Fage

Ticagrelor wani sabon abokin gaba ne na mai karɓar P2Y12 [1].

An ba da rahoton Ticagrelor don hana tasirin prothrombotic na ADP akan platelet ta kan mai karɓar P2Y12.Ticagrelor ya nuna cikakken hanawar tarawar platelet ex vivo.Bugu da ƙari, Ticagrelor ya ba da shawarar hanawa na dogaro da kashi na haɗin platelet a cikin ɗan adam.Baya ga waɗannan, Ticagrelor shima ya nuna ɗan adawa na baka, a rayayye, mai jujjuya ɗaurin kai.Ba kamar sauran masu hanawa ba, Ticagrelor kuma ya ba da rahoton hana mai karɓar P2Y12 ba tare da canji na rayuwa ba.Bayan haka, Ticagrelor shine farkon thienopyridine anti-platelet wakili kuma galibi ana daidaita shi ta CYP3A4 da CYP2C19 [1] [2].

Magana:
[1] Zhou D1, Andersson TB, Grimm SW.Ƙimar in vitro na yuwuwar hulɗar miyagun ƙwayoyi-magunguna tare da ticagrelor: cytochrome P450 reaction phenotyping, hanawa, ƙaddamarwa, da bambancin motsin rai.Drug Metab Dispos.2011 Afrilu; 39 (4): 703-10.
[2] Li Y1, Landqvist C, Grimm SW.Hali da metabolism na ticagrelor, wani labari P2Y12 antagonist mai karɓa, a cikin mice, berayen, da marmosets.Drug Metab Dispos.2011 Satumba; 39 (9): 1555-67.doi: 10.1124/dmd.111.039669.Epub 2011 Yuni 13.

Bayani

Ticagrelor (AZD6140) antagonist P2Y12 na baka mai jujjuyawa ne don maganin tarawar platelet.

A cikin Vitro

Ticagrelor yana haɓaka mafi girman hana adenosine 5"Diphosphate (ADP)-haifar da sakin Ca2+ a cikin platelet ished vs sauran P2Y12R antagonists.Wannan ƙarin tasirin ticagrelor da ya wuce P2Y12R antagonism yana cikin wani ɓangare saboda sakamakon ticagrelor yana hana jigilar jigilar nucleoside 1 (ENT1) daidai akan platelet, yana haifar da tarawar adenosine na waje da kunna Gs-haɗe da adenosine A2A masu karɓa[1].Kwayoyin B16-F10 suna nuna raguwar hulɗa tare da platelets daga berayen da aka yi wa ticagrelor idan aka kwatanta da berayen da aka yi wa gishiri[2].

A cikin B16-F10 melanoma intravenous da intrasplenic metastasis model, berayen da aka bi da su tare da kashi na asibiti na ticagrelor (10 mg/kg) suna nuna alamar raguwa a cikin huhu (84%) da hanta (86%) metastases.Bugu da ƙari kuma, maganin ticagrelor yana inganta rayuwa idan aka kwatanta da dabbobin da aka yi wa gishiri.Ana lura da irin wannan tasiri a cikin samfurin ciwon nono na 4T1, tare da raguwa a cikin huhu (55%) da marrow kashi (87%) metastases bayan maganin ticagrelor[2].Gudanar da baki ɗaya na ticagrelor (1-10 mg/kg) yana haifar da tasirin hanawa mai alaƙa da kashi akan tarawar platelet.Ticagrelor, a mafi girman kashi (10 mg / kg) yana hana haɓakar platelet a cikin sa'o'i 1 bayan yin amfani da shi kuma ana lura da mafi girman hanawa a cikin sa'o'i 4 bayan shan magani.

Ajiya

4°C, kariya daga haske, adana a ƙarƙashin nitrogen

*Cikin karin ruwa:-80°C, watanni 6;-20°C, wata 1 (kare haske, adana a ƙarƙashin nitrogen)

Tsarin sinadaran