Abaperidone |
| رقم الكتالوجGC31055 |
Abaperidone هو مضاد قوي لمستقبلات 5-HT2A ومستقبلات الدوبامين D2 مع IC50s من 6.2 و 17 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 183849-43-6
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[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.
Kinase experiment: | 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 experiment: | 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: [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. | |
| Cas No. | 183849-43-6 | SDF | |
| Canonical SMILES | O=C1C(CO)=COC2=CC(OCCCN3CCC(C4=NOC5=C4C=CC(F)=C5)CC3)=CC=C12 | ||
| Formula | C25H25FN2O5 | M.Wt | 452.47 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2101 mL | 11.0505 mL | 22.1009 mL |
| 5 mM | 0.442 mL | 2.2101 mL | 4.4202 mL |
| 10 mM | 0.221 mL | 1.105 mL | 2.2101 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
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