>98%,Standard References

A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X.

B-973 (B973) is a potent, selective α7 nAChR ago-PAM, denonstrates analgesic effect with attenuating pain behavior and decreasing paw edema in vivo.

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

GTS 21 dihydrochloride is a partial agonist of α7 nicotinic acetylcholine receptors (nAChRs); also a weak α4β2 and 5-HT3 antagonist at micromolar concentrations.

Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia..

PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

Tebanicline hydrochloride (ABT594 hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.

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.

Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.

SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.

3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively.

D-Tubocurarine chloride pentahydrate is the chloride salt form of Tubocurarine, a nicotinic acetylcholine receptors (AChR) antagonist, and can be used as a skeletal muscle relaxant during surgery or mechanical ventilation. D-Tubocurarine chloride pentahydrate is also a potent neuromuscular blocking agent.

nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.

Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM.

Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.

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.

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.

TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 μM. Antinociceptive effect.

nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 μM) with an EC50 of 0.26 μM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.

5-AAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist.

5-AMAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist.

(S)-UFR2709 is a competitive nAChR antagonist?and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction.

(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist?and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction.

SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.

Benzoquinonium dibromide is a nicotinic acetylcholine receptors (nAChRs) antagonist, with an IC50 of 0.46 μM. Benzoquinonium dibromide can block neuromuscular and ganglionic transmission.

(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).

Ferulamide is a Ferulic acid derivative isolated from Portulaca oleracea L. with anticholinesterase activities.

COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.

α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.

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.

α-Conotoxin PnIA TFA, 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.

α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。

α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。

α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.

α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.

Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.

Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.

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 > 200-fold selectivity for α3β2 over α2β2, α4β2 and α3β4.

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

Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.

Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical?pesticide?nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 μM).

BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-drug like properties and clinical candidate potential. .

Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.

(Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively.

Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.

CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties.

α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.

DPNB-ABT594 is a nitrobenzyl-caged ABT594 and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca2+ signalling in the MHb.

TQS is a α7 nicotinic acetylcholine receptor (nAChR) positive allosteric modulator. TQS can be used for the research of neuroinflammatory pain.

Sulfoxaflor is a sulfoximine insecticide and is an agonist of nAChR1 and nAChR2 subtypes. Sulfoxaflor is used for the control of sap-feeding insects such as Myzus persicae, Aphis gossypii, Bemissia tabaci and Nilaparvata lugens.

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.

Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression.

Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM.

Anabaseine, an alkaloid, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular receptors and α7 AChRs.

CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α3β4 (Ki=21 nM) as at α4β2 nAChRs (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 readily penetrates the CNS.

nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).

PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM.

PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation.

PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR).PHA 568487 reduces neuroinflammation and oxidative stress. PHA-568487 has rapid brain penetration.

S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.

(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.

Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide.

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.

Flupyrimin acts as an antagonist at the insect nicotinic acetylcholine receptor (nAChR).

nAChR modulator-2, a insecticide, is a insect nAChR orthosteric modulator.

nAChR modulator-1, a insecticide, is a insect nAChR orthosteric modulator.

AP-202 (AP202) is a highly potent and selective α4β2 nAChR antagonist with binding Ki of 18 nM, 57-fold selectivity over α3β4 receptor.AP-202 is agonist activity, also dispalys 40-fold, 10-fold and 90-fold selectivity over α4β4, α3β2, α3β4α5 receptors, does not activate α7 nAChR or block acetylcholine induced changes in membrane potential.AP-202 showed significant activity in blocking nicotine priming-induced as well as cue-induced reinstatement of nicotine seeking in vivo.

RGM079 (RGM-079) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 8.3 uM.RGM079 exhibited a balanced pharmacokinetic profile and antioxidant properties comparable or even higher than well-known natural polyphenols.RGM079 shows neuroprotective properties in Alzheimer's disease (AD)-toxicity related models.RGM079 causes a concentration-dependent neuroprotective effect against the toxicity induced by okadaic acid (OA) in the human neuroblastoma cell line SH-SY5Y.RGM079 is able to restore the cellular viability after exposure to OA and amyloid peptide Aβ1–42, with cell death almost completely prevented at 10 and 30 μM, respectively, in primary cultures of rat cortical neurons;RGM079 shows in vivo analgesic activity in the complete CFA-induced paw inflammation model after intraperitoneal administration.

RJR-2403 (Rivanicline, Metanicotine) is a potent, selective neuronal nicotinic ACh (nAChR) agonist with high affinity to rat brain cortex (Ki=26 nM), does not significantly activate muscle type nAChRs or muscarinic receptors; RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes with EC50 of 732 nM; significantly improves passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats, also demonstrates greatly reduced cardiovascular effects; exerts its antinociceptive effect via nicotinic rather than either opioid or muscarinic mechanisms.

TC-6683 (AZD1446) is a potent and highly selective α4β2 nAChR agonist with Ki of 30/34 nM against hα4β2/rα4β2, with little to no affinity against h α3β2 and h α7 (Ki>6.7 uM).TC-6683 (10 uM) produced <30% inhibition of specific binding or enzyme activity at all targets except the human (87%) and murine (97%) 5-HT3 receptors at a panel of 70 receptors, ion channels, and enzymes at NovaScreen/Caliper.TC-6683 (AZD1446) enhanced working memory in the object recognition paradigm in rats at every dose tested (0.1−3 mg/kg, po), exhibited favorable pharmaceutical properties and in vivo efficacy in animal models.

S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the treatment of aging-related memory disturbances.

Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way.

T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist.

Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist.

Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.

Pyrantel is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel can cause spasmodic muscle paralysis in parasites. Pyrantel can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis.

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.

UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [3H]-nicotine binding in rat brain.

ABT-418 hydrochloride (ABT418) is an analog of (-)-nicotine and cholinergic ligand (activator) of nAChRs, a potent inhibitor of [3H]-cytisine binding to nAChR in rat brain with Ki of 2 nM.

Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).

AN317 is a functionally selective, partial agonist of α6β2-containing nicotinic acetylcholine receptor (nAChR) with pEC50 of 7.17 (α6/α3β2β3V9'S receptor) in cell-based assays, inhibits the effect of nicotine with IC50 of 1.1 uM.

AT1001 (AT-1001) is a high affinity and selective α3β4 nAChR antagonist with Ki value of 2.4 nM, >90-fold selectivity over the other major subtypes (α4β2 and α7 nAChR).

Cris-104 is a selective α4β2* neuronal nAChR agonist, demonstrates antinociceptive and antihypersensitivity in rodent acute/inflammatory and chronic pain models.

CVN417 (CVN-417) is a potent, selective and brain-penetrant α6-containing nicotinic acetylcholine receptor (α6 nAChR) antagonist with Ca2+ flux IC50 of 86 nM.

DM506 is a novel ibogamine derivative and inhibitor of α7 and α9α10 nicotinic acetylcholine receptors (nAChRs) with IC50 of 5.1 uM, 5.6 uM and 6.4 uM for α9α10, α7β2 and α7nAChR, respectively.

JWX-A0108 is a novel selective type I α7 nAChR positive allosteric modulator (PAM) with EC50 of 4.35 uM, shows no potentiation effect on α3β4 nAChR, α4β2 nAChR, or 5-HT3AR.

MK4334 is a potent, selective positive allosteric modulator (PAM) of the α7 nAChR with potential for treatment of Alzheimer's disease.

RGH-560 (RGH560) is a potent, selective α7 nAChR positive allosteric modulator (PAM) with EC50 of 190 nM (Ca2+-influx).