Ka hope

ʻO Ticagrelor kahi mea kū'ē hou o ka P2Y12 receptor [1].

Ua hōʻike ʻia ʻo Ticagrelor e kāohi i nā hopena prothrombotic o ADP ma ka platelet e kūʻē i ka P2Y12 receptor.Ua hōʻike ʻo Ticagrelor i ka pale piha ʻana o ka platelet aggregation ex vivo.Eia kekahi, ua ʻōlelo ʻo Ticagrelor i ka hoʻopaʻa ʻana i ka hopena o ka platelet aggregation i ke kanaka.Ma waho aʻe o kēia mau mea, ua hōʻike pū ʻo Ticagrelor i kahi antagonist paʻa waha, ikaika, reversibly.ʻAʻole like me nā mea hoʻopaneʻe ʻē aʻe, ua hōʻike pū ʻo Ticagrelor i ka pale ʻana i ka receptor P2Y12 me ka ʻole o ka hoʻololi metabolic.Ma waho aʻe o kēlā, ʻo Ticagrelor ka mea mua thienopyridine anti-platelet agent a me ka nui o ka metabolized e CYP3A4 a me CYP2C19 [1] [2].

Kuhikuhi:
[1] Zhou D1, Anderson TB, Grimm SW.ʻO ka loiloi in vitro o nā pilina lāʻau lapaʻau me ka ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics.ʻO ka lāʻau lapaʻau Metab Dispos.2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW.ʻO ka hana a me ka metabolism o ticagrelor, kahi moʻolelo P2Y12 receptor antagonist, i nā ʻiole, nā ʻiole, a me nā marmosets.ʻO ka lāʻau lapaʻau Metab Dispos.2011 Sep;39(9):1555-67.doi: 10.1124/dmd.111.039669.Epub 2011 Iune 13.

wehewehe

ʻO Ticagrelor (AZD6140) he antagonist receptor P2Y12 oral reversible no ka mālama ʻana i ka platelet aggregation.

In Vitro

Hoʻolaha ʻo Ticagrelor i kahi kaohi nui o ka adenosine 5'-diphosphate (ADP)–hoʻokuʻu ʻia ʻo Ca2+ i loko o nā platelet ished me nā mea kūʻē P2Y12R ʻē aʻe.ʻO kēia hopena hou aʻe o ka ticagrelor ma mua o ka P2Y12R antagonism he hapa ia o ka ticagrelor e kāohi ana i ka equilibrative nucleoside transporter 1 (ENT1) ma nā platelets, e alakaʻi ana i ka hōʻiliʻili ʻana o ka adenosine extracellular a me ka hoʻoulu ʻana o Gs-coupled adenosine A2A receptors [1].Hōʻike nā pūnaewele B16-F10 i ka emi ʻana o ka launa pū ʻana me nā platelets mai nā ʻiole i mālama ʻia e ticagrelor i hoʻohālikelike ʻia me nā ʻiole i mālama ʻia i ka saline [2].

Ma ka B16-F10 melanoma intravenous a me intrasplenic metastasis models, nāʻiole i mālamaʻia me ka lāʻau lapaʻau o ticagrelor (10 mg / kg) e hōʻike ana i ka emiʻana o ka māmā (84%) a me ka ate (86%) metastases.Eia kekahi, hoʻomaikaʻi ka lāʻau ticagrelor i ke ola ma mua o nā holoholona i mālama ʻia i ka saline.ʻIke ʻia kahi hopena like i kahi ʻano maʻi maʻi umauma 4T1, me ka hoʻemi ʻana i ka māmā (55%) a me ka iwi iwi (87%) metastases ma hope o ka mālama ʻana i ka ticagrelor [2].ʻO ka hoʻokele waha waha hoʻokahi o ticagrelor (1-10 mg / kg) ke kumu i ka hopena inhibitory e pili ana i ka hopena ma ka platelet aggregation.ʻO Ticagrelor, ma ke kiʻekiʻe kiʻekiʻe (10 mg / kg) ke kāohi nui i ka platelet aggregation ma 1 h ma hope o ka hoʻopaʻa ʻana a ʻike ʻia ka inhibition kiʻekiʻe ma 4 h ma hope o ka dosing.

Waihona

4°C, pale mai ka malamalama, mālama ʻia ma lalo o ka nitrogen

*Ma ka solvent: -80°C, 6 mahina;-20°C, 1 mahina (pale mai ka malamalama, mālama ʻia ma lalo o ka nitrogen)

ʻO ke kinona