Ticagrelor

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Ticagrelor Anticoagulant Mumba 28984  

Chigadzirwa Chigadzirwa

Chigadzirwa Mateki

CHIDZIDZO CHIDZIDZO

Mhemberero

Ticagrelor inopikisana neruzivo rweP2Y12 receptor [1].

Ticagrelor yakanzi inhibit prothrombotic mhedzisiro yeADP pane platelet nekurwisa iyo P2Y12 receptor. Ticagrelor yakaratidza iyo yakazara inhibition yeplatelet kuunganidzwa ex vivo. Pamusoro pezvo Ticagrelor akataura nezvedanho rinoenderana nedziviriro yeplatelet kuunganidzwa mumunhu. Kunze kweizvi, Ticagrelor aratidzirawo nemuromo, achishinga, achidzosera anosunga anopikisa. Kusiyana nemamwe ma inhibitors, Ticagrelor akataura zvakare kuti inhibit P2Y12 receptor pasina metabolic shanduko. Kunze kwezvo, Ticagrelor ndiyo yekutanga thienopyridine anti-platelet mumiririri uye inonyanya kugadziriswa neCYP3A4 uye CYP2C19 [1] [2].

Zvinyorwa:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro kuongororwa kweanogona kudyidzana zvinodhaka-zvinodhaka ne ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, uye mutsauko kinetics. Zvinodhaka Metab Dispos. 2011 Kubvumbi; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW. Disposition uye metabolism ye ticagrelor, inoverengeka P2Y12 receptor anopikisa, mumakonzo, makonzo, uye mammosets. Zvinodhaka Metab Dispos. 2011 Sep; 39 (9): 1555-67. doi: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Tsananguro

Ticagrelor (AZD6140) inodzoserwa pamuromo P2Y12 receptor anopikisana yekurapa kweplatelet kuwanda.

MuVitro

Ticagrelor inosimudzira yakakura kuvharidzira adenosine 5'-diphosphate (ADP)-yakakurudzira Ca2 + kuburitswa mumashedhi maplatelet vs vamwe P2Y12R vanopikisa. Iyi yekuwedzera mhedzisiro ye ticagrelor kupfuura P2Y12R kupesana kuri muchikamu semhedzisiro ye ticagrelor ichitadzisa iyo yakaenzana nucleoside mutakuri 1 (ENT1) pamaplatelet, zvichitungamira kuunganidzwa kwe extracellular adenosine uye kumisikidza kweGs-yakabatanidzwa adenosine A2A receptors [1]. B16-F10 masero anoratidzira kudzikira kwekudyidzana nemaplatelet kubva kumakonzo akaitwa ticagrelor achienzaniswa nemakonzo anorapwa nesaline [2].

MuB16-F10 melanoma intravenous uye intrasplenic metastasis modhi, mbeva dzakarapwa nekiriniki muyero we ticagrelor (10 mg / kg) inoratidzira yakaderedzwa mapapu (84%) uye chiropa (86%) metastases. Uyezve, ticagrelor kurapwa inovandudza kupona kana ichienzaniswa nemhuka dzakarapwa nemunyu. Mhedzisiro yakafanana inoonekwa mune 4T1 kenza yemazamu modhi, nekudzikiswa mumapapu (55%) uye mapfupa emafuta (87%) metastases anotevera kurapwa kweticagrelor [2]. Kamwe kamwe kwemuromo manejimendi ye ticagrelor (1-10 mg / kg) inokonzeresa-zvine chekuita neanodzivirira maitiro pane platelet kuwanda. Ticagrelor, padanho repamusoro (10 mg / kg) zvakanyanya inhibits platelet kuunganidzwa pa1 h mushure mekuita dosing uye iyo yepamusoro inhibition inoonekwa pa4 h mushure mekuita dosing.

Kuchengetedza

4°C, chengetedza kubva pachiedza, zvakachengetwa pasi senitrogen

* Mune solvent: -80°C, mwedzi mitanhatu; -20°C, 1 mwedzi (chengetedza kubva pachiedza, zvakachengetwa pasi pe nitrogen)

Chimiro chemakemikari

Ticagrelor

CERTIFICATE

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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