Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987. CTT2274 is composed of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and MMAE payload. CTT2274 shows selective binding to PSMA and delivers MMAE. CTT2274 inhibits prostate cancer.

Epibatidine is a α7nACh agonist with a Kd of 100 nM. Epibatidine can be used in the study of Alzheimer's, Parkinson's and schizophrenia.

Cypenamine hydrochloride is an antidepressant agent. Cypenamine binds to the human nAchR subtypes, α2β4, α3β4 and α4β4, with Ki values of 4.65 μM, 2.69 and 4.11 μM, respectively.

A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile.

(E/Z)-Acetamiprid is the E/Z mixture of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.

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

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

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.

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.

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.

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

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).

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.

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).

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.

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

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.

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.

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

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

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.

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.

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.

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.

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.

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

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.

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

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.

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.