Imvelaphi

I-Ticagrelor ngumchasi wenoveli we-P2Y12 receptor [1].

I-Ticagrelor iye yabikwa ukuba inqanda imiphumo ye-prothrombotic ye-ADP kwiplatelet ngokuchasene ne-P2Y12 receptor.I-Ticagrelor ibonise inhibition epheleleyo ye-platelet aggregation ex vivo.Ukongeza i-Ticagrelor iphakamise ukuvinjelwa kwe-dose ye-platelet aggregation emntwini.Ngaphandle kwezi, i-Ticagrelor nayo ibonise umchasi obophelelayo ngomlomo, ngokusebenzayo, ngokubuyisela umva.Ngokungafani nezinye i-inhibitors, i-Ticagrelor nayo ibike ukuba inqanda i-P2Y12 i-receptor ngaphandle kokuguqulwa kwe-metabolic.Ngaphandle koko, i-Ticagrelor yi-agent yokuqala ye-thienopyridine ye-anti-platelet kwaye ngokukodwa i-metabolized yi-CYP3A4 kunye ne-CYP2C19 [1] [2].

IiReferensi:
[1] Zhou D1, Andersson TB, Grimm SW.Uvavanyo lwe-in vitro yokusebenzisana kweziyobisi kunye ne-ticagrelor: i-cytochrome ye-P450 yokuphendula i-phenotyping, inhibition, induction, kunye ne-kinetics eyahlukileyo.Iziyobisi Metab Dispos.2011 Epreli;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW.I-Disposition kunye ne-metabolism ye-ticagrelor, i-novel P2Y12 i-receptor antagonist, kwiigundane, iigundane, kunye ne-marmosets.Iziyobisi Metab Dispos.2011 Sep;39(9):1555-67.doi: 10.1124/dmd.111.039669.Epub 2011 Jun 13.

Inkcazo

I-Ticagrelor (AZD6140) i-reversible yomlomo ye-P2Y12 i-receptor antagonist yonyango lwe-platelet aggregation.

I-In vitro

I-Ticagrelor ikhuthaza ukuvinjelwa okukhulu kwe-adenosine 5"-idiphosphate (ADP)-ukukhutshwa kwe-Ca2+ kwiiplatelet ze-ish vs abanye abachasi be-P2Y12R.Le mpembelelo eyongezelelweyo ye-ticagrelor ngaphaya kwe-P2Y12R i-antagonism iyingxenye njengesiphumo se-ticagrelor inhibiting i-nucleoside transporter elinganayo 1 (ENT1) kwiiplatelet, ezikhokelela ekuqokeleleni i-adenosine ye-extracellular kunye nokusebenza kwe-Gs-coupled adenosine A2A receptors [1].Iiseli ze-B16-F10 zibonisa ukuncipha kwentsebenziswano kunye neeplatelet ezivela kwiigundane eziphathwe nge-ticagrelor xa kuthelekiswa neempuku eziphathwe nge-saline [2].

Kwimizekelo ye-B16-F10 ye-melanoma ye-intravenous kunye ne-intrasplenic metastasis, iigundane eziphathwe nge-dose yekliniki ye-ticagrelor (10 mg / kg) ibonisa ukunciphisa okuphawulweyo kwimiphunga (84%) kunye nesibindi (86%) i-metastases.Ngaphezu koko, unyango lwe-ticagrelor luphucula ukusinda xa kuthelekiswa nezilwanyana eziphathwe nge-saline.Umphumo ofanayo ubonwa kwi-4T1 imodeli yomhlaza wesifuba, kunye nokunciphisa imiphunga (55%) kunye nomnkantsha wethambo (87%) i-metastases elandela unyango lwe-ticagrelor [2].Ukulawulwa komlomo omnye we-ticagrelor (1-10 mg / kg) kubangela i-dose-related inhibitory effect kwi-platelet aggregation.I-Ticagrelor, kwi-dose ephezulu (i-10 mg / kg) inqanda kakhulu ukuhlanganiswa kweplatelet kwi-1 h emva kwe-dosing kunye ne-peak inhibition ibonwa kwi-4 h emva kwe-dosing.

Ugcino

4°C, ukukhusela ekukhanyeni, egcinwe phantsi kwenitrogen

*kwi-solvent : -80°C, iinyanga ezi-6;-20°C, inyanga eyi-1 (khusela ekukhanyeni, egcinwe phantsi kwenitrogen)

Ubume beMichiza