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Relationship between thresholds to convulsions induced by a benzodiazepine inverse agonist and [H-3]-L-glutamate binding in the membranes of brain regions
(Springer, 2013-04-01)
Although some studies have investigated the influence of kindling model of epilepsy on the glutamatergic neurotransmission, the relation between glutamatergic receptors and seizure susceptibility remains unclear. the present ...
Involvement of histamine H1 and H2 receptor inverse agonists in receptor's crossregulation
(Elsevier Science, 2019-03)
Histamine [2-(4-Imidazolyl)-ethylamine] modulates different biological processes, through histamine H1 and H2 receptors, and their respective blockers are widely used in treating allergic and gastric acid-related disorders. ...
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold
(American Chemical Society, 2020-09)
GHSR controls, among others, growth hormone and insulin secretion, adiposity, feeding, and glucose metabolism. Therefore, an inverse agonist ligand capable of selectively targeting GHSR and reducing its high constitutive ...
Cholestenoic acid analogues as inverse agonists of the liver X receptors
(Pergamon-Elsevier Science Ltd, 2020-05)
Liver X Receptors (LXRs) are ligand dependent transcription factors activated by oxidized cholesterol metabolites (oxysterols) that play fundamental roles in the transcriptional control of lipid metabolism, cholesterol ...
N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor
(American Chemical Society, 2018-12-13)
The ghrelin receptor or growth hormone secretagogue receptor (GHSR) is a G-protein-coupled receptor that controls growth hormone and insulin secretion, food intake, and reward-seeking behaviors. Liver-expressed antimicrobial ...
Measurement of inverse agonism in β-adrenoceptors
(Elsevier Inc, 2010-12)
Increasing numbers of compounds, previously classified as antagonists, were shown to inhibit this spontaneous or constitutive receptor activity, instead of leave it unaffected as expected for a formal antagonist. In addition, ...
Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model.
(American Society for Pharmacology and Experimental Therapeutics, 2003-08-01)
Knowing the importance for research and pharmacological uses of proper ligand classification into agonists, inverse agonists, and antagonists, the aim of this work was to study the behavior of tiotidine, a controversial ...
Similar anxiolytic-like effects following intra-amygdala infusions of benzodiazepine receptor agonist and antagonist: Evidence for the release of an endogenous benzodiazepine inverse agonist in mice exposed to elevated plus-maze test
(Elsevier B.V., 2009-04-24)
Previous studies have demonstrated that microinjections of midazolam, a benzodiazepine receptor agonist, into the amygdala produce anxiolytic-like effects in elevated plus-maze (EPM)-naive rodents. However, systemic or ...
Similar anxiolytic-like effects following intra-amygdala infusions of benzodiazepine receptor agonist and antagonist: Evidence for the release of an endogenous benzodiazepine inverse agonist in mice exposed to elevated plus-maze test
(Elsevier B.V., 2009-04-24)
Previous studies have demonstrated that microinjections of midazolam, a benzodiazepine receptor agonist, into the amygdala produce anxiolytic-like effects in elevated plus-maze (EPM)-naive rodents. However, systemic or ...