Quantitation in receptor pharmacology.
The activity of drugs on receptors can be visualized in appropriate systems. However, for comparisons of activity to be made, these effects must be quantified. The common currency for this quantitation is the dose-response curve. Thus, the shape, location (along the concentration axis), and maximal asymptote of dose-response curves are used to quantify drug activity and comparisons to mathematical models of receptors are made to describe mechanism of action. This review cites examples of where these quantitative procedure yield information beyond what is readily apparent through observation of the data and thus support the use of quantitative methods to maximize the information gained from experiments.
Kenakin
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Department of Receptor Biochemistry, GlaxoSmithKline Research and Development, 5, Moore Drive, Research Triangle Park, NC 27709, USA. tpk1348@gsk.com
D000494:Allosteric Regulation; D000682:Amyloid / Q000494:pharmacology; D000818:Animals; D002217:Carbachol / Q000494:pharmacology; D018679:Cholinergic Agonists / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D047908:Intracellular Signaling Peptides and Proteins; D058228:Islet Amyloid Polypeptide; D008565:Membrane Proteins / Q000378:metabolism; D008962:Models, Theoretical; D018727:Muscarinic Antagonists / Q000494:pharmacology; D051381:Rats; D058261:Receptor Activity-Modifying Proteins; D018003:Receptors, Calcitonin / Q000187:drug effects; D011956:Receptors, Cell Surface / Q000819:agonists / Q000037:antagonists & inhibitors / Q000187:drug effects*; D012601:Scopolamine / Q000494:pharmacology
D000682:Amyloid; D018679:Cholinergic Agonists; D047908:Intracellular Signaling Peptides and Proteins; D058228:Islet Amyloid Polypeptide; D008565:Membrane Proteins; D018727:Muscarinic Antagonists; D058261:Receptor Activity-Modifying Proteins; D018003:Receptors, Calcitonin; D011956:Receptors, Cell Surface; D002217:Carbachol; D012601:Scopolamine