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Details

Stereochemistry ACHIRAL
Molecular Formula C28H37ClN4O
Molecular Weight 481.073
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOCAPRAMINE

SMILES

NC(=O)C1(CCN(CCCN2C3=CC=CC=C3CCC4=C2C=C(Cl)C=C4)CC1)N5CCCCC5

InChI

InChIKey=QAZKXHSIKKNOHH-UHFFFAOYSA-N
InChI=1S/C28H37ClN4O/c29-24-12-11-23-10-9-22-7-2-3-8-25(22)33(26(23)21-24)18-6-15-31-19-13-28(14-20-31,27(30)34)32-16-4-1-5-17-32/h2-3,7-8,11-12,21H,1,4-6,9-10,13-20H2,(H2,30,34)

HIDE SMILES / InChI

Molecular Formula C28H37ClN4O
Molecular Weight 481.073
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Clocapramine is a chlorinated derivative of carpipramine. The hydrochloride has been given orally in the treatment of schizophrenia. Clocapramine is an antagonist of the Dopamine D2 and Serotonine (5-HT2) receptors. It has been implicated in at least one strange death, including a suicide. It augments the paroxetine in the panic disorder treatment.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
13.0 nM [Ki]
1.9 nM [Ki]
1.5 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CLOFEKTON

PubMed

Sample Use Guides

In Vivo Use Guide
30 to 150 mg daily in three divided doses
Route of Administration: Oral
In Vitro Use Guide
Various concentrations of clocapramine was applied to NCB20 cells and reward currents were recorded. The cells were voltage-clamped at -60 mV. The compositions of internal and external solutions were both normal. Concentration-response curves for each compound were obtained from 6 to 10 cell. The Hill coefficients of clocapramine was 0.79. The Ka values for these compounds was 1.1 uM.
Substance Class Chemical
Record UNII
6EEL1GB72K
Record Status Validated (UNII)
Record Version