Altanserin is a compound that binds to the 5-HT 2A receptor (5-Hydroxytryptamine 2A receptor).Labeled with the isotope fluorine-18 it is used as a radioligand in positron emission tomography (PET) studies of the brain, i.e., studies of the 5-HT 2A neuroreceptors.Besides human neuroimaging studies altanserin has also been used in the study of rats. An alternative for PET imaging the 5-HT 2A.
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Nelotanserin (former developmental code name APD-125) is a drug developed by Arena Pharmaceuticals which acts as an inverse agonist on the serotonin receptor subtype 5-HT 2A and was under development for the treatment of insomnia. It was shown to be effective and well tolerated in clinical trials, but development was halted in December 2008 because the substance did not meet the trial's.
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References. References are publications that support the biological activity of the product. Herth et al (2009) Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18 F-radioligands for 5-HT 2A receptor imaging with PET. Bioorg.Med.Chem. 17 2989 PMID: 19329329 Kennett et al (1994) Evidence that 5-HT 2C receptor antagonists are anxiolytic in the rat Geller-Seifter.
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