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• W2079400921 abstract "Allosteric modulators of the serotonin (5-HT) 5-HT2C receptor (5-HT2CR) present a unique drug design strategy to augment the response to endogenous 5-HT in a site- and event-specific manner with great potential as novel central nervous system probes and therapeutics. To date, PNU-69176E is the only reported selective positive allosteric modulator for the 5-HT2CR. For the first time, an optimized synthetic route to readily access PNU-69176E (1) and its diastereomer 2 has been established in moderate to good overall yields over 10 steps starting from commercially available picolinic acid. This synthetic approach not only enables a feasible preparation of a sufficient amount of 1 for use as a reference compound for secondary pharmacological studies, but also provides an efficient synthesis of key intermediates to develop novel and simplified 5-HT2CR allosteric modulators. Compound 1 and its diastereomer 2 were functionally characterized in Chinese hamster ovary (CHO) cells stably transfected with the 5-HT2CR using an intracellular calcium (Cai2+) release assay. Compound 1 demonstrated efficacy and potency as an allosteric modulator for the 5-HT2CR with no intrinsic agonist activity. Compound 1 did not alter 5-HT-evoked Cai2+ in CHO cells stably transfected with the highly homologous 5-HT2AR. In contrast, the diastereomer 2 did not alter 5-HT-evoked Cai2+ release in 5-HT2AR-CHO or 5-HT2CR-CHO cells or exhibit intrinsic agonist activity." @default.
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• W2079400921 date "2012-04-27" @default.
• W2079400921 modified "2023-10-16" @default.
• W2079400921 title "Exploration of Synthetic Approaches and Pharmacological Evaluation of PNU-69176E and Its Stereoisomer as 5-HT_2C Receptor Allosteric Modulators" @default.
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• W2079400921 doi "https://doi.org/10.1021/cn300020x" @default.
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