Ka morao

Ticagrelor ke mohanyetsi oa mocha oa P2Y12 receptor [1].

Ticagrelor e tlalehiloe hore e thibela liphello tsa prothrombotic tsa ADP ho platelet ka khahlanong le P2Y12 receptor. Ticagrelor e bontšitse thibelo e feletseng ea platelet aggregation ex vivo. Ho feta moo, Ticagrelor o khothalelitse thibelo e itšetlehileng ka tekanyo ea platelet aggregation ho motho. Ntle le tsena, Ticagrelor e boetse e bontšitse mohanyetsi ea tlamang ka molomo, ka mafolofolo, ka mokhoa o fetohang. Ho fapana le li-inhibitors tse ling, Ticagrelor e boetse e tlalehile ho thibela P2Y12 receptor ntle le phetoho ea metabolism. Ntle ho moo, Ticagrelor ke moemeli oa pele oa thienopyridine anti-platelet mme haholo-holo o sebelisoa ke CYP3A4 le CYP2C19 [1][2].

Litšupiso:
[1] Zhou D1, Andersson TB, Grimm SW. Tlhahlobo ea in vitro ea ho sebelisana ha lithethefatsi le lithethefatsi le ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, le kinetics e fapaneng. Lithethefatsi Metab Dispos. 2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Boitšoaro le metabolism ea ticagrelor, e leng mohanyetsi oa P2Y12 ea receptor, ho litoeba, likhoto le marmosets. Lithethefatsi Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.

Tlhaloso

Ticagrelor (AZD6140) ke mohanyetsi oa molomo oa P2Y12 o fetolehang bakeng sa phekolo ea platelet aggregation.

Ka Vitro

Ticagrelor e khothalletsa thibelo e kholo ea adenosine 5"- diphosphate (ADP)-e khothalelitse ho lokolloa ha Ca2+ ho liplatelete tsa ished vs bahanyetsi ba bang ba P2Y12R. Phello ena e eketsehileng ea ticagrelor ho feta P2Y12R antagonism ke karolo e itseng e le phello ea ticagrelor e thibelang nucleoside transporter 1 (ENT1) ho li-platelet, e lebisang ho bokelleng ha extracellular adenosine le ts'ebetso ea Gs-coupled adenosine A2A receptors [1]. Lisele tsa B16-F10 li bonts'a tšebelisano e fokotsehileng le liplatelete tse tsoang ho litoeba tse tšoaroang ke ticagrelor ha li bapisoa le litoeba tse nang le letsoai [2].

Ka B16-F10 melanoma mehlala ea methapo le methapo ea methapo ea methapo, litoeba tse tšoaroang ka tekanyo ea kliniki ea ticagrelor (10 mg / kg) li bontša ho fokotseha ha matšoafo (84%) le sebete (86%) metastases. Ho feta moo, phekolo ea ticagrelor e ntlafatsa bophelo ha e bapisoa le liphoofolo tse tšoaroang ka letsoai. Phello e tšoanang e bonoa ka mohlala oa kankere ea matsoele ea 4T1, ka ho fokotseha ha matšoafo (55%) le masapo a masapo (87%) metastases ka mor'a phekolo ea ticagrelor [2]. Tsamaiso e le 'ngoe ea molomo ea ticagrelor (1-10 mg / kg) e baka phello e thibelang tekanyo e amanang le tekanyo ea platelet aggregation. Ticagrelor, ka tekanyo e phahameng ka ho fetisisa (10 mg / kg) e thibela haholo platelet aggregation ka 1 h ka mor'a dosing le ho thibela tlhōrō ho hlokomeloa ka 4 h ka mor'a dosing.

Polokelo

4°C, sireletsa ho tloha leseli, bolokoa tlas'a naetrojene

*Ka solvent : -80°C, likhoeli tse 6; -20°C, khoeli e le 'ngoe (sireletsa leseli, e bolokiloe ka tlas'a naetrojene)

Sebopeho sa lik'hemik'hale