Pharmacology letter accelerated communication[11C]MDL 100907, a radioligand for selective imaging of 5-HT2A receptors with positron emission tomography
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2021, Progress in Brain Research<sup>11</sup>C-labeling and preliminary evaluation of pimavanserin as a 5-HT<inf>2A</inf> receptor PET-radioligand
2015, Bioorganic and Medicinal Chemistry LettersAlterations in the serotonin system in schizophrenia: A systematic review and meta-analysis of postmortem and molecular imaging studies
2014, Neuroscience and Biobehavioral ReviewsDevelopment of novel chiral capillary electrophoresis methods for the serotonin receptor (5-HT<inf>2A</inf>) antagonist MDL 100,907 (volinanserin) and for its key intermediate compound
2014, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Its R-enantiomer binds to its receptor with higher affinity (Ki ∼ 0.4 nM) than its racemic form (Ki ∼ 2.1 nM) [2]. MDL 100,907 has about 100-fold or greater selectivity for 5-HT2A than for the other 5-HT receptor subtypes [3,4]. This drug is widely used in the investigation of the 5-HT2A receptor function [1,5–8].
Characterization of [<sup>11</sup>C]Cimbi-36 as an agonist PET radioligand for the 5-HT<inf>2A</inf> and 5-HT<inf>2C</inf> receptors in the nonhuman primate brain
2014, NeuroImageCitation Excerpt :PET studies examining 5-HT2A receptors have been conducted to evaluate the role of 5-HT2A receptors in physiology (Erritzoe et al., 2009) and neuropsychiatric disorders (Adams et al., 2005; Haugbol et al., 2007). A limitation of the available 5-HT2A receptor PET radioligands, e.g. [18F]altanserin (Biver et al., 1994; Lemaire et al., 1991) or [11C]MDL 100907 (Ito et al., 1998; Lundkvist et al., 1996), is that they are antagonists. Classical receptor binding assay studies have demonstrated that 5-HT2A receptors exist in two affinity states for agonists (Fitzgerald et al., 1999; Lopez-Gimenez et al., 2001c; Song et al., 2005), similar as for other G protein-coupled receptors.