ndabere

Ticagrelor bụ onye mmegide ọhụụ nke onye nnabata P2Y12 [1].

A kọwo na Ticagrelor na-egbochi mmetụta prothrombotic nke ADP na platelet site na onye nata P2Y12.Ticagrelor egosila nkwụsị zuru oke nke nchịkọta platelet ex vivo.Na mgbakwunye, Ticagrelor atụwo aro maka mgbochi na-adabere na dose nke mkpokọta platelet n'ime mmadụ.Ewezuga ihe ndị a, Ticagrelor egosipụtakwala onye na-emegide ya n'okwu ọnụ, na-arụsi ọrụ ike, na-agbanwe agbanwe.N'adịghị ka ndị na-egbochi ndị ọzọ, Ticagrelor akọpụtakwala ka ọ gbochie P2Y12 nnabata na-enweghị mgbanwe metabolic.Na mgbakwunye na nke ahụ, Ticagrelor bụ onye na-ahụ maka mgbochi thienopyridine nke mbụ yana metabolized site na CYP3A4 na CYP2C19 [1] [2].

Ntụaka:
[1] Zhou D1, Andersson TB, Grimm SW.Nyocha in vitro nke enwere ike ịmekọrịta ọgwụ-ọgwụ na ticagrelor: cytochrome P450 mmeghachi omume phenotyping, mgbochi, ntinye, na kinetics dị iche iche.Mwepu ọgwụ Metab.2011 Eprel; 39 (4): 703-10 .
[2] Li Y1, Landqvist C, Grimm SW.Ọnọdụ na metabolism nke ticagrelor, akwụkwọ akụkọ P2Y12 antagonist nnabata, na ụmụ oke, oke na marmosets.Mwepu ọgwụ Metab.2011 Septemba; 39 (9): 1555-67 .doi: 10.1124/dmd.111.039669.Epub 2011 Jun 13.

Nkọwa

Ticagrelor (AZD6140) bụ onye na-emegide ndị na-anabata ọnụ P2Y12 maka ọgwụgwọ mkpokọta platelet.

Na Vitro

Ticagrelor na-akwalite mgbochi ka ukwuu nke adenosine 5'diphosphate (ADP)-ewepụtara Ca2+ n'ime platelet ished vs ndị ọzọ na-emegide P2Y12R.Mmetụta ọzọ nke ticagrelor gafere P2Y12R antagonism bụ akụkụ dị ka nsonaazụ nke ticagrelor na-egbochi 1 (ENT1) na-ebugharị nucleoside na platelet, na-eduga n'ịgbakọta adenosine extracellular na ịgbalite Gs-coupled adenosine A2A receptors[1].Mkpụrụ ndụ B16-F10 na-egosipụta mbelata mmekọrịta ya na platelet sitere na ụmụ oke ndị a na-agwọ ticagrelor ma e jiri ya tụnyere ụmụ oke ejiri saline mesoo[2].

Na B16-F10 melanoma intravenous na intrasplenic metastasis ụdị, ụmụ oke ejiri ọgwụ ticagrelor (10 mg / kg) na-egosiputa mbelata akara na ngụgụ (84%) na imeju (86%) metastases.Ọzọkwa, ọgwụgwọ ticagrelor na-eme ka ndụ dịkwuo mma ma e jiri ya tụnyere anụmanụ ndị a na-agwọ saline.A na-ahụ mmetụta yiri nke ahụ na ụdị ọrịa cancer ara 4T1, yana mbelata na ngụgụ (55%) na ụmị ọkpụkpụ (87%) metastases na-eso ọgwụgwọ ticagrelor [2].Otu nchịkwa ọnụ nke ticagrelor (1-10 mg / kg) na-ebute mmetụta mgbochi metụtara dose na nchịkọta platelet.Ticagrelor, na ọgwụ kachasị elu (10 mg / kg) na-egbochi nchịkọta platelet n'ụzọ dị ukwuu na awa 1 mgbe usoro ọgwụgwọ gasịrị, a na-ahụkwa mgbochi kachasị na awa 4 ka emechara ya.

Nchekwa

4°C, chebe site na ìhè, echekwara n'okpuru nitrogen

* Na ihe mgbaze: -80°C, ọnwa 6;-20°C, ọnwa 1 (chebe ọkụ, echekwara n'okpuru nitrogen)

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