Facinicline (MEM-63908 or R-4996) is a selective nicotinic alpha-7 receptor (α7nAChR) partial agonist. It also has properties of a serotonin 3 receptor antagonist. It has hydrochloride form: RG3487 (formerly MEM3454). Facinicline enhances DA efflux by nAChR stimulation, whereas ACh efflux is primarily mediated via 5-HT3 receptor antagonism. It improves cognition and sensorimotor gating in rodents. It has been tested in Alzheimer's disease and cognitive symptoms of schizophrenia.

Bradanicline (formerly known as ATA-101 or TC-5619), a selective full agonist for the alpha7 neuronal nicotinic receptor (NNR) subtype was developed for the treatment of central nervous system diseases and disorders. Bradanicline participated in phase II clinical trials for patients with negative and cognitive symptoms of schizophrenia; however, results did not support a benefit of the drug. The development was also discontinued for Alzheimer's disease and attention-deficit hyperactivity disorder. In addition, it was announced that the first patient had been treated in Phase 2 clinical trial in chronic cough with bradanicline. Phase 2 will test the efficacy and safety of bradanicline in up to 49 patients with refractory chronic cough. Refractory chronic cough is defined as a cough that persists for eight weeks or more. In the plans will conduct additional clinical trials to test the safety and efficacy of bradanicline.

Sabcomeline (SB-202026) is a potent and functionally selective M1 receptor partial agonist that originally was developed by GlaxoSmithKline. Sabcomeline had been in phase III clinical trials for the treatment of Alzheimer's disease and phase II for schizophrenia and major depressive disorder. In addition, it was studied for patients with Type 2 diabetes mellitus. However, due to poor results, the development of this drug was discontinued.

Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.

Milameline (previously known as RU 35926/CI-979), a partial muscarinic agonist that was developed as a cognition-enhancing agent for the treatment of patients with Alzheimer's disease. In spite of this drug has achieved phase III clinical trials, further studies were apparently discontinued.

Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.

Tazomeline (also known as LY 287041), a neuropsychiatric agent, is a muscarinic M1 acetylcholine receptor agonist that was studied in patients with cognitive dysfunction. Tazomeline participated in clinical trials for the treatment of Alzheimer’s disease and dementia. However, all these studied were discontinued for unknown reasons.

Espatropate (UK 88060) is an antagonist of M3 muscarinic receptors. Espatropate is a bronchodilator with anticholinergic activity. It was undergoing preclinical development with Pfizer for the treatment of asthma.

GTS-21 (also known as DMBX-A), a selective alpha-7 nicotinic acetylcholine receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. GTS-21 has been studied in Phase II in patients with schizophrenia and in patients with Alzheimer disease. However, these studies were discontinued. GTS-21 was also involved in phase II to reduce negative affect, improve cognition and/or reduce smoking relapse in healthy adult men and women who are chronic cigarette smokers. However, this study was withdrawn. Besides, GTS-21 has participated in phase II to investigate safety and efficacy in adults with attention-deficit hyperactivity disorder.

ISPRONICLINE is a partial agonist at the a4b2 subtype of nicotinic acetylcholine receptors (nAChRs) without interaction with other nAChRs or other receptor systems. It has antidepressant, nootropic, and neuroprotective effects. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease but is no longer under development.