Esoxybutynin is (S)-enantiomer of oxybutynin. Esoxybutynin exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.

AVL-3288 is a type I selective positive allosteric modulator of α7 nACHRs. It represents a "first-in-class" drug for the treatment of cognitive deficits in CNS disorders such as schizophrenia and potentially other diseases of cognitive impairment such as Alzheimer’s disease and ADHD. AVL-3288 was successfully tested in representative animal models of cognitive dysfunction in schizophrenia, a disease where α7 nAChR function is impaired. To date, no specific treatments for cognitive deficits in schizophrenia exist and approved therapies do not satisfactorily improve cognition. AVL-3288 is currently in human phase I trials.

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.

Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Anisodamine is a non-specific cholinergic antagonist. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Anisodamine has been employed therapeutically since 1965 in the People’s Republic of China primarily to improve blood flow in circulatory disorders such as septic shock, disseminated intravascular coagulation (DIC) and as an antidote to organophosphate poisoning.

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.