CAS NO: | 129029-23-8 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 420.49 |
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Formula | C24H25FN4O2 |
CAS No. | 129029-23-8 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 10 mM |
Water: N/A | |
Ethanol: N/A | |
Chemical Name | 3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one |
Synonyms | Ocaperidone; R 79,598; R-79,598; R79598; R-79598; R 79598; R79,598 |
SMILES Code | O=C1C(CCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)=C(C)N=C5N1C=CC=C5C |
In Vitro | In vitro activity: Ocaperidone has high affinity for 5-HT2 and dopamine D2, with Ki values of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5HT2, a1-adrenergic, dopamine D2, histamine H1 and a2-adrenergic, respectively. Ocaperidone shows 5-HT1A receptor agonist activity, with a pEC50 and pKi of 7.60 and 8.08. Kinase Assay: The membranes are prepared from frozen HA7 cells. Cells are harvested in ice-cold Tris-HCl pH 7.4, homogenized and centrifuged at 40 000×g, 4°C for 10 min. The pellet is suspended in the same buffer and centrifuged again. After the second centrifugation, the pellet is suspended in an assay buffer consisting of pargyline (10 μM) and CaCl2 (4 mM) in Tris-HCl (50 mM, pH 7.4). Membrane protein, 0.031-0.084 mg/tube, is incubated with [3H] 8-OH-DPAT (1 nM final concentration) and Ocaperidone at seven concentrations, for 30 min, room temperature. The reaction is terminated by filtration through Whatman filters, and radioactivity is counted by liquid scintillation spectrometry. The experiments are performed in triplicate. Data are analyzed using the non-linear curve fitting program EBDA/LIGAND. Results expressed as pKi values are means of three determinations. |
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In Vivo | Ocaperidone shows a potent occupation of 5HT2 receptor via in vivo binding in the frontal cortex of rats with an ED50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D2 receptor in the striatum and the nucleus accumbens. Ocaperidone (R 79598) antagonizes dopamine D2 and 5-HT2, and shows a a partial generalization to buspirone with an ED50 of 0.163 mg/kg. |
Animal model | Rats |
Formulation & Dosage | various dosages (0.01-10 or 2.5-40 mg/kg) of caperidone dissolved in saline (injection of 1 mL of drug solution/100 g of body weight) or with saline (control) |
References | Mol Pharmacol. 1992 Mar;41(3):494-508; Eur J Pharmacol. 2001 Dec 14;433(1):55-62. |