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Details

Stereochemistry ACHIRAL
Molecular Formula C28H37ClN4O.2ClH
Molecular Weight 553.994
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOCAPRAMINE DIHYDROCHLORIDE ANHYDROUS

SMILES

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

InChI

InChIKey=UUTRFZNTTSPNOY-UHFFFAOYSA-N
InChI=1S/C28H37ClN4O.2ClH/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);2*1H

HIDE SMILES / InChI

Description
Curator's Comment: description was created based on several sources, including: http://www.kegg.jp/medicus-bin/japic_med_product?id=00048317-003 | http://en.pharmacodia.com/web/drug/1_10640.html

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.

Approval Year

Targets

Targets

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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CLOFEKTON

Approved Use

Clofekton 10% is indicated for the treatment of schizophrenia.

Launch Date

1974
PubMed

PubMed

TitleDatePubMed
A crossover study of clocapramine and haloperidol in chronic schizophrenia.
1985
Patents

Sample Use Guides

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.
Name Type Language
CLOCAPRAMINE DIHYDROCHLORIDE ANHYDROUS
Common Name English
Clocapramine hydrochloride [WHO-DD]
Common Name English
CLOCAPRAMINE HYDROCHLORIDE ANHYDROUS
Common Name English
(1,4'-BIPIPERIDINE)-4'-CARBOXAMIDE, 1'-(3-(3-CHLORO-10,11-DIHYDRO-5H-DIBENZ(B,F)AZEPIN-5-YL)PROPYL)-, HYDROCHLORIDE (1:2)
Systematic Name English
CLOCAPRAMINE DIHYDROCHLORIDE [MI]
Common Name English
3-CHLORO-5-(3-(4-PIPERIDINO-4-CARBAMOYLPIPERIDINO)PROPYL)-10,11-DIHYDRO-5H-DIBENZ(B,F)AZEPINE DIHYDROCHLORIDE
Systematic Name English
Code System Code Type Description
CAS
28058-62-0
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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SMS_ID
100000087950
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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PUBCHEM
34129
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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ECHA (EC/EINECS)
248-805-8
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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EPA CompTox
DTXSID20950770
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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FDA UNII
K7UMH49J6Q
Created by admin on Sat Dec 16 05:42:46 GMT 2023 , Edited by admin on Sat Dec 16 05:42:46 GMT 2023
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