Pharmacological receptor theory is discussed with special reference to advances made
during the past 25 years. Thus, the operational model has supplanted analysis of drug–receptor …

With the emergence of information describing functional selectivity and biased agonists and
antagonists has come a lack of confidence in “one size fits all” assays for detection of …

G protein-coupled receptors (GPCRs) represent the largest family of cell-surface receptors.
These receptors are natural allosteric proteins because agonist-mediated signaling by …

Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors (GPCRs),
do not uniformly activate all cellular signalling pathways linked to a given seven-…

Activation of seven-transmembrane (7TM) receptors by agonists does not always lead to
uniform activation of all signaling pathways mediated by a given receptor. Relative to other …

The neuromodulator melatonin synchronizes circadian rhythms and related physiological
functions through the actions of two G-protein-coupled receptors: MT 1 and MT 2 . Circadian …

Early work in pharmacology characterized the interaction of receptors and ligands in terms
of two parameters, affinity and efficacy, an approach we term the bipartite view. A precise …

… This latter scheme is referred to as agonist-receptor trafficking, and is discussed in this,
the second of two articles by Terry Kenakin. One way to approach these questions is to study …

The recommendations that follow have been updated from the proposals of a Technical
Subcommittee set up by the International Union of Pharmacology Committee on Receptor …

It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able
to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …