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 hadal ahaan, firfircooni, dib-u-celin ku xidhidh.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 suurtagalka ah ee ticagrelor: cytochrome P450 falcelinta phenotyping, ka-hortagga, kicinta, iyo kinetics kala duwan.Daawada Metab Dispos.2011 Abriil; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW.Dabeecadda iyo dheef-shiid kiimikaadka ticagrelor, sheeko cusub P2Y12 antagonist receptor, 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 soo dhawaynta soo dhawaynta afka ah ee daawaynta isu geynta platelet.

In Vitro

Ticagrelor waxay kor u qaadaa joojinta weyn ee adenosine 5"diphosphate (ADP)-Ca2+ oo ay keentay in lagu sii daayo platelets-ka la ildaran iyo kuwa kale ee P2Y12R.Saamayntan dheeriga ah ee ticagrelor ee ka baxsan P2Y12R antagonism waa qayb ka mid ah natiijada ticagrelor ee xakameynaya qaadaha nucleoside-ka dheellitiran 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 milixda-la daweeyey[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 la barbar dhigo 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 keliya ee ticagrelor (1-10 mg/kg) wuxuu keenaa saamaynta xannibaadda ee la xiriirta qiyaasta isku-darka platelet.Ticagrelor, qiyaasta ugu sareysa (10 mg / kg) waxay si weyn u joojisaa isku-darka platelet 1 saac ka dib qaadashada daawada ugu sarreysana waxaa lagu arkay 4 saacadood ka dib qiyaasta.

Kaydinta

4°C, ka ilaali iftiinka, oo 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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