Assay Method Information

Assay Name:  Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Activity against Muscarinic Panel
Description:  Assay Provider: P. Jeffrey Conn Assay Provider Affiliation: Vanderbilt University Grant Title: Discovery of novel allosteric modulators of the M1 muscarinic receptor Grant Number: 1 R03 MH077606-01 The M1 muscarinic receptor is thought to be an important therapeutic target in schizophrenia. A cell-based fluorometric calcium assay was developed for high throughput screening. This assay was used to identify compounds with high selectivity for the M1 receptor subtype that act at an allosteric site on the receptor, thus providing increased specificity for this single receptor subtype. It is anticipated that these compounds will provide important tools for the study of muscarinic receptor function in the CNS. Agents that enhance cholinergic transmission or activate muscarinic acetylcholine receptors (mAChRs) have been developed to ameliorate the loss of cognitive function in patients with Alzheimer's Disease (AD). While cholinergic agents have been partially successful in improving c
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