I-Clenbuterol, iyi-agonist ye-β2-adrenergic (β2-adrenergic agonist), efana ne-ephedrine (Ephedrine), ivame ukusetshenziswa emtholampilo ukwelapha isifo esingamahlalakhona sokuvimbela i-pulmonary (COPD), Ibuye isetshenziswe njenge-bronchodilator ukuze ikhulule ukukhuphuka okukhulu kwesifuba somoya.Ekuqaleni kwawo-1980, inkampani yaseMelika iCyanamid yathola ngephutha ukuthi inemiphumela esobala yokukhuthaza ukukhula, ukuthuthukisa izinga lenyama enomzimba omncane kanye nokunciphisa amafutha, ngakho yayisetshenziswa njenge-clenbuterol ekufuyweni kwezilwane.Nokho, ngenxa yemiphumela yayo engemihle, Umphakathi waseYurophu uvinjelwe ukusetshenziswa kwe-clenbuterol njengesengezo sokudla kusukela ngoJanuwari 1, 1988. Yavinjelwa yi-FDA ngo-1991. Ngo-1997, uMnyango Wezolimo waseRiphabhulikhi Yabantu baseChina wenqabela ngokuqinile. ukusetshenziswa kwamahomoni e-beta-adrenergic ekudleni nasekukhiqizeni izilwane, kanye neClenbuterol hydrochloride ibekwe kuqala.
Nokho, Clenbuterol racemic isanda kuboniswa ukunciphisa ingozi yesifo sikaParkinson.Ukuqinisekisa ukuthi yimaphi (noma womabili) ama-isomer akhiqiza lo mphumela, i-clenbuterol enantiomer ehlanzekile idinga ukufundwa ngokuhlukana.
Esihlokweni sakamuva, iqembu locwaningo lika-Elisabeth Egholm Jacobsen woMnyango Wezekhemikhali, iNorwegian University of Science and Technology, ngokubambisana noDkt. Zhu Wei we-Shangke Bio, lenze ukuhlanganiswa kwe-ketoreductase KRED kanye ne-cofactor nicotinamide adenine dinucleoside phosphate (NADPH) ).(R) -1-(4-Amino-3,5-dichlorophenyl) -2-bromoethhan-1-ol, ee > 93%;kanye (S)-N-(2 kwahlanganiswa uhlelo olufanayo ,6-Dichloro-4-(1-hydroxyethyl)phenyl)acetamide, ee >98%.Zombili lezi intermediates ngenhla kukhona ezingaba izandulela clenbuterol isomers.I-ketoreductase ES-KRED-228 esetshenziswe kulolu cwaningo yayivela kwa-Shangke Biopharmaceutical (Shanghai) Co., Ltd. Umphumela wocwaningo othi "Chemoenzymatic Synthesis of Synthons as Precursors for Enantiopure Clenbuterol and Other -2-Agonists" yanyatheliswa ku-"Catalysts" on. Novemba 4, 2018.
Isikhathi sokuthumela: Aug-26-2022