ANAVEX 2-73 is an orally available drug candidate developed to potentially modify Alzheimer’s. This drug is in Phase II trials for Alzheimer's disease and Rett syndrome, phase I trials for epilepsy and in preclinical trials for multiple sclerosis and Parkinson's disease. ANAVEX 2-73 is a sigma-1 receptor agonist, which also has micromolar affinities for muscarinic M1–M4 receptors, the sodium channel site 2 and NMDAreceptors. Observed adverse events at doses above the maximum tolerated single dose (60 mg) included headache and dizziness, which were moderate in severity and reversible.

Tarafenacin (also known as SVT-40776) was developed as muscarinic M3 receptor antagonist for the treatment of overactive bladder. The drug participated in phase II clinical trial in patients suffering from overactive bladder, where both dose levels of tarafenacin were well tolerated. However, information about the further development of tarafenacin is not available.

JNJ-39393406 is a positive allosteric alpha-7 nicotinic acetylcholine receptor modulator. It was under development for the treatment of smoking cessation, schizophrenia, Alzheimer's disease, but development for these indications was discontinued.

(R)-Mequitazine or V0162 (10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine) is an anticholinergic enantiomer of mequitazine, an existing oral racemic antihistamine commercialized for over 30 years. (R)-Mequitazine was found to be an antagonist at muscarinic acetylcholine receptors behaving as an inverse agonist. (R)-Mequitazine was investigated in clinical trials for the treatment of chronic obstructive pulmonary disease, asthma and urinary incontinence.