I-LCZ696(Sacubitril + Valsartan)
Incazelo
I-LCZ696 (Sacubitril/Valsartan), ehlanganisa i-Valsartan (an ARB) ne-Sacubitril (AHU377) ku-1:1 molar ratio, iyisigaba sokuqala, i-oral bioavailable, kanye ne-angiotensin receptor-neprilysin (ARN) inhibitor esebenza kabili ye-hypertension. kanye nokwehluleka kwenhliziyo[1][2][3]. I-LCZ696 ithuthukisa i-cardiomyopathy yesifo sikashukela ngokuvimbela ukuvuvukala, ukucindezeleka okwenziwe nge-oxidative kanye ne-apoptosis.
Ingemuva
I-LCZ696 ingeyokuqala ekilasini i-ARNi (i-angiotensin receptor neprilysin inhibitor) ehlanganisa izingxenye ze-anionic ze-AR valsartan kanye ne-neprilysin inhibitor prodrug AHU377 (1:1 isilinganiso) sokuhluleka kwenhliziyo nomfutho wegazi ophezulu.
Ama-angiotensin receptors ama-G-protein-coupled receptors. Balamula imithambo yenhliziyo neminye imiphumela ye-angiotensin II okuyi-peptide esebenzayo yohlelo lwe-renin-angiotensin. I-Neprilysin iyi-endopeptidase engathathi hlangothi eyehlisa i-endo native vasoactive peptides njenge-natriuretic peptides. Ukuvinjelwa kwe-neprilysin kukhulisa ukugxila kwe-natriuretic peptides okube nomthelela ekuvikelweni kwenhliziyo, imithambo yegazi nezinso. [1]
Emagundaneni e-Sprague-Dawley, ukuphathwa ngomlomo kwe-LCZ696 kuholele ekukhuphukeni okuncike kumthamo ku-immunoreactivity ye-atrial natriuretic peptide okubangelwa ukuvinjelwa kwe-neprilysin. Kumagundane e-hypertensive aphindwe kabili e-transgenic, i-LCZ696 ibangele ukwehla okuncike kumthamo kanye nokuqhubekayo ekucindezelweni kwe-arterial. Abahlanganyeli abanempilo, ucwaningo olungahleliwe, oluyimpumputhe kabili, olulawulwa yi-placebo luqinisekisile ukuthi i-LCZ696 inikeze ukuvinjelwa kwe-neprilysin ngesikhathi esifanayo kanye nokuvinjelwa kwe-AT1 receptor. I-LCZ696 yayiphephile futhi ibekezelelwa kahle kumuntu. [2] [3]
Izithenjwa:
McMurray JJ, Packer M, Desai AS et al. I-Angiotensin-neprilysin inhibition ngokumelene ne-enalapril ekuhlulekeni kwenhliziyo. N Engl J Med. 2014 Sep 11;371(11):993-1004.
U-Gu J, uNoe A, u-Chandra P, u-Al-Fayoumi S et al. I-Pharmacokinetics kanye ne-pharmacodynamics ye-LCZ696, inoveli esebenza kabili ye-angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14.
Langenickel TH, Dole WP. I-Angiotensin receptor-neprilysin inhibition nge-LCZ696: indlela entsha yokwelapha ukuhluleka kwenhliziyo, i-Drug Discov Today: Ther Strategies (2014),
Isitoreji
| Impushana | -20°C | 3 iminyaka |
| 4°C | iminyaka engu-2 | |
| Ku-solvent | -80°C | 6 izinyanga |
| -20°C | Inyanga engu-1 |
Isakhiwo samakhemikhali
Isiphakamiso18Amaphrojekthi Wokuhlola Ukuvumelana Kwekhwalithi asegunyaziwe4, futhi6amaphrojekthi angaphansi kokugunyazwa.
Uhlelo lokuphatha ikhwalithi yamazwe ngamazwe oluthuthukile lwenze isisekelo esiqinile sokuthengisa.
Ukugadwa kwekhwalithi kusebenza kuwo wonke umjikelezo wempilo womkhiqizo ukuze kuqinisekiswe ikhwalithi nomphumela wokwelapha.
Ithimba Lezindaba Zokulawula Ochwepheshe lisekela izimfuno zekhwalithi ngesikhathi sokufaka isicelo nokubhaliswa.
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