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Details

Stereochemistry ACHIRAL
Molecular Formula C26H35N3O2.C4H6O4
Molecular Weight 539.663
Optical Activity UNSPECIFIED
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of MAZAPERTINE SUCCINATE

SMILES

OC(=O)CCC(O)=O.CC(C)OC1=C(C=CC=C1)N2CCN(CC3=CC(=CC=C3)C(=O)N4CCCCC4)CC2

InChI

InChIKey=WAHFGTZTVZRLEY-UHFFFAOYSA-N
InChI=1S/C26H35N3O2.C4H6O4/c1-21(2)31-25-12-5-4-11-24(25)28-17-15-27(16-18-28)20-22-9-8-10-23(19-22)26(30)29-13-6-3-7-14-29;5-3(6)1-2-4(7)8/h4-5,8-12,19,21H,3,6-7,13-18,20H2,1-2H3;1-2H2,(H,5,6)(H,7,8)

HIDE SMILES / InChI

Molecular Formula C4H6O4
Molecular Weight 118.088
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C26H35N3O2
Molecular Weight 421.575
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.7 nM [Ki]
1.3 nM [Ki]
2.2 nM [Ki]
PubMed

PubMed

TitleDatePubMed
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
1994 Apr 15

Sample Use Guides

In Vivo Use Guide
healthy male subjects received incremental oral doses of mazapertine (from 5 to 50 mg over 7 days; n = 10) or placebo (n = 3) in part I and single doses in parts II (20 or 30 mg or placebo) and III (40 mg or placebo) in a double-blind fashion.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Tue Oct 22 14:28:41 UTC 2019
Edited
by admin
on Tue Oct 22 14:28:41 UTC 2019
Record UNII
NAA0O2XC28
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MAZAPERTINE SUCCINATE
USAN  
USAN  
Official Name English
PIPERIDINE, 1-(3-((4-(2-(1-METHYLETHOXY)PHENYL)-1-PIPERAZINYL)METHYL)BENZOYL)-, BUTANEDIOATE (1:1)
Systematic Name English
RWJ-37796
Code English
1-(.ALPHA.-(4-(O-ISOPROPOXYPHENYL)-1-PIPERAZINYL)-M-TOLUOYL)PIPERIDINE SUCCINATE (1:1)
Common Name English
MAZAPERTINE SUCCINATE [USAN]
Common Name English
RWJ 37796
Code English
Code System Code Type Description
PUBCHEM
60819
Created by admin on Tue Oct 22 14:28:41 UTC 2019 , Edited by admin on Tue Oct 22 14:28:41 UTC 2019
PRIMARY
MESH
C086897
Created by admin on Tue Oct 22 14:28:41 UTC 2019 , Edited by admin on Tue Oct 22 14:28:41 UTC 2019
PRIMARY
CAS
134208-18-7
Created by admin on Tue Oct 22 14:28:41 UTC 2019 , Edited by admin on Tue Oct 22 14:28:41 UTC 2019
PRIMARY
ChEMBL
CHEMBL10085
Created by admin on Tue Oct 22 14:28:41 UTC 2019 , Edited by admin on Tue Oct 22 14:28:41 UTC 2019
PRIMARY
EPA CompTox
134208-18-7
Created by admin on Tue Oct 22 14:28:41 UTC 2019 , Edited by admin on Tue Oct 22 14:28:41 UTC 2019
PRIMARY
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ACTIVE MOIETY