title: In vitro isolated tissue functional muscarinic receptor assays.
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.
authors.affiliation: Theravance, South San Francisco, California, USA.
authors.forename: M Teresa
authors.initials: MT
authors.lastname: Pulido-Rios
authors.forename: Tod
authors.initials: T
authors.lastname: Steinfeld
authors.forename: Scott
authors.initials: S
authors.lastname: Armstrong
authors.forename: Nikki
authors.initials: N
authors.lastname: Watson
authors.forename: Agnes
authors.initials: A
authors.lastname: Choppin
authors.forename: Richard
authors.initials: R
authors.lastname: Eglen
authors.forename: Sharath S
authors.initials: SS
authors.lastname: Hegde
mesh_terms: D000818:Animals; D001681:Biological Assay / Q000379:methods*; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D051379:Mice; D018721:Muscarinic Agonists / Q000494:pharmacology*; D018727:Muscarinic Antagonists / Q000494:pharmacology*; D009130:Muscle, Smooth / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D011976:Receptors, Muscarinic / Q000378:metabolism*
chemical_list: D008024:Ligands; D018721:Muscarinic Agonists; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic