Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H20FN3O4.2H2O |
Molecular Weight | 433.4302 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.FC1=CC=C(CC2CCN(CC2)C(=O)C(=O)NC3=CC4=C(NC(=O)O4)C=C3)C=C1
InChI
InChIKey=FOQSBLBAJDFAEC-UHFFFAOYSA-N
InChI=1S/C21H20FN3O4.2H2O/c22-15-3-1-13(2-4-15)11-14-7-9-25(10-8-14)20(27)19(26)23-16-5-6-17-18(12-16)29-21(28)24-17;;/h1-6,12,14H,7-11H2,(H,23,26)(H,24,28);2*1H2
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C21H20FN3O4 |
Molecular Weight | 397.3996 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.neuropathie.nu/research-development/radiprodil-fails-in-diabetic-neuropathy.htmlCurator's Comment: description was created based on several sources, including
http://ir.frx.com/phoenix.zhtml?c=83198&p=irol-newsArticle&ID=790577&highlight=
Sources: http://www.neuropathie.nu/research-development/radiprodil-fails-in-diabetic-neuropathy.html
Curator's Comment: description was created based on several sources, including
http://ir.frx.com/phoenix.zhtml?c=83198&p=irol-newsArticle&ID=790577&highlight=
RGH-896 (radiprodi) is orally active and selective NMDA NR2B antagonist, a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions. It blocks pain signaling without interacting with other NMDA receptor subtypes thus potentially improving therapeutic index and side effect profile. RGH-896 is the first of this group and is currently in early clinical development. Forest and Richter initiated a Phase IIb study in neuropathic pain in the United Stated in the second half of 2006. The drug did not produce significant reductions in patient-reported pain scores for all the dosages tested. Forest says that it and Gedeon Richter will review the findings before making a decision about the further development of radiprodil. In addition to neuropathic pain, the companies intend to investigate various other pain conditions and possibly CNS indications not related to pain. Forest will pay Richter undisclosed upfront and milestone payments in addition to royalties and will have exclusive rights in the U.S. and Canada. The two companies will jointly fund the development program. RGH-896 has patent applications that provide patent protection until at least 2022.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1904 Sources: http://etheses.dur.ac.uk/2736/ |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
89.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30705758 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
RADIPRODIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2042 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30705758 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
RADIPRODIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
15.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30705758 |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
RADIPRODIL plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:50:59 UTC 2023
by
admin
on
Fri Dec 15 15:50:59 UTC 2023
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Record UNII |
88UD2G2LYQ
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Record Status |
Validated (UNII)
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Record Version |
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1204354-40-4
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88UD2G2LYQ
Created by
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46908665
Created by
admin on Fri Dec 15 15:50:59 UTC 2023 , Edited by admin on Fri Dec 15 15:50:59 UTC 2023
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |
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