Ocaperidone
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MedKoo CAT#: 329518

CAS#: 129029-23-8

Description: Ocaperidone, also known as R 79598, is a highly potent and efficacious dopamine-D2 antagonist with concomitant, equivalent serotonin 5-HT2 antagonism. Ocaperidone inhibited dopamine agonist (apomorphine, amphetamine or cocaine)-induced behavioral effects at low doses (0.014-0.042 mg/kg). Ocaperidone completely blocked the dopamine agonist behavior at slightly higher doses (0.064 mg/kg). Ocaperidone is expected to exert pronounced haloperidol-like effects on the positive symptoms of schizophrenic patients but with risperidone-like low extrapyramidal side effect liability and improved patient compliance.


Price and Availability

Size
Price

10mg
USD 150
200mg
USD 1250
5g
USD 7250
Size
Price

50mg
USD 450
500mg
USD 2150
Size
Price

100mg
USD 750
1g
USD 3250

Ocaperidone, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 100mg may be 2 months


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 329518
Name: Ocaperidone
CAS#: 129029-23-8
Chemical Formula: C24H25FN4O2
Exact Mass: 420.1962
Molecular Weight: 420.4884
Elemental Analysis: C, 68.55; H, 5.99; F, 4.52; N, 13.32; O, 7.61


Synonym: Ocaperidone; R 79598; R-79598; R79598; R 79,598; R-79,598; R79,598.

IUPAC/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

InChi Key: ZZQNEJILGNNOEP-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=C1C(CCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)=C(C)N=C5N1C=CC=C5C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Megens AA, Awouters FH, Meert TF, Schellekens KH, Niemegeers CJ, Janssen PA. Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59. PubMed PMID: 1370538.

2: Geerts H, Spiros A, Roberts P, Twyman R, Alphs L, Grace AA. Blinded prospective evaluation of computer-based mechanistic schizophrenia disease model for predicting drug response. PLoS One. 2012;7(12):e49732. doi: 10.1371/journal.pone.0049732. PubMed PMID: 23251349; PubMed Central PMCID: PMC3522663.

3: Leysen JE, Janssen PM, Gommeren W, Wynants J, Pauwels PJ, Janssen PA. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Mol Pharmacol. 1992 Mar;41(3):494-508. PubMed PMID: 1372084.

4: Megens AA, Niemegeers CJ, Awouters FH. Behavioral disinhibition and depression in amphetaminized rats: a comparison of risperidone, ocaperidone and haloperidol. J Pharmacol Exp Ther. 1992 Jan;260(1):160-7. PubMed PMID: 1370539.

5: Brys R, Josson K, Castelli MP, Jurzak M, Lijnen P, Gommeren W, Leysen JE. Reconstitution of the human 5-HT(1D) receptor-G-protein coupling: evidence for constitutive activity and multiple receptor conformations. Mol Pharmacol. 2000 Jun;57(6):1132-41. PubMed PMID: 10825383.

6: Newman-Tancredi A, Verrièle L, Touzard M, Millan MJ. Efficacy of antipsychotic agents at human 5-HT(1A) receptors determined by [3H]WAY100,635 binding affinity ratios: relationship to efficacy for G-protein activation. Eur J Pharmacol. 2001 Oct 5;428(2):177-84. PubMed PMID: 11675034.

7: Cussac D, Duqueyroix D, Newman-Tancredi A, Millan MJ. Stimulation by antipsychotic agents of mitogen-activated protein kinase (MAPK) coupled to cloned, human (h)serotonin (5-HT)(1A) receptors. Psychopharmacology (Berl). 2002 Jul;162(2):168-77. PubMed PMID: 12110994.

8: Cosi C, Koek W. Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells. Eur J Pharmacol. 2001 Dec 14;433(1):55-62. PubMed PMID: 11755134.

9: Audinot V, Newman-Tancredi A, Cussac D, Millan MJ. Inverse agonist properties of antipsychotic agents at cloned, human (h) serotonin (5-HT)(1B) and h5-HT(1D) receptors. Neuropsychopharmacology. 2001 Sep;25(3):410-22. PubMed PMID: 11522469.

10: Lesage AS, Wouters R, Van Gompel P, Heylen L, Vanhoenacker P, Haegeman G, Luyten WH, Leysen JE. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. PubMed PMID: 9605573; PubMed Central PMCID: PMC1565323.

11: Leysen JE, Gommeren W, Heylen L, Luyten WH, Van de Weyer I, Vanhoenacker P, Haegeman G, Schotte A, Van Gompel P, Wouters R, Lesage AS. Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol. 1996 Dec;50(6):1567-80. PubMed PMID: 8967979.

12: Pauwels PJ, Van Gompel P, Leysen JE. Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells. Biochem Pharmacol. 1993 Jan 26;45(2):375-83. PubMed PMID: 8382063.