| Identification | Back Directory | [Name]
ABAPERIDONE | [CAS]
183849-43-6 | [Synonyms]
ABAPERIDONE
4H-1-Benzopyran-4-one, 7-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-(hydroxymethyl)- | [Molecular Formula]
C25H25FN2O5 | [MDL Number]
MFCD00951995 | [MOL File]
183849-43-6.mol | [Molecular Weight]
452.47 |
| Chemical Properties | Back Directory | [Boiling point ]
667.3±55.0 °C(Predicted) | [density ]
1.320±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
13.48±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM. | [in vivo]
The time course of the inhibition of climbing behavior for a period of several hours after oral administration of either 0.5 mg/kg of Abaperidone or risperidone is tested in mice. Also is included a comparative test of catalepsy induced by Abaperidone and risperidone along several hours following oral administration at several doses in rats. A somewhat lesser induction of catalepsy is observed for Abaperidone. A study of serum prolactin levels after oral administration of Abaperidone, haloperidol, and risperidone at 5 mg/kg for either 1 or 3 days in rats. Increases in prolactin levels after oral administration of Abaperidone are smaller than those for reference drugs[1]. | [IC 50]
D2 Receptor: 17 nM (IC50); 5-HT2A Receptor: 6.2 nM (IC50) | [References]
[1] Bolós J, et al. 7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). J Med Chem. 1998 Dec 31;41(27):5402-9. DOI:10.1021/jm9810396 |
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LGM Pharma
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BOC Sciences
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MedChemExpress
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