Amifostine hydrate - CAS 63717-27-1
Category: Inhibitor
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Amifostine hydrate is a radiation-protective agent.
Amifostinum; Amifostine monohydrate; Amifostinum; Amifostina
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1.Mechanism of the protective activity of ICRF-187 against alloxan-induced diabetes in mice.
el-Hage A;Herman EH;Yang GC;Crouch RK;Ferrans VJ Res Commun Chem Pathol Pharmacol. 1986 Jun;52(3):341-60.
ICRF-187, (+)-1,2-bis(3,5-dioxopiperazine-1-yl)propane, has been shown to protect against alloxan diabetes (el-Hage et al., 1981). Since alloxan-induced pancreatic beta cell damage is thought to be mediated through the generation of highly reactive oxygen radicals by a metal catalyzed reaction involving both superoxide anion and hydrogen peroxide, in the present study the protective activity of ICRF-187 was compared with that of free radical scavengers, microsomal enzyme inhibitors and chelating agents. The free radical scavengers DMSO, vitamin E and WR2721 markedly reduced alloxan-induced hyperglycemia. ICRF-187 was found not to interact with superoxide anions, and there is no evidence to indicate that any of the known biological effects of ICRF-187 are mediated through free radical scavenging activity. SKF-525 and cimetidine, known inhibitors of drug metabolizing enzymes, also protected against the diabetogenic action of alloxan. Since it was found that ICRF-187 did not alter hexobarbital sleeping time, this compound must protect by a mechanism other than microsomal enzyme inhibition. Since the chelating agents EDTA and DETAPAC were found to protect against alloxan diabetes, ICRF-187 or its hydrolytic products, which are structurally similar to EDTA, could function as chelating agents.
2.Influence of different radioprotective compounds on radiotolerance and cell cycle distribution of human progenitor cells of granulocytopoiesis in vitro.
Klingler W;Kreja L;Nothdurft W;Selig C Br J Haematol. 2002 Oct;119(1):244-54.
Ficoll-separated mononuclear cells (MNC) of cryopreserved human bone marrow were incubated with isotoxic doses of diltiazem, N-acetylcysteine (NAC), glycopolysaccharide extract of spirulina platensis (SPE), tempol, thiopental, WR2721 and WR1065. After irradiation with a single dose of 0.73 Gy, survival of granulocyte/macrophage colony-forming cells (GM-CFC) was determined at d 10-14, using an agar culture system. Diltiazem, NAC, tempol and WR1065 significantly improved radiotolerance with protection factors (PF) between 1.21 and 1.36 (n = 5, P < 0.05) at 0.73 Gy (PF-0.73 Gy). The survival curves of diltiazem (D0 = 0.88 Gy, n = 1.00), NAC (D0 = 0.92 Gy, n = 1.10), tempol (D0 = 0.99 Gy, n = 1.10), WR1065 (D0 = 0.89 Gy, n = 1.16) and control (D0 = 0.78 Gy, n = 1.00) over 0.36-2.91 Gy showed a significant radioprotective effect for D0 only for tempol (P = 0.018) and for the extrapolation number 'n' only in the case of NAC (P = 0.023). Cell cycle analysis of the CD34+ cell subpopulation (control-0 h: G1 = 82.7%, S = 13.7%, G2/M = 3.6%) revealed that all compounds with a significant PF-0.73 Gy also caused a significant increase in CD34+ cells in S phase up to 48 h. Within the first 24 h, only NAC (26.
3.[Protective effects of WR2721 on early bone marrow hematopoietic function in mice exposed to 6.5 Gy of (60)Co γ-rays].
Deng ZL;Zhang LZ;Cong Y;Liu XL;Yu ZY;Shan YJ;Cui Y;Wang LM;Xing S;Cong YW;Luo QL Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Jun;22(3):791-6. doi: 10.7534/j.issn.1009-2137.2014.03.040.
The aim of this study was to investigate the effect of WR2721(amifostine) against bone marrow hematopoietic damage of mice exposed to 6.5 Gy of (60)Co-γ ray. A total of 60 C57/BL6J mice was divided into 3 groups:normal group (mice were injected with physiological salt solution), irradiation group (mice were injected with physiologic salt solution before irradiation) and WR2721 group (mice were injected with WR2721 before irradiation). The WBC, neutrophil (Neut), Plt and RBC levels in peripheral blood of 3 group mice were counted within 60 days after irradiation; the bone marrow nuclear cells (BMNC) were counted at 2 and 24 hours after irradiation; the hematopoietic stem/progenitor cell (LK/LSK) level and colony formation capability were detected by flow cytometry at 2 and 24 hours after irradiation. The results indicated that the counts of WBC and neut at 4 and 18 days, Plt at 7-18 days and RBC at 10-30 day after irradiation in WR2721 group were higher than those in irradiation group (P < 0.05); the BMNC, LSK and LK levels obviously increased at 24 hours after irradiation (P < 0.05), the CFU-GEMM, CFU-GM, CFU-MK BFU-E and CFU-E all significantly increased at 2 and 24 hours after irradiation (P < 0.
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CAS 63717-27-1 Amifostine hydrate

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