Trends in Pharmacological Sciences
Volume 13, 1992, Pages 376-380
PrinciplesReverse intrinsic activity of antagonists on G protein-coupled receptors
References (24)
Prog. Neurobiol.
(1988)- et al.
Biochim. Biophys. Acta
(1990) - et al.
Eur. J. Pharmacol.
(1981) - et al.
Eur. J. Pharmacol. Mol. Pharmacol.
225
(1992) - et al.
Eur. J. Pharmacol.
(1989) - et al.
Science
(1982) - et al.
FASEB J.
(1989) - et al.
Physiol. Rev.
(1984) - et al.
- et al.
J. Cyclic. Nucleotide Res.
(1981)
J. Cyclic. Nucleotide Res.
(1985)
Cited by (152)
Dual expression of constitutively active Gα<inf>s</inf>-protein-coupled receptors differentially establishes the resting activity of the cAMP-gated HCN2 channel in a single compartment
2017, Biochemical and Biophysical Research CommunicationsCitation Excerpt :At each subcellular location, HCN channels have versatile functions, such as regulating membrane impedance [6], setting the membrane potential [7] or sensing changes in the extracellular environment [8]. Interestingly, some GPCRs show constitutive activation in the absence of ligands [8–15]. The ligand-independent spontaneous activation of GPCRs has been reported for various receptors, such as opioid receptors [16], acetylcholine receptors [17,18], serotonin receptors [19,20], bradykinin receptors [21], adrenergic receptors [12,22–26], histamine H3 receptors [27], odorant receptors (ORs) [28,29], and dopamine receptors [30].
Historical review: Negative efficacy and the constitutive activity of G-protein-coupled receptors
2005, Trends in Pharmacological SciencesDifferent mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists
2003, International Congress SeriesThe Transition from Agonist to Antagonist Activity. Symmetry and other Considerations.
2003, The Practice of Medicinal Chemistry: Second Edition
Copyright © 1992 Published by Elsevier Ltd.