Background

Ticagrelor mutsigiri mutsva weP2Y12 receptor [1].

Ticagrelor yakanzi inhibit prothrombotic migumisiro yeADP paplatelet nekurwisana neP2Y12 receptor. Ticagrelor yakaratidza kuvharwa kwakakwana kweplatelet aggregation ex vivo. Mukuwedzera Ticagrelor yakaratidza kuvharidzirwa-kunotsamira kweplatelet aggregation mumunhu. Kunze kweizvi, Ticagrelor yakaratidzawo nemuromo, kushingaira, reversibly kusunga anopikisa. Kusiyana nemamwe inhibitors, Ticagrelor yakashumawo kuti inhibit P2Y12 receptor pasina metabolic shanduko. Kunze kweizvozvo, Ticagrelor ndiyo yekutanga thienopyridine anti-platelet agent uye inonyanya kushandiswa neCYP3A4 uye CYP2C19 [1] [2].

References:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro kuongororwa kwezvinogona kushandiswa kwezvinodhaka-zvinodhaka ne ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, uye differential kinetics. Drug Metab Dispos. 2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Maitiro uye metabolism ye ticagrelor, inoveli P2Y12 receptor antagonist, mumakonzo, makonzo, uye marmosets. Drug Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.

Tsanangudzo

Ticagrelor (AZD6140) inopindurwa muromo weP2Y12 receptor antagonist yekurapa kweplatelet aggregation.

In Vitro

Ticagrelor inokurudzira kudziviswa kukuru kweadenosine 5'-diphosphate (ADP)-yakakonzera Ca2+ kuburitswa mumaplatelet ished vs vamwe vanopikisa P2Y12R. Iyi yakawedzera mhedzisiro yeticagrelor kupfuura P2Y12R antagonism iri muchikamu semhedzisiro yeticagrelor inhibiting equilibrative nucleoside transporter 1 (ENT1) pamaplatelet, zvichiita kuti kuunganidzwa kwe extracellular adenosine uye activation yeGs-coupled adenosine A2A receptors [1]. B16-F10 masero anoratidza kuderera kwekubatana nemaplatelet kubva kune ticagrelor-treated mice kana ichienzaniswa nesaline-treated mice[2].

MuB16-F10 melanoma intravenous uye intrasplenic metastasis mienzaniso, mice inobatwa nekiriniki yeticagrelor (10 mg / kg) inoratidza kuderedzwa kwemapapu (84%) uye chiropa (86%) metastases. Uyezve, kurapwa kweticagrelor kunovandudza kupona kana kuenzaniswa nemhuka dzine saline. Chiitiko chakafanana chinoonekwa mumuenzaniso wekenza yemazamu ye4T1, nekuderedza mumapapu (55%) uye bone marrow (87%) metastases inotevera ticagrelor kurapwa [2]. Single oral administration ye ticagrelor (1-10 mg / kg) inokonzera dose-related inhibitory effect pa platelet aggregation. Ticagrelor, pamwero wepamusoro (10 mg / kg) inodzivisa zvakanyanya kusanganiswa kweplatelet pa 1 h mushure mekuita dosing uye peak inhibition inoonekwa pa4 h mushure mekuita dosing.

Storage

4°C, kudzivirira kubva kuchiedza, kuchengetwa pasi penitrogen

*In solvent : -80°C, mwedzi mitanhatu; -20°C, mwedzi 1 (dzivirira kubva kuchiedza, yakachengetwa pasi penitrogen)

Chimiro chemakemikari