Analysis of functional responses at G protein-coupled receptors: Estimation of relative affinity constants for the inactive receptor state

Journal of Pharmacology and Experimental Therapeutics

Volumn 338, Issue 2, 2011, Pages 658-670

  Ehlert, Frederick J ^a   Griffin, Michael T ^b   Suga, Hinako ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b CHAPMAN UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[4 [(3 CHLOROPHENYL)CARBAMOYLOXY] 2 BUTYNYL]TRIMETHYLAMMONIUM; ACECLIDINE; ARECOLINE; BETHANECHOL; CARBACHOL; G PROTEIN COUPLED RECEPTOR; LIGAND; MUSCARINIC AGENT; MUSCARINIC M3 RECEPTOR; OXOTREMORINE; PILOCARPINE;

ANALYTICAL PARAMETERS; ARTICLE; BINDING AFFINITY; COMPUTER SIMULATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; PRIORITY JOURNAL; PROTEIN FUNCTION; RECEPTOR BINDING;

ANIMALS; CHO CELLS; COMPUTER SIMULATION; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; GUINEA PIGS; HUMANS; MICE; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PROTEIN BINDING; RECEPTOR, MUSCARINIC M2; RECEPTOR, MUSCARINIC M3;

EID: 79960534484     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.179291     Document Type: Article

References (13)

1. Black JW and Leff P (1983) Operational models of pharmacological agonism. Proc R Soc Lond B 220:141-162. (Pubitemid 14217337)
2. Colquhoun D and Sakmann B (1985) Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate. J Physiol 369:501-557. (Pubitemid 16176889)
3. De Lean A, Stadel JM, and Lefkowitz RJ (1980) A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J Biol Chem 255:7108-7117. (Pubitemid 11232874)
4. Ehlert FJ (2000) Ternary Complex Model, in Biomedical Applications of Computer Modeling (Christopoulos A ed) pp 21-85, CRC Press, Boca Raton, FL.
5. Ehlert FJ (2008) On the analysis of ligand-directed signaling at G protein-coupled receptors. Naunyn Schmiedebergs Arch Pharmacol 377:549-577.
6. Ehlert FJ, Griffin MT, Sawyer GW, and Bailon R (1999) A simple method for estimation of agonist activity at receptor subtypes: comparison of native and cloned M3 muscarinic receptors in guinea pig ileum and transfected cells. J Pharmacol Exp Ther 289:981-992. (Pubitemid 29191257)
7. Ehlert FJ and Rathbun BE (1990) Signaling through the muscarinic receptor-adenylate cyclase system of the heart is buffered against GTP over a range of concentrations. Mol Pharmacol 38:148-158. (Pubitemid 20231497)
8. Furchgott RF (1966) The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Adv Drug Res 3:21-55.
9. Kenakin T(2011) Functional selectivity and biased receptor signaling. J Pharmacol Exp Ther 336:296-301.
10. Oldham WM and Hamm HE (2008) Heterotrimeric G protein activation by G-protein-coupled receptors. Nat Rev Mol Cell Biol 9:60-71.
11. Stephenson RP (1956) A modification of receptor theory. Br J Pharmacol 11:379-393.
12. Strange PG (2008) Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors. Br J Pharmacol 153:1353-1363.
13. 3 muscarinic receptors. Mol Pharmacol 75:381-396.