Acute and 28-days subacute toxicity studies of Gαq-RGS2 signaling inhibitor.

IF 2.7 Q3 MEDICINE, RESEARCH & EXPERIMENTAL
Jayesh V Beladiya, Anita A Mehta
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引用次数: 3

Abstract

Background: The aim of study was to evaluate the single oral dose and 28 day repeated oral administration toxicity profile of the synthetic compound Gαq-RGS2 signaling inhibitor, (1-(5-chloro-2-hydroxyphenyl)-3-(4-(trifluoromethyl)phenyl)-1 H-1,2,4-triazol-5(4 H)-one) as per OECD guideline 425 (2008a) and 407 (2008b), respectively.

Results: In acute toxicity study, a single oral dose administration of Gαq-RGS2 signaling inhibitor did not show any mortality at doses of 5, 50, 300 and 2000 mg/kg within 24 h and 14 days. The treatment of Gαq-RGS2 signaling inhibitor at dose 10 and 100 mg/kg for 28 days did not show any mortality, significant changes in the increase of body weight, various organ damage markers, hematological parameters, relative organ/body weight ratio and microscopic anatomical texture of essential organs as compared to vehicle and normal control.

Conclusions: A single oral administration of Gαq-RGS2 signaling inhibitor up to dose of 2000 mg/kg in mice and repeated administration of Gαq-RGS2 signaling inhibitor at higher dose 100 mg/kg for 28 days in the rats is safe.

g - αq- rgs2信号抑制剂急性和28天亚急性毒性研究。
背景:本研究的目的是评估合成化合物Gαq-RGS2信号抑制剂(1-(5-氯-2-羟基苯基)-3-(4-(三氟甲基)苯基)-1 H-1,2,4-三唑-5(4 H)- 1)的单次口服和28天重复口服的毒性特征,分别按照OECD指南425 (2008a)和407 (2008b)。结果:在急性毒性研究中,单次口服5、50、300和2000 mg/kg剂量的Gαq-RGS2信号抑制剂在24 h和14 d内均无死亡。10和100 mg/kg剂量的Gαq-RGS2信号抑制剂治疗28 d,与对照组和正常对照组相比,体重增加、各种器官损伤指标、血液学参数、相对脏器/体重比和重要器官显微解剖结构均有显著变化。结论:小鼠单次口服Gαq-RGS2信号抑制剂至2000 mg/kg,大鼠连续28 d多次口服高剂量Gαq-RGS2信号抑制剂至100 mg/kg是安全的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
4.40
自引率
0.00%
发文量
32
审稿时长
8 weeks
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