Asalkii hore

Ticagrelor waa iska soo horjeeda cusub ee P2Y12 reseptor [1].

Ticagrelor ayaa lagu soo warramey in ay joojiso saameynta prothrombotic ee ADP ee platelet iyada oo ka soo horjeeda soo dhaweynta P2Y12. Ticagrelor ayaa muujisay joojinta dhammaystiran ee isku-darka platelet ex vivo. Intaa waxaa dheer Ticagrelor waxay soo jeedisay qiyaasta ku-tiirsanaanta joojinta isku-darka platelet ee bini'aadamka. Marka laga reebo kuwan, Ticagrelor waxa kale oo uu soo bandhigay af ahaan, firfircooni, dib-u-noqosho xidhidhiye. Si ka duwan kuwa kale ee xannibaya, Ticagrelor ayaa sidoo kale soo warisay in ay joojiso soo-dhoweynta P2Y12 iyada oo aan isbeddelin dheef-shiid kiimikaad. Taas ka sokow, Ticagrelor waa wakiilka ugu horreeya ee thienopyridine anti-platelet waxaana inta badan metabolized by CYP3A4 iyo CYP2C19 [1] [2].

Tixraacyo:
[1] Zhou D1, Andersson TB, Grimm SW. Qiimaynta in vitro ee isdhexgalka daroogada-daawoyinka ee suurtogalka ah ee ticagrelor: cytochrome P450 falcelinta phenotyping, xannibaadda, kicinta, iyo kinetics kala duwan. Daawada Metab Dispos. 2011 Abriil; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Dabeecadaha iyo dheef-shiid kiimikaadka ticagrelor, sheeko cusub P2Y12 antagonist, oo ku jira jiirarka, jiirka, iyo marmosets. Daawada Metab Dispos. 2011 Seb;39 (9): 1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Juun 13.

Sharaxaada

Ticagrelor (AZD6140) waa P2Y12 reseptor antagonist oo afka laga beddeli karo oo loogu talagalay daawaynta isku-darka platelet.

In Vitro

Ticagrelor wuxuu kor u qaadaa xannibaad weyn oo ah adenosine 5"diphosphate (ADP)-Ca2+ waxay keentay in lagu sii daayo platelets-ka la ildaran iyo kuwa kale ee P2Y12R. Saamayntan dheeraadka ah ee ticagrelor ee ka baxsan P2Y12R antagonism waa qayb ahaan iyada oo natiijada ticagrelor ay joojisay gaadiidka nucleoside-ka dheellitiran ee 1 (ENT1) ee platelet, taasoo horseedaysa uruurinta adenosine-ka ka baxsan iyo firfircoonida Gs-ku-xidhan adenosine A2A reseptors[1]. Unugyada B16-F10 waxay muujinayaan isdhexgalka hoos u dhaca ee platelets ee jiirka ticagrelor-daaweeyay marka la barbar dhigo jiirarka saline-daaweeyay[2].

B16-F10 melanoma faleebada iyo moodooyinka metastasis ee gudaha, jiirarka lagu daaweeyay qiyaasta kiliinikada ee ticagrelor (10 mg/kg) waxay muujinaysaa hoos u dhac muuqda oo sambabada ah (84%) iyo beerka (86%) metastases. Intaa waxaa dheer, daawaynta ticagrelor waxay wanaajisaa badbaadada marka loo eego xayawaanka cusbada lagu daweeyay. Saameyn la mid ah ayaa lagu arkay qaabka kansarka naasaha ee 4T1, iyadoo la dhimay sambabada (55%) iyo dhuuxa lafta (87%) ka dib daawaynta ticagrelor[2]. Maamulka afka kaliya ee ticagrelor (1-10 mg/kg) wuxuu keenaa saameyn laxiriirta qiyaasta daawada isku-darka platelet. Ticagrelor, qiyaasta ugu sareysa (10 mg / kg) waxay si weyn u joojisaa isku-darka platelet-ka 1 saac ka dib qiyaasta iyo xakamaynta ugu sarreysa ayaa lagu arkay 4 saacadood ka dib qaadashada.

Kaydinta

4°C, ka ilaali iftiinka, lagu kaydiyo nitrogen hoostiisa

*Ku jirta dareere: -80°C, 6 bilood; -20°C, 1 bil (ka ilaali iftiinka, lagu kaydiyo nitrogen hoostiisa)

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