Description
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
Product information
CAS Number: 129029-23-8
Molecular Weight: 420.48
Formula: C24H25FN4O2
Chemical Name: 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one
Smiles: CC1N=C2C(C)=CC=CN2C(=O)C=1CCN1CCC(CC1)C1=NOC2C=C(F)C=CC=21
InChiKey: ZZQNEJILGNNOEP-UHFFFAOYSA-N
InChi: InChI=1S/C24H25FN4O2/c1-15-4-3-10-29-23(15)26-16(2)19(24(29)30)9-13-28-11-7-17(8-12-28)22-20-6-5-18(25)14-21(20)31-27-22/h3-6,10,14,17H,7-9,11-13H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 16.67 mg/mL (39.65 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Ocaperidone has high affinify at 5-HT2 and dopamine D2, with Kis 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.
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.
Products are for research use only. Not for human use.
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