Protein Fragment (RV-MAT) is a polypeptide. Rabies Virus Matrix Protein Fragment targets the acetylcholine receptor (AChR) that exists on the cell surface[1].
Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418[1].
Triflumezopyrim, a mesoionic insecticide, has high efficiency at a low dosage, and is mainly used to control hopper species. Triflumezopyrim mainly acts on the nicotinic acetylcholine receptor (nAChR) inhibition, which is very highly 44 efficient, rapidly effective, and nearly nontoxic to nontarget arthropods[1].
nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM)[1].
MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM[1].
ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease[1].
RGH-560 (compound 53) shows highly advanced α7 nAChR positive modulator properties and favorable physicochemical features. RGH-560 has robust procognitive in vivo potential. RGH-560 can be used to study Scopolamine (HY-N0296) -induced amnesia in mice[1].
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM[1].
Lupanine (D-Lupanine) hydrochloride is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine hydrochloride shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM[1].
(R)-Dinotefuran ((R)-MTI-446), a neonicotinoid pesticide, exhibits comparative insecticidal activities (1.7-2.4 times) to typical sucking pests Aphis gossypii and Apolygus lucorum compared to racemic mixtures by inhibiting nicotinic acetylcholine receptors. (R)-Dinotefuran has a good efficacy in controlling target pests while minimizing hazard to honeybees[1].
RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist[1].
(Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases[1].
ABT-107 is a potent and selective α7 nAChR agonist with Ki of 0.2-0.6 nM for rat or human cortex α7 nAChRs; displays >100-fold selective versus non-α7 nAChRs and other receptors; potently evokes human and rat α7 nAChR current responses in oocytes (EC50=50-90 nM) enhanced by A-867744; reduces spinal tau hyperphosphorylation in tau/amyloid precursor protein transgenic AD mice; improves cognition in monkey. Alzheimer Disease Phase 2 Discontinued