Azilsartan CAS #147403-03-0

Azilsartan CAS#147403-03-0 yog ib qho antagonist ntawm angiotensin II hom 1 receptor (AT1; IC50=0.42 μM) thiab cov nquag metabolite ntawm azilsartan medoxomil. Azilsartan yog tsim los ntawm azilsartan medoxomil los ntawm hydrolysis nyob rau hauv lub plab thiab lub siab. Azilsartan kuj ua raws li tus inverse agonist, inhibiting angiotensin II-induced tsub zuj zuj ntawm inositol-1-phosphate hauv COS-7 hlwb qhia recombinant tib neeg AT1 (IC50=2.6 nM). Nws txo qis qhov kev cog lus siab tshaj plaws uas tshwm sim los ntawm angiotensin II hauv cov kab mob aortic uas cais tawm (pD2=9.9). Azilsartan (100 ng / kg, iv) inhibits angiotensin II-induced pressor teb nyob rau hauv cov nas nco qab normotensive.

Azilsartan thiab chlorthalidone ua ke yog siv los kho cov ntshav siab (hypertension). Azilsartan yog angiotensin II receptor blocker (ARB). Nws ua haujlwm los ntawm kev thaiv cov khoom hauv lub cev uas ua rau cov hlab ntsha kom nruj. Yog li ntawd, azilsartan relaxes cov hlab ntsha. Qhov no txo ​​qis ntshav siab thiab ua kom cov ntshav thiab oxygen mus rau lub plawv.

Azilsartan tau txais txiaj ntsig zoo hauv cov neeg mob feem ntau ntawm cov teeb meem tsis zoo. Hauv kev tswj hwm, ob qhov muag tsis pom kev, randomized soj ntsuam kev sim piv cov txiaj ntsig ntawm azilsartan medoxomil rau ACE inhibitor ramipril hauv 784 tus neeg mob, tag nrho cov xwm txheej tsis zoo tau tshaj tawm tias tsis tshua muaj tshwm sim nrog azilsartan. Thaum lub sij hawm kho mob, kiv taub hau thiab hypotension tshwm sim ntau zaus nrog cov pab pawg kho mob azilsartan, thiab hnoos, cov kev mob tshwm sim hauv chav kawm feem ntau ntsib nrog ACE inhibitors, tshwm sim ntau zaus nrog ramipril pawg (8.2% ntawm cov neeg koom). hnoos tsuas yog tshwm sim hauv 1% thiab 1.4% ntawm azilsartan 40 thiab 80 mg pawg, feem. Lwm cov txiaj ntsig tau pom nyob rau hauv pawg azilsartan yog qhov muaj feem cuam tshuam rau hauv cov poov tshuaj, sodium, thiab uric acid; tsis muaj kev tuag tshwm sim los ntawm qhov teebmeem no lossis cov teebmeem uas tau hais tseg saum toj no thiab.

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