Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H22ClF2N3O.C4H4O4 |
| Molecular Weight | 509.93 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.CC1=CC=C(CNCC2(F)CCN(CC2)C(=O)C3=CC=C(F)C(Cl)=C3)N=C1
InChI
InChIKey=HCRQBLXXJOROBP-WLHGVMLRSA-N
InChI=1S/C20H22ClF2N3O.C4H4O4/c1-14-2-4-16(25-11-14)12-24-13-20(23)6-8-26(9-7-20)19(27)15-3-5-18(22)17(21)10-15;5-3(6)1-2-4(7)8/h2-5,10-11,24H,6-9,12-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
Befiradol (also known as NLX-112) was initially developed by Pierre Fabre as a selective serotonin-1A receptor agonist for the treatment of cancer pain and neuropathic pain. However, these trials were discontinued. In 2013, the development and commercialization rights were licensed to Neurolixis. Neurolixis studied befiradol in Parkinson’s disease (PD) patients that exhibit dyskinesia. Dyskinesia is a side effect that appears after several years of action Levodopa, a drug that remains the gold standard treatment for PD. In 2019, FDA gave a positive response to Neurolixis’s befiradol to be tested in Phase 2 clinical in Parkinson's disease patients suffering from debilitating levodopa-induced dyskinesia.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. | 2010-10-14 |
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| [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. | 2010-10 |
|
| High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning. | 2006-02 |
|
| Conformational analysis and crystal structure of {[1-(3-chloro-4-fluorobenzoyl)-4-fluoropiperidin-4yl]methyl}[(5-methylpyridin-2-yl)methyl]amine, fumaric acid salt. | 2005-11 |
|
| High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury. | 2004-08-16 |
|
| Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640. | 2003-04-18 |
|
| Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain. | 2003-04 |
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100000183125
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208110-65-0
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87C9853CSK
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10229295
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ACTIVE MOIETY
SUBSTANCE RECORD
