生物活性 | |||
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描述 | Penicillamine (D-(-)-Penicillamine) is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease[3]. D-Penicillamine is the d isomer of a dimethylated cysteine and has been used for the treatment of rheumatoid arthritis. D-penicillamine significantly reduced L-cysteine-induced vasodilatation in a concentration-dependent manner through inhibition of H2 S biosynthesis, and this effect occurred at concentrations 10 times lower than those needed to induce the release of H2 S. In particular, D-penicillamine selectively inhibited CSE in a pyridoxal-5'-phosphate-dependent manner[4]. In animals, both intravenous D-penicillamine doses of 11 (low) and 44 mg/kg (high) decreased the mortality caused by s.c. isoprenaline (100 mg/kg) from 36% to 14% and 22%, respectively. However, whereas the low D-penicillamine dose decreased the release of cardiac troponin T (specific marker of myocardial injury), the high dose resulted in an increase[5]. In most normal human sera the addition of penicillamine to a final concentration of 0-2 mmol/l and subsequent dialysis caused a slight reduction in serum haemolytic complement (CH50). In vivo, a dose of 240 mg penicillamine caused a slight transient reduction in CH50 in rabbit serum, while 1000 mg penicillamine had no effect on serum CH50 in patients with rheumatoid arthritis[6]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01640548 | - | Completed | - | United Kingdom ... 展开 >> Abergavenny, United Kingdom, NP7 7EG Basildon, United Kingdom, SS16 5NL Basingstoke, United Kingdom, RG24 9NA Belfast, United Kingdom, BT9 7JB Blackburn, United Kingdom, BB2 3HH Bournemouth, United Kingdom, BH7 7DW Cambridge, United Kingdom, CB2 2QQ Cannock, United Kingdom, WS11 5XY Dewsbury, United Kingdom, WF13 4HS Dudley, United Kingdom, DY1 2HQ Durham, United Kingdom, DH15TW Eastbourne, United Kingdom, BN21 2UD Edinburgh, United Kingdom, EH4 2XU Glasgow, United Kingdom, G12 0YN Greenock, United Kingdom, PA16 0XN Harlow, United Kingdom, CM20 1QX Inverness, United Kingdom, IV2 3UV Kirkcaldy, United Kingdom, KY2 5AH London, United Kingdom, SE18 4QH Portsmouth, United Kingdom, PO6 3LY Sheffield, United Kingdom, S10 2JF Truro, United Kingdom, TR1 3LJ Warrington, United Kingdom, WA5 1QG Westbury-on-Trym, Bristol, United Kingdom, BS10 5NB Wigan, United Kingdom, WN6 9EW Wolverhampton, United Kingdom, WV10 0QP 收起 << | |
NCT01557348 | - | Completed | - | - | |
NCT01640548 | - | Completed | - | - |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.70mL 1.34mL 0.67mL |
33.51mL 6.70mL 3.35mL |
67.02mL 13.40mL 6.70mL |
参考文献 |
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