AI Article Synopsis
- Muscarinic receptor (mAChRs) subtypes are important targets for creating new drugs to treat various health disorders.
- These drugs can be better developed through in vitro functional assays that help evaluate how well different ligands bind and affect these receptors.
- The described methods focus on measuring ligand interactions with specific mAChR subtypes (M(1) to M(5)) using organ bath techniques in tissues that naturally express these receptors.
Article Abstract
Muscarinic receptor (mAChRs) subtypes are viable targets for the design of novel agents for use in a number of central and peripheral disorders. In vitro isolated tissue functional assays for muscarinic receptor subtypes have played an invaluable role in basic research and drug discovery. The availability of biological assays for generation of quantitative estimates of affinity and potency of ligands allows evaluation of the contribution of a given mAChR to the functional end organ response and also enables drug discovery by facilitating the iterative process of screening and optimization of chemical leads. This unit describes isolated tissue functional assays for the quantification of ligand affinity and efficacy at the M(1), M(2), M(3), M(4), and M(5) muscarinic receptor subtypes in tissues expressing the native receptor using organ bath techniques.
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| http://dx.doi.org/10.1002/0471141755.ph0415s48 | DOI Listing |
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