a complex consisting of an organic base in association with hydrogen chloride
English Journal
Cloning and Characterization of Four Rabbit Aldo-keto Reductases Featuring Broad Substrate Specificity for Xenobiotic and Endogenous Carbonyl Compounds: Relationship with Multiple Forms of Drug Ketone Reductases.
Endo S1, Matsunaga T, Arai Y, Ikari A, Tajima K, El-Kabbani O, Yamano S, Hara A, Kitade Y.Author information 1GIfu Pharmaceutical University;AbstractMultiple forms of reductases for several drug ketones were isolated from rabbit liver, but their interrelationship and physiological roles remain unknown. We isolated cDNAs for four aldo-keto reductases (AKRs: 1C30, 1C31, 1C32 and 1C33), which share high amino acid sequence identity with the partial sequences of two rabbit naloxone reductases. The four recombinant enzymes reduced a variety of carbonyl compounds, including endogenous α-dicarbonyls (such as isatin and diacetyl), aldehydes (such as farnesal and 4-oxo-2-nonenal) and ketosteroids. They differed in specificity for drug ketones and ketosteroids. Although daunorubicin and befunolol were common substrates of all the enzymes, other drugs were reduced specifically by the enzymes shown in parentheses: naloxone (AKR1C30, AKR1C32 and AKR1C33); metyrapone (AKR1C32 and AKR1C33); loxoprofen (AKR1C31 and AKR1C32); ketotifen (AKR1C30), and naltrexone and fenofibric acid (AKR1C33). AKR1C30 reduced only 17-keto-5β-androstanes, whereas the other enzymes were active towards 3/17/20-ketosteroids, and AKR1C33 further reduced 3-keto groups of bile acids and 7α-hydroxy-5β-cholestanes. In addition, AKR1C30, AKR1C31, AKR1C32 and AKR1C33 were selectively inhibited by carbenoxolone, baccharin, phenolphthalein and zearalenone, respectively. The mRNAs for the four enzymes were ubiquitously expressed in male rabbit tissues, in which highly expressed tissues were the brain, heart, liver, kidney, intestine, colon and testis (for AKR1C30 and AKR1C31), brain, heart, liver, kidney, testis, lung and adrenal gland (for AKR1C32), and liver and intestine (for AKR1C33). The data suggest that the four enzymes correspond to the multiple drug-ketone reductases in rabbits, and function in the metabolisms of steroids, isatin and reactive carbonyl compounds, and bile acid synthesis.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2014 Feb 7. [Epub ahead of print]
Multiple forms of reductases for several drug ketones were isolated from rabbit liver, but their interrelationship and physiological roles remain unknown. We isolated cDNAs for four aldo-keto reductases (AKRs: 1C30, 1C31, 1C32 and 1C33), which share high amino acid sequence identity with the partial
Pharmacological evaluation of ocular beta-adrenoceptors in rabbit by tissue segment binding method.
Horinouchi T1, Morishima S, Tanaka Y, Koike K, Miwa S, Muramatsu I.Author information 1Division of Pharmacology, Department of Biochemistry and Bioinformative Sciences, School of Medicine, University of Fukui, Eiheiji, Fukui 910-1193, Japan.AbstractAIMS: This study evaluates ocular (iris, ciliary body and ciliary process) and nonocular (atria and lung) beta-adrenoceptors in rabbit to characterize the plasma membrane beta-adrenoceptors and binding affinities of beta-adrenoceptor antagonists.
Life sciences.Life Sci.2009 Jan 30;84(5-6):181-7. doi: 10.1016/j.lfs.2008.11.016. Epub 2008 Dec 3.
AIMS: This study evaluates ocular (iris, ciliary body and ciliary process) and nonocular (atria and lung) beta-adrenoceptors in rabbit to characterize the plasma membrane beta-adrenoceptors and binding affinities of beta-adrenoceptor antagonists.MAIN METHODS: The tissue segment binding method with a
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