| Stereochemistry | ACHIRAL |
| Molecular Formula | C24H25FN4O2 |
| Molecular Weight | 420.4793 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CN2C(=O)C(CCN3CCC(CC3)C4=NOC5=C4C=CC(F)=C5)=C(C)N=C12
InChI
InChIKey=ZZQNEJILGNNOEP-UHFFFAOYSA-N
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
Ocaperidone [R 79598] is an equipotent antagonist of central dopamine D2 and serotonin2 receptors being investigated as a potential antipsychotic agent. Ocaperidone is a benzisoxazol piperidine antipsychotic primarily binds and with high affinity to 5-HT2 (serotonin) receptors, alpha1 and alpha 2 adrenergic receptors, dopamine D2 receptors and histamine H1 receptors. Ocaperidone is an antagonist primarily at the 5HT and D2 receptors. A proposed mechanism of action is the central D2 receptor blockade which is common to all neuroleptics that are used to treat positive symptoms of schizophrenia.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 9.52 null [pKi] | |||
| 7.55 null [pKi] | |||
| 8.43 null [pKi] |
PubMed
Sample Use Guides
Ocaperidone was studied at various time intervals after s.c. (10 ml/kg for rats and 0.5 ml/kg for
dogs), oral (10 ml/kg for mice and rats and 0.5 ml/kg for dogs) or i.v. administration (10 ml/kg for mice, 2 ml/kg for rats and 0.5 ml/kg for dogs).
Route of Administration:
Other
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.
ACTIVE MOIETY
