Amavu n'amavuko

Ticagrelor ni antagonist antagonist ya reseptor ya P2Y12 [1].

Ticagrelor yavuzwe ko ibuza ingaruka za prothrombotique ya ADP kuri platel na reseptor ya P2Y12. Ticagrelor yerekanye ibibujijwe byuzuye bya platelet agregation ex vivo. Byongeye kandi, Ticagrelor yatanze igitekerezo cyo kubuza gukwirakwizwa kwa platine mu bantu. Usibye ibyo, Ticagrelor yanagaragaje umunwa, ukora, guhuza byimazeyo. Bitandukanye nizindi inhibitor, Ticagrelor nayo yatangaje ko ibuza reseptor ya P2Y12 idahinduye metabolike. Uretse ibyo, Ticagrelor ni yo ya mbere ya thienopyridine irwanya platel kandi ikoreshwa cyane na CYP3A4 na CYP2C19 [1] [2].

Reba:
[1] Zhou D1, Andersson Igituntu, Grimm SW. Muri vitro isuzumabushobozi ishobora guhuza ibiyobyabwenge nibiyobyabwenge 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 cyane kubuza adenosine 5′-difosifate (ADP)-yateje Ca2 + kurekura muri platine ished vs abandi P2Y12R barwanya. Izi ngaruka zinyongera za ticagrelor zirenze P2Y12R antagonism nimwe mubice nkinkurikizi za ticagrelor ibuza gutwara nucleoside itwara abantu 1 (ENT1) kuri platine, bigatuma habaho kwirundanya kwa adenosine idasanzwe no gukora kwa Gs hamwe na adenosine A2A yakira [1]. Ingirabuzimafatizo za B16-F10 zigaragaza imikoranire yagabanutse na platine ziva mu mbeba zivuwe na ticagrelor ugereranije nimbeba zivuwe na saline [2].

Muri B16-F10 melanoma yerekana imiyoboro ya metastasis na intrasplenic metastasis, imbeba zavuwe hamwe nubuvuzi bwa ticagrelor (10 mg / kg) zigaragaza kugabanuka kwibihaha (84%) numwijima (86%). Byongeye kandi, kuvura ticagrelor biteza imbere kubaho ugereranije ninyamaswa zivuwe na saline. Ingaruka nk'iyi igaragara mu buryo bwa 4T1 ya kanseri y'ibere, hamwe no kugabanuka kw'ibihaha (55%) no mu magufa (87%) nyuma yo kuvura ticagrelor [2]. Ubuyobozi bumwe bwo mu kanwa bwa ticagrelor (1-10 mg / kg) butera ingaruka zijyanye no kubuza kwanduza platine. 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)

Imiterere yimiti