nAChR agonist 1 is a novel positive allosteric modulator of α7 nAChR. It has shown excellent safety profile in phase 1 clinical trials and is being evaluated for efficacy and safety as monotherapy in patients with mild to moderate Alzheimer’s disease.

EVP-6124 is a partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs) and shows selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.

N-Methylcytisine's nicotinic receptors have high affinity (KD = 50 nM)to nAChR from squid optical ganglia.

Biperiden HCl is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.

ABT 089 dihydrochloride is the high affinity and selective partial agonist of α4β2 with Ki of 16 nM.

Adiphenine HCl is a nicotinic receptor inhibitor with IC50 of 15 μM, used as an antispasmodic drug.

Arecaidine but-2-ynyl ester tosylate is a potent muscarinic agonist that shows 4.6-fold that is selectivity for mAChR M2 in the atrium versus those in the ileum.

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR.

Mepenzolate bromide mAchR antagonist, working as a post-ganglionic parasympathetic inhibitor to decrease gastric acid and pepsin secretion and suppresse spontaneous contractions of the colon.

Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.

Catharanthine showed muscarinic antagonism at 10 μM and fully inhibited nicotinic receptor mediated diaphragm contractions with an IC50 of 59.6 μM. As a precursor of the anti-tumor drugs vinblastine and vincristine, it also works as an inhibitor of tubulin self-assembly into microtubules.

Cisatracurium besylate is an antagonize of AchR and inhibits neuromuscular transmission, a nondepolarizing skeletal muscle relaxant.

Nitenpyram is a nAchR agonist, used an antiparasitic drug.

Vecuronium bromide is a competitive AchR inhibitor and binds to cholinergic receptors at neuromuscular junctions, used as an aminosteroidal neuromuscular blocking agent.

Solifenacin succinate is a muscarinic receptor antagonist. Solifenacin succinate is a competitive and selective M3 receptor antagonist with elimination half-life‎ of 45 to 68 hours.

Rivastigmine tartrate is an AchR inhibitor use for treatment of mild to moderate Alzheimer's disease and Parkinson's disease with elimination half-life of ‎1.5 hours.

Dinotefuran is the third generation of neonicotinoid group,which works through inhibiting nAchRs.