| Identification | Back Directory | [Name]
Clocapramine | [CAS]
47739-98-0 | [Synonyms]
Clocapramina
Clocapraminum
Clocarpramine
3-chlorocarpipramine
Clocapraminum [inn-latin]
Clocapramina [inn-spanish]
28058-62-0 (Di-hydrochloride)
65016-29-7 (Di-hydrochloride monohydrate)
1'-[3-(3-Chloro-10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl][1,4'-bipiperidine]-4'-carboxamide
1-[3-(3-Chloro-10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]-4-piperidino-4-piperidinecarboxamide
[1,4'-Bipiperidine]-4'-carboxamide, 1'-[3-(3-chloro-10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]- | [Molecular Formula]
C28H37ClN4O | [MDL Number]
MFCD00867742 | [MOL File]
47739-98-0.mol | [Molecular Weight]
481.07 |
| Chemical Properties | Back Directory | [Boiling point ]
662.1±55.0 °C(Predicted) | [density ]
1.23 g/cm3 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
16.20±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
Clocapramine is an antagonist of the D2, 5-HT2A receptors. | [Definition]
ChEBI: Clocapramine is a dibenzooxazepine. | [in vivo]
Clocapramine shows the lowest potency for D2-occupancy in vivo[1]. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2)[2]. | [IC 50]
D2 Receptor; 5-HT2A Receptor | [References]
[1] Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. DOI:10.1254/jjp.69.399
[2] Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64. DOI:10.1038/sj.npp.1380239 |
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