MAZAPERTINE SUCCINATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C26H35N3O2.C4H6O4
Molecular Weight	539.663
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

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	No
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	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7909336 | https://adisinsight.springer.com/drugs/800002662

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

Primary Target	Pharmacology	Potency
Adrenergic receptor alpha-1 169 Target ID: CHEMBL1907610 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9622541\|https://www.ncbi.nlm.nih.gov/pubmed/7909336	Antagonist 2778	1.3 nM [Ki]
Serotonin 1a (5-HT1a) receptor 172 Target ID: CHEMBL273 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9622541\|https://www.ncbi.nlm.nih.gov/pubmed/7909336	Antagonist 2778	1.7 nM [Ki]
Dopamine D2 receptor 297 Target ID: CHEMBL339 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9622541\|https://www.ncbi.nlm.nih.gov/pubmed/7909336	Antagonist 2778	2.2 nM [Ki]

PubMed

Title	Date	PubMed

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 `Fri Dec 15 15:41:45 UTC 2023` Edited by `admin` on `Fri Dec 15 15:41:45 UTC 2023`
Record UNII	NAA0O2XC28
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MAZAPERTINE SUCCINATE

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