Functional Selectivity and Classical Concepts of Quantitative Pharmacology

By J. Urban, W. Clarke, M. von Zastrow, David E. Nichols, Brian K. Kobilka, H. Weinstein, J. Javitch, Bryan L. Roth, Arthur Christopoulos, P. Sexton and 3 more. Journal of Pharmacology and Experimental Therapeutics, 2007

1,147 citations recorded by the source corpus.

Subfields: Cellular and Molecular Neuroscience, Molecular Biology, Pharmacology

View Paper: https://www.semanticscholar.org/paper/0960fd339d0a866a157c1648728146cc11f4eee1

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In Cellular and Molecular Neuroscience

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Citations in the corpus

Activation mechanism of the β2-adrenergic receptor (2011, background): “Although the number of functionally distinct states and their conformations remain unknown, some are thought to be intermediates along the activation pathway (7, 9).”
Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders (2009, background): “The ability of different ligands to induce unique GPCR conformational states that activate a discrete subset of the possible cellular behaviours that are linked to that GPCR has been termed ' stimulus-trafficking ', 'biased agonism' or 'functional selectivity”
Psychedelics (2016, methodology): “Viswanathan and Freeman (2007) used a dual microelectrode arrangement to make simultaneous colocalized extracellular measurements of tissue oxygen and neural activity in the cortex of the cat primary visual cortex to determine whether the BOLD signal reflected mainly neuronal input (synaptic activit”
CB2: a cannabinoid receptor with an identity crisis (2010, background): “It also important to bear in mind that selective agonists and antagonists for a particular receptor may differentially alter coupling to distinct signalling pathways, a concept known as functional selectivity (Urban et al., 2007).”
GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current (2008, background): “The inability of these latter compounds to increase intracellular calcium may be due to a difference between stably versus transiently transfected cells or to a functional selectivity (25) of different GPR55 agonists.”
Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors (2011, background): “Consistent with this view, agonists are considered to have linear efficacy (24, 25), as predicted by receptor occupancy theory that identifies a receptor as existing in either an inactive or an active conformation (26, 27).”