Oral toxicity and pharmacokinetic studies of SHetA2, a new chemopreventive agent, in rats and dogs

SHetA2 is a heteroarotinoid that has shown selective inhibition of cancer cell growth and an induction of apoptosis without activation of nuclear retinoic acid receptors. In the rat study, SHetA2 was administered in 1% aqueous methylcellulose/0.2% Tween 80 by oral gavage at 0, 100, 500, and 2,000 mg...

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Published in:Drug and chemical toxicology (New York, N.Y. 1978) N.Y. 1978), 2013-07, Vol.36 (3), p.284-295
Main Authors: Kabirov, Kasim K., Kapetanovic, Izet M., Benbrook, Doris M., Dinger, Nancy, Mankovskaya, Irina, Zakharov, Alexander, Detrisac, Carol, Pereira, Marcia, Martín-Jiménez, Tomás, Onua, Emmanuel, Banerjee, Aryamitra, van Breemen, Richard B., Nikoli, Dejan, Chen, Lian, Lyubimov, Alexander V.
Format: Article
Language:English
Subjects:
Administration, Oral
Adrenal Glands - drug effects
Adrenal Glands - pathology
Animals
Anticarcinogenic Agents - administration & dosage
Anticarcinogenic Agents - pharmacokinetics
Anticarcinogenic Agents - toxicity
Area Under Curve
Beagle dog
chemoprevention
Chromans - administration & dosage
Chromans - pharmacokinetics
Chromans - toxicity
Dogs
Eating - drug effects
Female
Male
Motor Activity - drug effects
No-Observed-Adverse-Effect Level
Organ Size - drug effects
pharmacokinetic
Prostate - drug effects
Prostate - pathology
rat
Rats
Rats, Sprague-Dawley
SHetA2
Species Specificity
Thiones - administration & dosage
Thiones - pharmacokinetics
Thiones - toxicity
toxicity
Toxicity Tests
Weight Gain - drug effects
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Summary:SHetA2 is a heteroarotinoid that has shown selective inhibition of cancer cell growth and an induction of apoptosis without activation of nuclear retinoic acid receptors. In the rat study, SHetA2 was administered in 1% aqueous methylcellulose/0.2% Tween 80 by oral gavage at 0, 100, 500, and 2,000 mg/kg/day for 28 days. The high-dose administration induced decreased activity in male rats, decreased body-weight gains and food consumption, and changes in organ weights. The major metabolite of SHetA2 in rat plasma was monohydroxy SHetA2, which was considerably higher than the parent compound after oral and intravenous administration. Pharmacokinetic analysis showed extremely low (
ISSN:0148-0545
1525-6014
DOI:10.3109/01480545.2012.710632