ABAPERIDONE
ABAPERIDONE Basic information
- Product Name:
- ABAPERIDONE
- Synonyms:
-
- ABAPERIDONE
- 4H-1-Benzopyran-4-one, 7-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-(hydroxymethyl)-
- CAS:
- 183849-43-6
- MF:
- C25H25FN2O5
- MW:
- 452.47
- Mol File:
- 183849-43-6.mol
ABAPERIDONE Chemical Properties
- 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)
ABAPERIDONE Usage And Synthesis
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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