183849-43-6
183849-43-6 structure
- Name: Abaperidone
- Chemical Name: 7-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-(hydroxymethyl)chromen-4-one
- CAS Number: 183849-43-6
- Molecular Formula: C25H25FN2O5
- Molecular Weight: 452.47500
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2016-11-21 10:33:15
- Modify Date: 2024-01-03 15:53:13
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Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
| Name | 7-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-(hydroxymethyl)chromen-4-one |
|---|---|
| Synonyms |
Abaperidone [INN]
7-[3-[4-(6-fluoro-1,2-benzisoxazole-3-yl)piperidin-1-yl]propoxy]-3-(hydroxymethyl)-chromen-4-one 7-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-(-hydroxymethyl)-4H-1-benzopyran-4-one 7-[3-[4-(6-fluorobenzo[d]isoxazole-3-yl)piperidin-1-yl]propoxy]-3-(hydroxymethyl)-chromen-4-one Abaperidone |
| Description | Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 17 nM (D2 receptor), 6.2 nM (5-HT2A receptor)[1] |
| In Vitro | Abaperidone possesses good affinity for dopamine D2 receptors, together with a greater affinity for 5-HT2 receptors with IC50 of 17 and 6.2 nM, reaspectively[1]. |
| 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]. |
| Kinase Assay | Receptor binding assays are performed by inhibition of radioligand binding according to reported procedures for D1, D2, D3, D4, 15a5-HT1A, 5-HT2A, α1, α2, β, muscarinic, and σ receptors. IC50 values are calculated from concentration−response curves at 11 different concentrations of the test compound, each done in duplicate[1]. |
| Animal Admin | Rats[1] Sprague-Dawley rats (220-240 g) are assigned to 8 groups of 5 animals each, and are orally dosed with either Abaperidone (5 mg/kg/day), Haloperidol (5 mg/kg/day), Risperidone (5 mg/kg/day), or the vehicle for 1 or 3 consecutive days. The animals are killed by decapitation 3 h after last dosing, blood samples of 2 mL are collected, and prolactin levels are determined by means of an EIA kit from Amersham. |
| References |
| Density | 1.32g/cm3 |
|---|---|
| Boiling Point | 667.3ºC at 760mmHg |
| Molecular Formula | C25H25FN2O5 |
| Molecular Weight | 452.47500 |
| Flash Point | 357.4ºC |
| Exact Mass | 452.17500 |
| PSA | 88.94000 |
| LogP | 4.15200 |
| Vapour Pressure | 1.02E-18mmHg at 25°C |
| Index of Refraction | 1.612 |
| Storage condition | 2-8℃ |