Clocapramine
Clocapramine Basic information
- Product Name:
- Clocapramine
- Synonyms:
-
- 3-chlorocarpipramine
- 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
- 28058-62-0 (Di-hydrochloride)
- 65016-29-7 (Di-hydrochloride monohydrate)
- Clocapramina
- Clocapramina [inn-spanish]
- Clocapraminum
- CAS:
- 47739-98-0
- MF:
- C28H37ClN4O
- MW:
- 481.07
- Mol File:
- 47739-98-0.mol
Clocapramine Chemical Properties
- 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)
Clocapramine Usage And Synthesis
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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