Bucladesine

Isicelo
I-Dibutyryl cyclic adenosine monophosphate sodium yi-derivative ye-cyclic adenosine monophosphate, esetyenziselwa ukunyanga ukutshatyalaliswa kwe-cardiogenic kunye nokuhluleka kwentliziyo.Kwi-1999, i-Dibutyryl cyclic adenosine monophosphate ointment sodium yaphuhliswa ukunyanga ukusuleleka kwesikhumba kunye nezilonda zesikhumba.

Ukulungiswa kwe-sodium dibutyryl cyclophosphate adenosine: Kwi-flask equlethe i-cyclophosphate adenosine ngokucothayo yongeza isisombululo se-aqueous sodium hydroxide (3 mol / L) ehlayo, inkqubo elawulwayo yobushushu, i-dropwise igqibile ukufudumala kwiqondo lokushisa, lungisa i-pH ukuya kwi-7 ~ 8 kunye nesisombululo se-HCl ( I-20%), yongeza imvula ye-ethanol ye-anhydrous yokuqina okumhlophe, ukuhluza, ukomisa ukufumana ityuwa yesodium emhlophe;ityuwa yesodium kunye ne-n-butyl anhydride phantsi kokhuseleko lwe-N2 yokufudumala ukuya kwi-140 ℃ reaction.Ukujongwa kwe-TLC, ukusabela kugqityiwe kwaye kuthotywe kwiqondo lobushushu begumbi, ngokucotha ukongeza i-methyl tert-butyl ether, inkqubo yokuvuselela ngamandla, iChemicalbook ukufumana imveliso ekrwada ephantse imhlophe eyomeleleyo.Umxube we-methyl tert-butyl ether kunye ne-acetone yaphinda yamiswa ukuze kufumaneke imveliso ekujoliswe kuyo engumgubo omhlophe.Biological activityDibutyryl-cAMP(Bucladesine,dbcAMP) yi-cell-permeable PKA activator eyenza ngokuxelisa i-endogenous cAMP.Dibutyryl-cAMP(Bucladesine) ikwayi-phosphodiesterase(PDE) inhibitor.
Izifundo ze-in vitro:I-Dibutyryl-cAMP inqanda ukufunyanwa kwe-glucose ye-neuronal ngokusebenza kwe-PKA.Kwi-hepatocytes yeerat, i-Dibutyryl-cAMP inqanda i-inducible nitric oxide synthase expression kunye ne-NF-kappaB yokubopha umsebenzi.I-dibutyrChemicalbookyl-cAMP ikwanqanda i-apoptosis yeseli ye-TNFalpha-induced rod ngokuthintela ukulawulwa kwe-FADD.
Kwizifundo ze-vivo: Kwimodeli yempuku, i-Bucladesine (600nM/mouse,ip) ibuyisele umva i-zinc chloride kunye ne-acetate ekhokelayo ebangela ukugcinwa kwememori evasive.