Alzheimer's disease (AD) is marked by deficits in learning and memory, as well as thinking and reasoning skills, and is the leading cause of dementia and aged-related cognitive decline. Acetylcholine is essential for facilitating the process of learning and memory and its activity is known to be reduced in AD. Previous drugs that enhance cholinergic transmission, such as acetylcholinesterase (AChE) inhibitors, provide modest improvements in cognitive function in patients suffering from AD and other age-related cognitive decline. However, their effectiveness is limited by dose-limiting side-effects that result from activity at unwanted targets. New research reveals that compounds that increase the activity of a receptor in the brain called muscarinic acetylcholine subtype 1 (M1) have exciting potential to treat the cognitive deficits associated with AD and age-related dementia. The Vanderbilt Center for Neuroscience Drug Discovery has recently discovered novel compounds that selectively activate M1 and enhance cognition in multiple preclinical studies, while avoiding undesirable side effects. Currently, our studies focus on determining the preclinical safety profile of our lead compound and perform the necessary safety assessment to advance to clinical trials.