U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C17H23N5O2
Molecular Weight 329.3975
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SUNEPITRON

SMILES

c1cnc(nc1)N2CCN3C[C@]([H])(CC[C@@]3([H])C2)CN4C(=O)CCC4=O

InChI

InChIKey=UXWBIYCPUVWKHP-KBPBESRZSA-N
InChI=1S/C17H23N5O2/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/t13-,14-/m0/s1

HIDE SMILES / InChI

Molecular Formula C17H23N5O2
Molecular Weight 329.3975
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
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.

Approval Year

Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.02 ng/mL
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
2.36 ng × h/mL
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
0.9 h
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
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
Doses

Doses

DosePopulationAdverse events​
5 mg single, oral
Dose: 5 mg
Route: oral
Route: single
Dose: 5 mg
Sources:
healthy
n = 6
Health Status: healthy
Sex: M
Food Status: UNKNOWN
Population Size: 6
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
PubMed

PubMed

TitleDatePubMed
Metabolism and excretion of a new antianxiety drug candidate, CP-93,393, in cynomolgus monkeys: identification of the novel pyrimidine ring cleaved metabolites.
1997 Dec
Metabolism and excretion of a new anxiolytic drug candidate, CP-93, 393, in healthy male volunteers.
1998 May
Assay and purity evaluation of sunepitron hydrochloride by reversed-phase liquid chromatography using a reference standard composite.
1998 Nov
Psychopharmacology of depression in the next millennium.
1999 Jul
Patents

Sample Use Guides

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
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Sat Jun 26 02:00:40 UTC 2021
Edited
by admin
on Sat Jun 26 02:00:40 UTC 2021
Record UNII
2GT50C8U60
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SUNEPITRON
INN  
INN  
Official Name English
SUNEPITRON [INN]
Common Name English
CP 93393
Code English
CP-93,393
Code English
2,5-PYRROLIDINEDIONE, 1-(((7S,9AS)-OCTAHYDRO-2-(2-PYRIMIDINYL)-2H-PYRIDO(1,2-A)PYRAZIN-7-YL)METHYL)-
Common Name English
CP-93393
Code English
Classification Tree Code System Code
NCI_THESAURUS C47794
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
NCI_THESAURUS C29713
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
Code System Code Type Description
WIKIPEDIA
Sunepitron
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
CAS
131831-03-3
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
PUBCHEM
183092
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
FDA UNII
2GT50C8U60
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
ChEMBL
CHEMBL2111058
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
INN
7670
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
EVMPD
SUB10774MIG
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
NCI_THESAURUS
C152473
Created by admin on Sat Jun 26 02:00:40 UTC 2021 , Edited by admin on Sat Jun 26 02:00:40 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> AGONIST
SELECTIVE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> AGONIST
Related Record Type Details
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN POOR METABOLIZERS
FECAL
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
PLASMA
METABOLITE -> PARENT
IN POOR METABOLIZERS
URINE
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
FECAL
METABOLITE -> PARENT
IN POOR METABOLIZERS
URINE
METABOLITE -> PARENT
IN POOR METABOLIZERS
PLASMA
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
FECAL
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN POOR METABOLIZERS
PLASMA
METABOLITE -> PARENT
PLASMA
METABOLITE -> PARENT
IN POOR METABOLIZERS
FECAL
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
PLASMA
METABOLITE -> PARENT
IN POOR METABOLIZERS
URINE
METABOLITE -> PARENT
IN POOR METABOLIZERS
PLASMA
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
URINE
METABOLITE -> PARENT
IN EXTENSIVE METABOLIZERS
PLASMA
METABOLITE -> PARENT
IN POOR METABOLIZERS
URINE
Related Record Type Details
ACTIVE MOIETY