NLX-204
NLX-204 Basic information
- Product Name:
- NLX-204
- Synonyms:
-
- NLX-204
- NLX-204 HCl
- Methanone, (3-chloro-4-fluorophenyl)[4-fluoro-4-[[[2-(2-pyridinyloxy)ethyl]amino]methyl]-1-piperidinyl]-
- CAS:
- 2170405-10-2
- MF:
- C20H22ClF2N3O2
- MW:
- 409.86
- Mol File:
- 2170405-10-2.mol
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NLX-204 Chemical Properties
- Boiling point:
- 559.6±50.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- pka
- 8.88±0.20(Predicted)
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NLX-204 Usage And Synthesis
Description
NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.