Talaaga

O le Ticagrelor o se faʻalavelave fou o le P2Y12 receptor [1].

Ticagrelor ua lipotia mai e taofia ai le prothrombotic aafiaga o le ADP i luga o le platelet e faasaga i le P2Y12 receptor. Ua faʻaalia e Ticagrelor le faʻatapulaʻaina atoa o le platelet aggregation ex vivo. E le gata i lea, ua fautuaina e Ticagrelor se faʻalavelave faʻalagolago i le faʻaogaina o platelet i le tagata. E ese mai i nei mea, ua faʻaalia foʻi e Ticagrelor se tuʻufaʻatasiga tautala, malosi, toe faʻafeiloaʻi. E le pei o isi inhibitors, ua lipotia mai foi e Ticagrelor e taofia le P2Y12 receptor e aunoa ma le suiga o le metabolic. E le gata i lea, o Ticagrelor o le muamua thienopyridine anti-platelet agent ma e masani ona faʻaogaina e CYP3A4 ma CYP2C19 [1] [2].

Fa'asinomaga:
[1] Zhou D1, Anderson TB, Grimm SW. Iloiloga in vitro e mafai ona fegalegaleai fualaau faasaina ma le ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Fualaau Metab Dispos. 2011 Ape;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Le faʻaogaina ma le metabolism o le ticagrelor, o se tala fou P2Y12 antagonist, i isumu, isumu, ma marmosets. Fualaau Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Iuni 13.

Fa'amatalaga

Ticagrelor (AZD6140) o se faʻalavelave faʻafeiloaʻi tautala P2Y12 mo le togafitiga o le faʻapipiʻiina o platelet.

I Vitro

Ticagrelor faʻamalosia se faʻalavelave sili atu o le adenosine 5'-diphosphate (ADP)–fa'aosoina le fa'asa'olotoina o le Ca2+ i platelets fa'afefeteina ma isi fa'afeagai P2Y12R. O lenei aafiaga faaopoopo o le ticagrelor i tua atu o le P2Y12R antagonism o se vaega o se taunuuga o le ticagrelor e taofia ai le faʻaogaina o le nucleoside transporter 1 (ENT1) i luga o platelets, e oʻo atu ai i le faʻaputuina o le adenosine extracellular ma le faʻamalosia o le Gs-coupled adenosine A2A receptors [1]. O sela B16-F10 o loʻo faʻaalia ai le faʻaitiitia o fegalegaleaiga ma platelets mai isumu e togafitia i le ticagrelor pe a faʻatusatusa i isumu e togafitia i le saline [2].

I totonu ole B16-F10 melanoma faʻataʻitaʻiga faʻataʻitaʻiga ma intrasplenic metastasis, o isumu o loʻo togafitia i se vailaʻau o le ticagrelor (10 mg / kg) o loʻo faʻaalia ai le faʻaitiitia o le mama (84%) ma le ate (86%) metastases. E le gata i lea, o togafitiga ticagrelor e faʻaleleia ai le ola pe a faʻatusatusa i manu faʻamaʻi saline. O se aafiaga talitutusa o loʻo matauina i le 4T1 faʻataʻitaʻiga o le kanesa o le susu, faʻatasi ai ma le faʻaitiitia o le mama (55%) ma le gaʻo ponaivi (87%) metastases pe a uma togafitiga ticagrelor [2]. O le tuʻu tautala tasi o le ticagrelor (1-10 mg / kg) e mafua ai le faʻaogaina o le faʻaogaina o le faʻaogaina i luga o le faʻapipiʻiina o platelet. Ticagrelor, i le maualuga maualuga (10 mg / kg) e matua faʻalavelaveina le faʻapipiʻiina o platelet i le 1 h i le maeʻa ai o le tui ma o le pito i luga e matauina i le 4 h pe a uma le tui.

Teuina

4°C, puipuia mai le malamalama, teuina i lalo ole nitrogen

* I le solvent: -80°C, 6 masina; -20°C, 1 masina (puipui mai le malamalama, teuina i lalo ole nitrogen)

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