Ticagrelor

Whakaahuatanga Poto:

Ingoa o API Tohu Whakatakotoranga US DMF  EU DMF  CEP
Ticagrelor Anticoagulant I-Roto 28984  

Taipitopito Hua

Tohu Hua

WHAKAWEHE KOREUTU

Papamuri

Ko Ticagrelor he tangata whakaeke i te kaiwhakautu P2Y12 [1].

Kua puta te korero mo te Ticagrelor ki te aukati i nga paanga o te ADP ki runga i te peihana ki te taha o te kaiwhakawhiwhi P2Y12. Kua whakaatuhia e Ticagrelor te aukati i te whakakotahitanga o te pereti whakatipuranga ex vivo. Hei taapiri kua whakaarohia e Ticagrelor te aukati i te horopeta-whakatoi mo te whakatipuranga peariki i te tangata I tua atu i enei, kua whakaatuhia hoki e Ticagrelor tetahi tangata haangai ki te waha, ki te kaha, ki te hoki whakamuri. Kaore i rite ki etahi atu aukati, kua kii te Ticagrelor ki te aukati i te kaitautoko P2Y12 me te kore whakarereke a-taapiri. I tua atu i tera, ko te Ticagrelor te tuatahi o te kaihoko anti-papahiko thienopyridine me te nuinga o nga mahi a CYP3A4 me CYP2C19 [1] [2].

Tohutoro:
[1] Zhou D1, Andersson TB, Grimm SW. Arotake in vitro o nga taunekeneke tarukino-tarukino pea me te ticagrelor: cytochrome P450 tauhohenga phenotyping, aukati, whakauru, me nga rereketanga rereketanga. Te Tukuna Meta Waipiro. 2011 Aperira; 39 (4): 703-10.
[2] Li Y1, Whenua Whenua C, Grimm SW. Te tuuroro me te pungao o te ticagrelor, he kaitautoko receptor P2Y12 pakiwaitara, i roto i nga kiore, iore, me nga marmosets. Te Tukuna Meta Waipiro. 2011 Hepetema; 39 (9): 1555-67. mahi: 10.1124 / dmd.111.039669. Epub 2011 Jun 13.

Whakaahuatanga

Ko te Ticagrelor (AZD6140) he kaitautoko kaiwhiwhi P2Y12 ka taea te whakahoki mo te maimoatanga o te whakahiato papara.

I Vitro

Ko te Ticagrelor te whakatairanga i te kaha ki te aukati i te adenosine 5'-diphosphate (ADP)-i whakauruhia a Ca2 + ki roto i nga peera kua whakahekehia me etahi atu kaiwhakarato P2Y12R. Ko tenei hua ke atu o te ticagrelor i tua atu o te P2Y12R antagonism he waahanga hei hua o te ticagrelor e aukati ana i te kaikawe o te kaipupuri nucleoside 1 (ENT1) ki runga i nga peara, e ahu ana ki te whakaeminga o te adenosine extracellular me te whakahohe i nga kaiwhakawhiwhi adenosine A2A o te Gs [1]. Ko nga waahanga B16-F10 e whakaatu ana i te whakahekenga o te taunekeneke me nga peera mai i nga kiore ticagrelorororororororororororatia i whakaritea ki nga kiore rongoa saline [2].

I roto i te B16-F10 melanoma tauira metastasis uaua me te intrasplenic, ko nga kiore e tukinotia ana me te horopeta haumanu o te ticagrelor (10 mg / kg) e whakaatu ana i nga whakahekenga kua kitea i roto i te pungarehu (84%) me nga ate (86%) metastases. Ano hoki, ko te rongoa ticagrelor te whakapai ake i te ora ki te whakaritea ki nga kararehe e rongohia ana e te tote. He penei ano te kitenga i roto i te tauira pukupuku pukupuku uma 4T1, me te whakahekenga o te puhukahu (55%) me te koiwi wheua (87%) metastases whai muri i te maimoatanga ticagrelor [2]. Ko te whakahaere a-waha kotahi o te ticagrelor (1-10 mg / kg) ka hua te aukati i te horopeta e pa ana ki te whakatipuranga papara. Ko te Ticagrelor, i te horopeta teitei (10 mg / kg) ka tino aukati i te whakahiatotanga o te papa i te 1 haora i muri o te werohanga, ka kitea te aukati i te tihi i te 4 h i muri o te werohanga

Rokiroki

4°C, tiakina mai i te maama, penapena i raro i te hauota

* I roto i te whakarewa: -80°C, 6 marama; -20°C, 1 marama (tiakina mai i te maama, penapena i raro i te hauota)

Hanganga matū

Ticagrelor

WHAKAMAHI

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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