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+
| Molecular Formula | C20H22ClF2N3O |
| Molecular Weight | 393.858 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C4H4O4 |
| Molecular Weight | 116.0722 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
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 |
|---|---|---|
| Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain. | 2003 Apr |
|
| High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury. | 2004 Aug 16 |
|
| 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 Nov |
|
| High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning. | 2006 Feb |
|
| [(3)H]-F13640, a novel, selective and high-efficacy serotonin 5-HT(1A) receptor agonist radioligand. | 2010 Oct |
|
| Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. | 2010 Oct 14 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 14:56:42 GMT 2023
by
admin
on
Sat Dec 16 14:56:42 GMT 2023
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| Record UNII |
87C9853CSK
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| Record Status |
Validated (UNII)
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| Record Version |
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208110-65-0
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87C9853CSK
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10229295
Created by
admin on Sat Dec 16 14:56:42 GMT 2023 , Edited by admin on Sat Dec 16 14:56:42 GMT 2023
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |