U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
PNU-96391A (known as OSU6162) is a weak dopamine (DA) D(2) receptor antagonist with behavioral stabilizing properties. OSU6162 seem to act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling (partial agonist on 5-HT2A receptor). OSU6162 in a phase II European clinical trial in treatment of Myalgic Encephalomyelitis/Chronic Fatigue Syndrome. One of the isomer of OSU 6162, has promise for treating Parkinson's disease, Huntington's disease and schizophrenia, but both enantiomers of OSU 6162 had dual effects on behavior, stimulating locomotor activity in 'low activity' animals and inhibiting locomotor activity in 'high activity' animals.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
447.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.245 μM
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.0178 μM
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.543 μM
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.1 μM
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2.19 μM
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.2 μM
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.372 μM
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.038 μM
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2.27 μM × h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.24 μM × h
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
6.18 μM × h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
12.53 μM × h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
14.8 μM × h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
6.87 μM × h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.69 μM × h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
0.223 μM × h
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.89 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
7.94 h
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.32 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.37 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
N-DEPROPYL-(-)-OSU 6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.66 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.39 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.33 h
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.77 h
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OSU-6162 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
45 mg 2 times / day multiple, oral (unknown)
Highest studied dose
Dose: 45 mg, 2 times / day
Route: oral
Route: multiple
Dose: 45 mg, 2 times / day
Sources:
unhealthy
n = 28
Health Status: unhealthy
Condition: multiple sclerosis
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
Other AEs: Fatigue, Headache...
Other AEs:
Fatigue (3.6%)
Headache (7.1%)
Nasopharyngitis (3.6%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fatigue 3.6%
45 mg 2 times / day multiple, oral (unknown)
Highest studied dose
Dose: 45 mg, 2 times / day
Route: oral
Route: multiple
Dose: 45 mg, 2 times / day
Sources:
unhealthy
n = 28
Health Status: unhealthy
Condition: multiple sclerosis
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
Nasopharyngitis 3.6%
45 mg 2 times / day multiple, oral (unknown)
Highest studied dose
Dose: 45 mg, 2 times / day
Route: oral
Route: multiple
Dose: 45 mg, 2 times / day
Sources:
unhealthy
n = 28
Health Status: unhealthy
Condition: multiple sclerosis
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
Headache 7.1%
45 mg 2 times / day multiple, oral (unknown)
Highest studied dose
Dose: 45 mg, 2 times / day
Route: oral
Route: multiple
Dose: 45 mg, 2 times / day
Sources:
unhealthy
n = 28
Health Status: unhealthy
Condition: multiple sclerosis
Sex: M+F
Food Status: UNKNOWN
Population Size: 28
Sources:
PubMed

PubMed

TitleDatePubMed
Coadministration of (-)-OSU6162 with l-DOPA normalizes preproenkephalin mRNA expression in the sensorimotor striatum of primates with unilateral 6-OHDA lesions.
2001 May
The Effects of (-)-OSU6162 on Chronic Fatigue in Patients With Traumatic Brain Injury: A Randomized Controlled Trial.
2017 Mar/Apr
Patents

Sample Use Guides

OSU6162 of 30-60 mg/day
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment:: To elucidate a plausible mechanism of action for both enantiomers of OSU6162, it was evaluated the intrinsic actions of (-)- and (+)-OSU6162, and a collection of other antipsychotic and antiparkinsonian agents at 5-HT2A and D2 receptors in functional assays with various degrees of receptor reserve, including cellular proliferation, phosphatidyl inositol hydrolysis, GTPγS and beta-arrestin recruitment assays. Both enantiomers of OSU6162 were medium intrinsic activity partial agonists at 5-HT2A receptors and low intrinsic activity partial agonists at D2 receptors.
Unknown
Substance Class
Concept
Record UNII
V5SBJBUJW6
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OSU-6162 HYDROCHLORIDE
Code English
PIPERIDINE, 3-(3-(METHYLSULFONYL)PHENYL)-1-PROPYL-, HYDROCHLORIDE, (S)-
Systematic Name English
3-(3-METHANESULFONYL-PHENYL)-1-PROPYL-PIPERIDINE HYDROCHLORIDE
Common Name English
Classification Tree Code System Code
EU-Orphan Drug 3-(3-Methanesulfonyl-phenyl)-1-propyl-piperidine hydrochloride
Created by admin on Sat Jun 26 09:04:22 UTC 2021 , Edited by admin on Sat Jun 26 09:04:22 UTC 2021
Code System Code Type Description
FDA UNII
V5SBJBUJW6
Created by admin on Sat Jun 26 09:04:22 UTC 2021 , Edited by admin on Sat Jun 26 09:04:22 UTC 2021
PRIMARY
CAS
156907-84-5
Created by admin on Sat Jun 26 09:04:22 UTC 2021 , Edited by admin on Sat Jun 26 09:04:22 UTC 2021
PRIMARY
EVMPD
SUB193816
Created by admin on Sat Jun 26 09:04:22 UTC 2021 , Edited by admin on Sat Jun 26 09:04:22 UTC 2021
PRIMARY
PUBCHEM
9836644
Created by admin on Sat Jun 26 09:04:22 UTC 2021 , Edited by admin on Sat Jun 26 09:04:22 UTC 2021
PRIMARY
This is a non-substance concept
Related Record Type Details
PARENT -> SALT/SOLVATE
This is a non-substance concept