F-15,599

F-15,599

Clinical data
Routes of administration	Oral
Legal status
Legal status	In general: uncontrolled
Identifiers
IUPAC name 3-chloro-4-fluorophenyl-[4-fluoro-4-[[(5-methylpyrimidin-2-ylmethyl)amino]methyl]piperidin-1-yl]methanone
PubChem CID	11741361
IUPHAR/BPS	3924
ChemSpider	9916065 N
Chemical and physical data
Formula	C19H22ClF2N4O
Molar mass	395.854 g/mol
3D model (Jmol)	Interactive image
SMILES Cc3cnc(nc3)CNCC(F)(CC2)CCN2C(=O)c(cc1Cl)ccc1F
InChI InChI=1S/C19H21ClF2N4O/c1-13-9-24-17(25-10-13)11-23-12-19(22)4-6-26(7-5-19)18(27)14-2-3-16(21)15(20)8-14/h2-3,8-10,23H,4-7,11-12H2,1H3 N Key:WAAXKNFGOFTGLP-UHFFFAOYSA-N N
NY (what is this?)

F-15,599, also known as NLX-101, is a very potent and highly selective 5-HT_1A receptor full agonist. It displays functional selectivity (also known as "biased agonism") by strongly activating 5-HT_1A 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-HT_1A 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. and obtained Orphan Drug designation from the United States Food and Drug Administration (FDA) and from the European Commission for this indication.