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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
Structure of RADIPRODIL DIHYDRATE

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

HIDE SMILES / InChI

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

Description
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
89.4 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
2042 ng × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
15.8 h
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
Doses

Doses

DosePopulationAdverse events​
30 mg single, oral
Studied dose
Dose: 30 mg
Route: oral
Route: single
Dose: 30 mg
Sources: Page: p.4
healthy, ADULT
n = 10
Health Status: healthy
Age Group: ADULT
Sex: M+F
Food Status: FASTED
Population Size: 10
Sources: Page: p.4

Sample Use Guides

45 mg capsules three times a day, 14 weeks
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:50:59 UTC 2023
Edited
by admin
on Fri Dec 15 15:50:59 UTC 2023
Record UNII
88UD2G2LYQ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RADIPRODIL DIHYDRATE
Common Name English
2-[4-(4-Fluorobenzyl)piperidin-1-yl]-2-oxo-N-(2-oxo-2,3-dihydrobenzoxazol-6-yl)acetamide dihydrate
Systematic Name English
RGH-896 DIHYDRATE
Code English
1-Piperidineacetamide, N-(2,3-dihydro-2-oxo-6-benzoxazolyl)-4-[(4-fluorophenyl)methyl]-α-oxo-, hydrate (1:2)
Systematic Name English
Code System Code Type Description
CAS
1204354-40-4
Created by admin on Fri Dec 15 15:50:59 UTC 2023 , Edited by admin on Fri Dec 15 15:50:59 UTC 2023
PRIMARY
FDA UNII
88UD2G2LYQ
Created by admin on Fri Dec 15 15:50:59 UTC 2023 , Edited by admin on Fri Dec 15 15:50:59 UTC 2023
PRIMARY
PUBCHEM
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
PRIMARY
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