Role of partial agonism in selectivity of benzodiazepines.
In pharmacological research and education a barrier often exists between pharmacodynamics and pharmacokinetics. It is helpful to construct models in which pharmacodynamics and pharmacokinetics are linked to improve insight into the situation in vivo. Arnold Scaf presents such a model which describes the contribution of intrinsic activity to the selective anxiolytic/anticonvulsant action of fully and partially agonistic benzodiazepines. It is based on the pharmacodynamic model, presented in TiPS by Haefely et al. last year.
Scaf
A H
AH
Department of Pharmacology/Clinical Pharmacology, University of Groningen, Netherlands.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology*; D001569:Benzodiazepines; D058787:GABA-A Receptor Antagonists; D006801:Humans; D008954:Models, Biological; D010599:Pharmacokinetics; D011963:Receptors, GABA-A / Q000187:drug effects*
D014151:Anti-Anxiety Agents; D058787:GABA-A Receptor Antagonists; D011963:Receptors, GABA-A; D001569:Benzodiazepines