compositum chemicum From Wikipedia, the free encyclopedia
Cariprazinum est substantia antipsychotica, agonista dopamini partialis (D3 > D2), ad schizophreniam tractandam[1]. In senectute periculum apoplexiae cerebri auctum est. Neque valor prolactini auctus neque intervallum QT prolongatum observantur.
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Cognitores | |
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ChemSpider | 25999972 |
PubChem | 11154555 |
DrugBank | DB06016 |
Natura chemica | |
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Formula chemica | C 21H 32Cl 2N 4O |
Massa molaris | 427.411 g/mol |
Natura pharmacologica | |
Codex ATC | N05AX15 (WHO) |
Semivita biologica | 2-5 d desmethyl~: 2-3 hebd. |
Metabolismus | iecore (hepaticus): CYP3A4 |
Metaboliti | Desmethylo- Cariprazinum (DCAR) Didesmethylo-Cariprazinum (DDCAR) |
Excretio | renibus (21%), faecibus |
Ad usum therapeuticum | |
Applicatio | per os |
Ante annum 2008 grex Hungaricus societatis Richter Gedeon Nyrt. varias substantias receptoria dopamini D3 et minus D2 inhibentes investigavit[2]. Paulo post sub nomen Cariprazini pristinum RGH-188 inventum erat[3] et anno 2012 Cariprazinum praesentatum est[4].
Cariprazinum est piperazinum. Nomen chemicum (IUPAC) est 3-[4-[2-[4-(2,3-dichloro-phenyl)-piperazino-1-yl]-aethyl]-cyclohexyl]-1,1-dimethyl-urea. Massa molaris est 427.411 g/mol.
Cariprazinum est medicamentum cum virtutibus antipsychoticis et antidepressivis. Codex ATC est N05AX15 (WHO).
Cariprazinum potissime receptoria dopamini D3, paulo minus receptoria D2 obsidet[5].
Receptorium | Cariprazini affinitas ligandi, Ki (nM)[6] | Actio |
---|---|---|
dopamini D2L | 0.49 | agonista partialis |
dopamini D2S | 0.69 | agonista partialis |
dopamini D3 | 0.085 | agonista partialis |
serotonini 5-HT1A | 2.6 | agonista partialis |
serotonini 5-HT2A | 18.8 | antagonista |
serotonini 5-HT2B | 0.58 | antagonista |
serotonini 5-HT2C | 134 | agonista inversa |
serotonini 5-HT7 | 111 | antagonista |
adrenergicum α1A | 155 | antagonista |
histamini H1 | 23.2 | antagonista |
muscarinicum acetylcholini | > 1,000 | antagonista |
Tempus semivitae biologicum Cariprazini est duo dies usque ad quinque dies. Cariprazinum substratum Cytochromatis P450 CYP3A4 (minus CYP2D6) est.
Metaboliti sunt Desmethylo-Cariprazinum (DCAR) et Di-Desmethylo-Cariprazinum (DDCAR)[7]. Tempora semivitae biologica metabolitorum Cariprazino magis longiora sunt, ita Desmethylo-Cariprazino 2-3 hebdomades est.
Cytochromatis CYP3A4 ope in duo gradus primo DCAR deinde DDCAR oriuntur.
In schizophrenia Cariprazinum effectus sympatomum negativorum deminuat[8].
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