Pharmacological onomastics: what's in a name?
Drugs are named for their primary receptor target and overt action (agonism, antagonism) but the observation of multiple or collateral efficacies emanating from drugs activating a single receptor target is posing a challenge for drug classification and nomenclature. With increasing abilities to detect alteration in cellular function has come the identification of efficacies that are not necessarily manifest in obvious changes in cell response. Specifically, some agonists selectively activate cellular pathways, demonstrate phenotypic behaviour associated with cell type and some antagonists actively induce receptor internalization without activation. In addition, the effects of allosteric modulators can be linked to the nature of the co-binding ligand posing a similar complication in classification and naming. Thus, accurate labels for this new generation of selective drugs may require identification of receptor partners (G-protein type, beta-arrestin) or pathway or, in the case of allosteric modulators, identification of co-binding ligands. The association of distinct phenotypic behaviours with molecules opens the opportunity to better associate clinical effects with distinct pharmacological properties.
Kenakin
T P
TP
Biochemical and Cellular Targets, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. Terry.P.Kenakin@gsk.com
D000494:Allosteric Regulation; D054313:Drug Agonism; D004336:Drug Antagonism; D016503:Drug Delivery Systems / Q000145:classification*; D006801:Humans; D008024:Ligands; D004364:Pharmaceutical Preparations / Q000145:classification*; D009626:Terminology as Topic
D008024:Ligands; D004364:Pharmaceutical Preparations
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