tailieunhanh - Báo cáo y học: "Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate"

Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học 'Respiratory Research cung cấp cho các bạn kiến thức về ngành y đề tài: "Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate. | Respiratory Research BioMed Central Research Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate Anagnostis Valotis and Petra Hogger Open Access Address Universitat Wurzburg Institut fur Pharmazie und Lebensmittelchemie Wurzburg Germany Email Anagnostis Valotis - valotis@ Petra Hogger - hogger@ Corresponding author Published 25 July 2007 Received 28 August 2006 Respiratory Research 2007 8 54 doi 1465-9921 -8-54 Accepted 25 July 2007 This article is available from http content 8 1 54 2007 Valotis and Hogger licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License http licenses by which permits unrestricted use distribution and reproduction in any medium provided the original work is properly cited. Abstract Fluticasone furoate FF - USAN approved name a new topically active glucocorticoid has been recently identified. The aim of this study was to characterise the binding affinity of this compound to the human lung glucocorticoid receptor in relation to other glucocorticoids. Additionally we sought to determine the binding behaviour of fluticasone furoate to human lung tissue. The glucocorticoid receptor binding kinetics of fluticasone furoate revealed a remarkably fast association and a slow dissociation resulting in a relative receptor affinity RRA of 2989 I 35 with reference to dexamethasone RRA I00 5 . Thus the RRA of FF exceeds the RRAs of all currently clinically used corticosteroids such as mometasone furoate MF RRA 2244 fluticasone propionate FP RRA I775 ciclesonide s active metabolite RRA I2I2 - rat receptor data or budesonide RRA 855 . FP and FF displayed pronounced retention in human lung tissue in vitro. Lowest tissue binding was found for MF. There was no indication of instability or chemical modification of FF in human lung .

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