Ticagrelor

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Ticagrelor Anticoagulant Hauv 28984  

Khoom Nthuav dav

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KHOOM NTES

Tom Qab

Ticagrelor yog cov tshuaj tawm tsam tshiab ntawm P2Y12 receptor [1].

Ticagrelor tau tshaj tawm tias yuav txwv cov prothrombotic ntawm ADP ntawm lub platelet los ntawm kev cuam tshuam P2Y12 receptor. Ticagrelor tau qhia qhov ua tiav ntawm kev txwv tsis pub platelet aggregation ex vivo. Ntxiv rau Ticagrelor tau qhia tias koob tshuaj yog-inhibition ntawm platelet aggregation hauv tib neeg. Sib nrug ntawm cov no, Ticagrelor kuj tseem tau ua qhov ncauj hais lus, nquag, thim rov qab kev thaiv kev tawm tsam. Tsis zoo li lwm cov tshuaj tiv thaiv kab mob, Ticagrelor kuj tseem tau tshaj tawm tias inhibit P2Y12 receptor tsis muaj qhov hloov pauv hauv metabolic. Dhau li ntawd, Ticagrelor yog thawj thienopyridine los tiv thaiv platelet tus neeg sawv cev thiab tsuas yog metabolized los ntawm CYP3A4 thiab CYP2C19 [1] [2].

Chiv keeb:
[1] Zhou D1, Andersson TB, Grimm SW. Hauv kev soj ntsuam vitro ntawm cov tshuaj muaj peev xwm-kev sib txuam nrog ticagrelor: cytochrome P450 cov tshuaj tiv thaiv phenotyping, inhibition, induction, thiab kinetics txawv. Tshuaj Mob Cawv Lub Cev. 2011 Plaub Hlis; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Kev cais tawm thiab cov metabolism ntawm ticagrelor, tshiab P2Y12 receptor antagonist, hauv nas, nas, thiab marmosets. Tshuaj Mob Cawv Lub Cev. 2011 Sep; 39 (9): 1555-67. doi: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Kev piav qhia

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

Hauv Vitro

Ticagrelor txhawb txoj kev txwv loj dua ntawm adenosine 5-diphosphate (ADP)-ntxias Ca2 + tso tawm hauv ished platelets vs lwm P2Y12R cov thaiv kev. Qhov no ntxiv ntawm ticagrelor dhau P2Y12R kev thaiv kev ua yeeb yaj kiab yog nyob rau hauv ib feem ntawm qhov muaj txiaj ntsig ntawm ticagrelor inhibiting qhov sib luag nucleoside transporter 1 (ENT1) ntawm platelets, ua rau kom tsub zuj zuj ntxiv ntawm adenosine thiab ua kom Gs-coupled adenosine A2A receptors [1]. B16-F10 cov hlwb ua pov thawj txo qis kev sib txuam nrog platelets los ntawm cov ticagrelor-kho cov nas piv rau cov nas ntsev muaj kev kho mob [2].

Hauv B16-F10 melanoma ua rau mob siab thiab mob ua kom zoo nkauj, cov nas kho nrog lub chaw txhaj tshuaj ntawm ticagrelor (10 mg / kg) cov khoom pov thawj txo cov ntsws (84%) thiab mob siab (86%) metastases. Tsis tas li ntawd, kev kho mob ticagrelor txhim kho kev muaj sia nyob piv rau cov tsiaj muaj tshuaj tua ntsev. Ib qho zoo sib xws yog pom nyob rau hauv tus qauv 4T1 mob cancer ntawm lub mis, nrog kev txo qis ntsws (55%) thiab hlwb pob txha (87%) metastases tom qab kho ticagrelor [2]. Kev noj ib leeg qhov ncauj ntawm ticagrelor (1-10 mg / kg) ua rau koob tshuaj hais txog kev hloov tshuaj ntawm platelet aggregation. Ticagrelor, ntawm qhov siab tshaj plaws (10 mg / kg) cuam tshuam loj heev ntawm platelet sib sau ntawm 1 h tom qab noj tshuaj thiab qhov siab tshaj plaws raug pom nyob ntawm 4 h tom qab noj tshuaj.

Cia

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

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

Tshuaj qauv

Ticagrelor

TXUJ CI NTSEEG

Quality management1

Kev Tawm Tsam 18 Cov Kev Ntsuas Xyuas Kom Zoo Kom Zoo Li Qub uas tau pom zoo 4, thiab 6 tej yaam num yog nyob rau hauv kev pom zoo.

Quality management2

Advanced thoob ntiaj teb zoo tswj system tau tso paus ruaj khov rau kev muag khoom.

Quality management3

Kev saib xyuas kev ua tau zoo khiav thoob plaws lub neej tag nrho ntawm cov khoom kom ntseeg tau tias qhov zoo thiab ua kom zoo. 

Quality management4

Pawg kws tshaj lij ntxawg koom tes txhawb nqa qhov kev xav tau zoo thaum thov thiab sau npe.

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