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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 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

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

Johnson & Johnson
15

Approval Year

Unknown
139,594

Targets

Primary TargetPharmacologyConditionPotency
Adrenergic receptor alpha-1
169
Antagonist
2,778
 1.3 nM [Ki]
Serotonin 1a (5-HT1a) receptor
172
Antagonist
2,778
 1.7 nM [Ki]
Dopamine D2 receptor
297
Antagonist
2,778
 2.2 nM [Ki]

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
ACTIVE MOIETY
Structure of MAZAPERTINE
PARENT (SALT/SOLVATE)
Structure of SUCCINIC ACID
NIH
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