Keeb kwm

Ticagrelor yog ib tug tshiab antagonist ntawm P2Y12 receptor [1].

Ticagrelor tau tshaj tawm tias inhibit qhov kev cuam tshuam prothrombotic ntawm ADP ntawm platelet los ntawm kev tawm tsam P2Y12 receptor. Ticagrelor tau qhia tag nrho inhibition ntawm platelet aggregation ex vivo. Tsis tas li ntawd, Ticagrelor tau qhia txog kev siv tshuaj tiv thaiv ntawm platelet aggregation hauv tib neeg. Sib nrug ntawm cov no, Ticagrelor kuj tau ua kom pom qhov ncauj, nquag, thim rov qab khi antagonist. Tsis zoo li lwm cov inhibitors, Ticagrelor kuj tau tshaj tawm tias inhibit P2Y12 receptor yam tsis muaj kev hloov pauv hauv metabolic. Tsis tas li ntawd, Ticagrelor yog thawj thienopyridine anti-platelet tus neeg sawv cev thiab feem ntau metabolized los ntawm CYP3A4 thiab CYP2C19 [1][2].

Cov ntaub ntawv:
[1] Zhou D1, Andersson TB, Grimm SW. Hauv vitro kev soj ntsuam ntawm cov tshuaj muaj peev xwm-tshuaj cuam tshuam nrog ticagrelor: cytochrome P450 cov tshuaj tiv thaiv phenotyping, inhibition, induction, thiab sib txawv kinetics. Tshuaj Metab Dispos. Peb Hlis 2011; 39(4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Kev cuam tshuam thiab metabolism ntawm ticagrelor, ib qho tshiab P2Y12 receptor antagonist, hauv nas, nas, thiab marmosets. Tshuaj Metab Dispos. 2011 Sep; 39(9):1555-67. doi: 10.1124/dmd.111.039669 ib. Epub 2011 Jun 13.

Kev piav qhia

Ticagrelor (AZD6140) yog ib qho rov qab qhov ncauj P2Y12 receptor antagonist rau kev kho mob ntawm platelet aggregation.

Hauv Vitro

Ticagrelor txhawb kev inhibition ntau dua ntawm adenosine 5'- Diphosphate (ADP)-induced Ca2+ tso tawm hauv ished platelets vs lwm P2Y12R antagonists. Qhov kev cuam tshuam ntxiv ntawm ticagrelor dhau ntawm P2Y12R antagonism yog ib feem ntawm qhov tshwm sim ntawm ticagrelor inhibiting qhov sib npaug ntawm nucleoside transporter 1 (ENT1) ntawm platelets, ua rau tsub zuj zuj ntawm extracellular adenosine thiab ua kom Gs-coupled adenosine A2A receptors [1] B16-F10 hlwb pom tias muaj kev cuam tshuam nrog cov platelets los ntawm cov nas uas tau kho ticagrelor piv rau cov nas uas tau noj cov ntsev[2].

Hauv B16-F10 melanoma intravenous thiab intrasplenic metastasis qauv, nas kho nrog kev kho mob koob tshuaj ticagrelor (10 mg / kg) qhia pom tias txo qis hauv ntsws (84%) thiab siab (86%) metastases. Tsis tas li ntawd, kev kho mob ticagrelor txhim kho txoj sia nyob piv rau cov tsiaj uas muaj ntsev. Ib qho txiaj ntsig zoo sib xws tau pom hauv 4T1 tus qauv mob qog noj ntshav, nrog txo qis hauv lub ntsws (55%) thiab cov pob txha pob txha (87%) metastases tom qab kho ticagrelor[2]. Kev tswj hwm qhov ncauj ib leeg ntawm ticagrelor (1-10 mg / kg) ua rau muaj kev cuam tshuam ntawm cov tshuaj tiv thaiv ntawm platelet aggregation. Ticagrelor, ntawm qhov koob tshuaj ntau tshaj (10 mg / kg) cuam tshuam cov platelet aggregation ntawm 1 teev tom qab noj thiab qhov siab tshaj plaws inhibition tau pom nyob rau 4 teev tom qab noj.

Cia

4°C, tiv thaiv los ntawm lub teeb, khaws cia hauv nitrogen

* Nyob rau hauv hnyav: -80°C, 6 hli; -20°C, 1 lub hlis (tiv thaiv los ntawm lub teeb, khaws cia hauv nitrogen)

Cov qauv tshuaj