Research reportFurther evidence for differential affinity states of the serotonin1A receptor in rat hippocampus
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Translating biased agonists from molecules to medications: Serotonin 5-HT<inf>1A</inf> receptor functional selectivity for CNS disorders
2022, Pharmacology and TherapeuticsCitation Excerpt :Alternatively, binding of agonist compounds to the receptor may itself induce GPCRs to couple to their interacting G proteins (Laruelle, 2000; Skinbjerg et al., 2010). As concerns 5-HT1A receptors, the above comments are important in the study of novel agonist ligands because these may differentially label the receptors depending on their G-protein coupling state (see Table 2), thus generating affinity states which may differ between the biased agonists (Aznavour et al., 2006; Emerit, el Mestikawy, Gozlan, Rouot, & Hamon, 1990; Mongeau et al., 1992; Razakarivony, Newman-Tancredi, & Zimmer, 2021; Zimmer, 2016). PET studies with radiolabeled biased agonists can therefore be informative for investigating which brain regions are targeted and the coupling state of the receptors therein.
Fast-acting antidepressant activity of ketamine: highlights on brain serotonin, glutamate, and GABA neurotransmission in preclinical studies
2019, Pharmacology and TherapeuticsSerotonin receptor imaging by <sup>18</sup>F-PET
2018, Fluorine in Life Sciences: Pharmaceuticals, Medicinal Diagnostics, and Agrochemicals Progress in Fluorine Science SeriesAgonist and antagonist bind differently to 5-HT<inf>1A</inf> receptors during Alzheimer's disease: A post-mortem study with PET radiopharmaceuticals
2016, NeuropharmacologyCitation Excerpt :An improved understanding of the functional role of 5-HT1A receptors in AD may be gained by taking into account additional aspects of their pharmacological profile. Indeed, as G-protein-coupled receptors (GPCR), they have been shown to exist in different states (Mongeau et al., 1992; Nenonene et al., 1994): a high-affinity state for agonists, (effective receptor/G-protein coupling, supposedly active), and a low affinity (G-protein uncoupled, non-functional). Contrary to an agonist, an antagonist, like [18F]MPPF used in previous PET studies, indiscriminately labels all 5-HT1A receptors, regardless of their G-protein coupling state (Gozlan et al., 1995; Burnet et al., 1997).
Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT<inf>1A/2A</inf> receptor function
2014, Neurochemistry InternationalCitation Excerpt :In Fig. 3, we estimated levels of 5-HT1A receptor by [3H]8-OH-DPAT binding. However, [3H]-8-OH-DPAT is not without limitations, since it binds with high affinity only to those 5-HT1A receptors which are G protein-coupled (Emerit et al., 1990; Hall et al., 1985; Mongeau et al., 1992; Nenonene et al., 1994). Moreover, the ligand binding does not completely discriminate between surface and intracellular receptors.