The measurement of efficacy in the drug discovery agonist selection process

Journal of Pharmacological and Toxicological Methods

Volumn 42, Issue 4, 1999, Pages 177-187

  Kenakin, Terry ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBACHOL; DRUG; OXOTREMORINE; RECEPTOR;

DRUG DESIGN; DRUG DEVELOPMENT; DRUG RECEPTOR BINDING; DRUG RESEARCH; HUMAN; RECEPTOR OCCUPANCY; SHORT SURVEY;

EID: 0033303377     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(00)00070-8     Document Type: Article

References (15)

1. Operational models of pharmacological agonists
2. General pharmacology
3. The elusive nature of intrinsic efficacy
4. Imprecision in presentation of binding studies
5. Affinity, efficacy, and receptor classification; is the classical theory still useful?
6. The use of β-haloalkylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes
7. Efficacy in drug-receptor theory; outdated concept or under-valued tool?
8. Is prenalterol (H133/80) really a selective beta-1 adrenoceptor agonist? Tissue selectivity resulting from differences in stimulus-response relationships
9. 2-adrenergic receptor; extending the ternary complex model
10. A modification of receptor theory
11. The cubic ternary complex receptor-occupancy model I; model description
12. The cubic ternary complex receptor-occupancy model II; understanding apparent affinity
13. The cubic ternary complex receptor-occupancy model III; resurrecting efficacy