Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C17H23N5O2.ClH |
| Molecular Weight | 365.858 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.O=C1CCC(=O)N1C[C@H]2CC[C@H]3CN(CCN3C2)C4=NC=CC=N4
InChI
InChIKey=HWGPYTRJVVMHGT-IODNYQNNSA-N
InChI=1S/C17H23N5O2.ClH/c23-15-4-5-16(24)22(15)11-13-2-3-14-12-21(9-8-20(14)10-13)17-18-6-1-7-19-17;/h1,6-7,13-14H,2-5,8-12H2;1H/t13-,14-;/m0./s1
| Molecular Formula | C17H23N5O2 |
| Molecular Weight | 329.3968 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/9571226Curator's Comment: Description was created based on several sources, including: http://en.pharmacodia.com/web/drug/1_8718.html
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9571226
Curator's Comment: Description was created based on several sources, including: http://en.pharmacodia.com/web/drug/1_8718.html
Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800004255 | http://en.pharmacodia.com/web/drug/1_8718.html
Curator's Comment: # Pfizer
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.02 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
10.92 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.36 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
87.33 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9571226/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
SUNEPITRON plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Psychopharmacology of depression in the next millennium. | 1999-07 |
|
| Assay and purity evaluation of sunepitron hydrochloride by reversed-phase liquid chromatography using a reference standard composite. | 1998-11 |
|
| Metabolism and excretion of a new anxiolytic drug candidate, CP-93, 393, in healthy male volunteers. | 1998-05 |
|
| Metabolism and excretion of a new antianxiety drug candidate, CP-93,393, in cynomolgus monkeys: identification of the novel pyrimidine ring cleaved metabolites. | 1997-12 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9571226
The excretion, biotransformation, and pharmacokinetics of Sunepitron (CP-93,393) were investigated in six healthy male volunteers after oral administration of a 5-mg dose of [14C]CP-93,393.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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| Record UNII |
1NYW5HLO1E
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Validated (UNII)
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C47794
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C29713
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CHEMBL2111058
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6918176
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DTXSID10869968
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1NYW5HLO1E
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300000055255
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C152474
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148408-65-5
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FF-80
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ACTIVE MOIETY |