Mivazerol
Mivazerol is a selective α2-adrenoceptor agonist. Mivazerol decreases the spontaneous release of serotonin (5-HT) and significantly inhibits the immobilization stress-induced enhancement of norepinephrine (NE), dopamine (DA) and dihydroxyphenylacetic acid (DOPAC). Mivazerol inhibits intrathecal release of glutamate evoked by halothane withdrawal in rats, and exerts neuroprotective effects in forebrain ischemia rats. Mivazerol can be used for myocardial ischemia research.
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- CAS 番号: 125472-02-8
- 分子式: C11H11N3O2
- 分子量:217.22
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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α2-adrenergic receptor |
by halothane withdrawal in rats[1].
Mivazerol (2.5 μg/kg; i.t.; microinjection over 1 minute; 2 minutes prior to halothane withdrawal) inhibits intrathecal release of glutamate evoked
by halothane withdrawal in rats[1].
Mivazerol (10-40 μg/kg; s.c.; single dose; 30 min pre-ischemia) exerts neuroprotective effects in rat forebrain ischemia models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250-400 g) anesthetized with 1.1% halothane then subjected to halothane withdrawal[1]
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Dosage:15 μg/kg/h
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Administration:continuous infusion; starting 30 minutes prior to halothane withdrawal
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Result:Reduced the maximal halothane withdrawal-induced HR increase and reduced the maximal intrathecal glutamate release.
Attenuated the aspartate response but had no significant effect on BP response.
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Animal Model:Male Sprague-Dawley rats (250-400 g) anesthetized with 1.1% halothane then subjected to halothane withdrawal[1]
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Dosage:2.5 μg/kg
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Administration:i.t.; microinjection over 1 minute; 2 minutes prior to halothane withdrawal
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Result:Reduced the maximal halothane withdrawal-induced HR increase and reduced the maximal intrathecal glutamate release, with inhibition lasting at least 60 minutes post-withdrawal.
Had no significant effect on BP or aspartate responses with intrathecal administration.
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Animal Model:Male Sprague-Dawley rats (300-400 g) with forebrain ischemia[2]
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Dosage:10; 20; 40 μg/kg
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Administration:s.c.; single dose; 30 min pre-ischemia
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Result:Reduced 7-day survival rate to 40% in the 40 μg/kg group, compared to 90% in the 10 μg/kg and 20 μg/kg groups.
Recorded median neurologic deficit scores (NDS) of 10.0 at 24 h, 27.5 at 48 h, and ~5 at 7 days for the 10 μg/kg group; 30.0 at 24 h, 27.5 at 48 h, and ~5 at 7 days for the 20 μg/kg group; 43.0 at 24 h, 100.0 at 48 h, and 100 at 7 days for the 40 μg/kg group.
Observed significantly greater number of intact neurons in the hippocampal CA1 subfield in the 20 μg/kg group than in all other groups.
Lowered neocortex damage scores significantly in the 20 μg/kg group compared to the control and 40 μg/kg groups.
化学情報
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CAS 番号 125472-02-8
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分子量 217.22
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分子式 C11H11N3O2
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SMILES
O=C(C1=CC=CC(CC2=CN=CN2)=C1O)N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Zhang X, et al. Mivazerol inhibits intrathecal release of glutamate evoked by halothane withdrawal in rats. Acta Anaesthesiol Scand. 1998;42(8):1004-1009. [Content Brief]
[2]. Kimura T, et al. Neuroprotective effect of mivazerol, an alpha 2-agonist, after transient forebrain ischemia in rats. Acta Anaesthesiol Scand. 2005 Sep;49(8):1117-23. [Content Brief]
[3]. Kimura T, et al. Effect of mivazerol, a alpha-agonist, on striatal norepinephrine concentration during transient forebrain ischemia in rats. Acta Anaesthesiol Scand. 2008 Aug;52(7):997-1002. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Mivazerol 関連分類
HY-106865 関連分類
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