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F-15,599, also known as NLX-101, is a very potent and highly selective 5-HT1A receptor full agonist. It displays functional selectivity (also known as "biased agonism") by strongly activating 5-HT1A receptors in the postsynaptic prefrontal cortex while having little effect on somatodendritic autoreceptors in the raphe nucleus.〔〔 As a result, it has been touted as a preferential postsynaptic 5-HT1A receptor agonist and has been investigated as a novel potential antidepressant.〔〔 In cognitive tests in rodent, F-15,599 attenuates memory deficits elicited by the NMDA receptor antagonist PCP, suggesting that it may improve cognitive function in disorders such as schizophrenia. A subsequent study showed that F-15,599 reduces breathing irregularity and apneas observed in mice with mutations of the MeCP2 gene. Dysruption of MeCP2 gene expression underlies Rett syndrome, a debilitating neurodevelopmental orphan disease. F-15,599 was discovered and initially developed by Pierre Fabre Médicament, a French pharmaceuticals company. In September 2013, F-15,599 was out-licensed to Neurolixis, a California-based biotechnology company. Neurolixis announced that it intends to re-purpose F-15,599 for the treatment of Rett syndrome.〔http://neurolixis.com/images/stories/nlx_pf_license_23sept13.pdf〕 and obtained Orphan Drug designation from the United States Food and Drug Administration (FDA)〔http://www.accessdata.fda.gov/scripts/opdlisting/oopd/OOPD_Results_2.cfm?Index_Number=410613〕 and from the European Commission for this indication.〔http://ec.europa.eu/health/documents/community-register/html/o1242.htm〕 Researchers at the University of Bristol are investigating the activity of F-15599 in animal models of Rett Syndrome, with support from the International Rett Syndrome Foundation.〔http://www.bristol.ac.uk/news/2014/april/rett-syndrome-research.html〕 In June 2015, the Rett Syndrome Research Trust awarded a grant to ] to advance F-15599 to clinical development.〔https://rettsyndrome.wordpress.com/2015/06/24/rsrt-awards-530000-to-neurolixis-for-clinical-development-of-nlx-101/〕 == See also == * Befiradol (F-13,640) * Eptapirone (F-11,440) 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「F-15,599」の詳細全文を読む スポンサード リンク
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