Amavu n'amavuko

Ticagrelor ni antagonisti ya reseptor ya P2Y12 [1].

Ticagrelor yavuzwe ko ibuza ingaruka za prothrombotique ya ADP kuri platel hamwe na reseptor ya P2Y12.Ticagrelor yerekanye ibibujijwe byuzuye byo guteranya plato ex vivo.Mubyongeyeho, Ticagrelor yatanze igitekerezo cyo kubuza gukwirakwizwa kwa platine mubantu.Usibye ibyo, Ticagrelor yerekanye umunwa, ukora, guhuza guhuza antagonist.Bitandukanye nizindi inhibitor, Ticagrelor nayo yatangaje ko ibuza reseptor ya P2Y12 idahindutse.Uretse ibyo, Ticagrelor niyambere ya thienopyridine anti-platelet kandi ikoreshwa cyane na CYP3A4 na CYP2C19 [1] [2].

Reba:
[1] Zhou D1, Igituntu cya Andersson, Grimm SW.Muri vitro isuzumabushobozi ishobora guhuza ibiyobyabwenge na ticagrelor: cytochrome P450 reaction phenotyping, kubuza, kwinjiza, hamwe na kinetics zitandukanye.Ibiyobyabwenge bya Metab.2011 Mata; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW.Imyitwarire hamwe na metabolism ya ticagrelor, igitabo cyitwa P2Y12 reseptor antagonist, mu mbeba, imbeba, na marmoseti.Ibiyobyabwenge bya Metab.2011 Nzeri; 39 (9): 1555-67.doi: 10.1124 / dmd.111.039669.Epub 2011 Jun 13.

Ibisobanuro

Ticagrelor (AZD6140) ni uburyo bwo guhinduranya umunwa P2Y12 reseptor antagonist kugirango ivurwe hamwe.

Muri Vitro

Ticagrelor iteza imbere kubuza adenosine 5′-difosifate (ADP)-yateje Ca2 + kurekura muri platine yogejwe hamwe nabandi barwanya P2Y12R.Izi ngaruka zinyongera za ticagrelor zirenze P2Y12R antagonism nimwe mubice nkinkurikizi za ticagrelor ibuza gutwara nucleoside itwara 1 (ENT1) kuri platine, biganisha ku kwirundanya kwa adenosine idasanzwe no gukora kwa Gs hamwe na adenosine A2A yakira [1].Ingirabuzimafatizo za B16-F10 zigaragaza imikoranire yagabanutse na platine kuva imbeba zivuwe na ticagrelor ugereranije nimbeba zivuwe na saline.

Muri B16-F10 melanoma yerekana imiterere ya metastasis, imbeba zavuwe hamwe na ticagrelor (10 mg / kg) zigaragaza kugabanuka kwibihaha (84%) numwijima (86%).Byongeye kandi, kuvura ticagrelor bitezimbere kubaho ugereranije ninyamaswa zivuwe na saline.Ingaruka nkiyi igaragara muburyo bwa 4T1 ya kanseri yamabere, hamwe no kugabanuka kw ibihaha (55%) hamwe na magufa (87%) nyuma yo kuvura ticagrelor [2].Ubuyobozi bumwe bwo mu kanwa bwa ticagrelor (1-10 mg / kg) butera ingaruka zijyanye no kubuza kwishyira hamwe.Ticagrelor, ku kigero kinini (10 mg / kg) irabuza cyane guteranya platine kuri 1 h nyuma yo kuyinywa kandi kubuza impinga kugaragara saa yine nyuma yo kunywa.

Ububiko

4°C, urinde urumuri, ubitswe munsi ya azote

* Mubisubizo: -80°C, amezi 6;-20°C, ukwezi 1 (kurinda urumuri, ubitswe munsi ya azote)

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