Azapetine
Azapetine is an antagonist of α1-adrenoceptor, with an IC50 of 0.205 μM at rat α1-adrenoceptor and an IC50 of 1.3 μM at rat α2-adrenoceptor, and exhibits higher selectivity for α1-adrenoceptor than for α2-adrenoceptor. Azapetine functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine is used in related research on hypotension.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 146-36-1
- 分子式: C17H17N
- 分子量:235.32
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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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Help & FAQs
生物活性
製品説明
体外実験
Azapetine (15 min) acts as an α1-adrenoceptor antagonist on isolated rat anococcygeus muscle with a pA2 value of 7.82[1].
Azapetine (10 min) acts as an α2-adrenoceptor antagonist on isolated rat vas deferens with a pA2 value of 6.43[1].
Azapetine (10 min) acts as an α2-adrenoceptor antagonist on isolated guinea-pig ileum (Clonidine (HY-12721)-induced twitch inhibition) with a pA2 value of 6.80[1].
Azapetine (10 min) acts as an α2-adrenoceptor antagonist on isolated guinea-pig ileum (Norepinephrine (HY-13715)-induced twitch inhibition) with a pA2 value of 6.70[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Azapetine (100 μg/kg; i.c.; single dose) produces a long-lasting central hypotensive effect in rabbits, and Clonidine does not induce further hypotension in Azapetine-pretreated animals[3].
Azapetine (200 μg/kg; i.c.; single dose) produces a long-lasting central hypotensive effect in dogs, and Clonidine still induces significant hypotension and bradycardia in Azapetine-pretreated animals[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:either sex, 200-300 g[3]
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Dosage:200 μg/kg
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Administration:i.c.; single dose
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Result:Induced a mean maximal hypotensive effect of 60 mmHg.
Reduced the mean blood pressure fall induced by clonidine from 54 mmHg to 30 mmHg.
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Animal Model:either sex, 2-3 kg[3]
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Dosage:100 μg/kg
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Administration:i.c.; single dose
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Result:Significantly reduced blood pressure, with mean blood pressure remaining at 75/47 mmHg 1 hour post-injection, which was significantly lower than baseline.
Prevented clonidine from producing additional hypotension.
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Animal Model:either sex, 7-12 kg[3]
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Dosage:200 μg/kg
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Administration:i.c.; single dose
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Result:Reduced blood pressure from 141/97 mmHg to 128/89 mmHg, with blood pressure remaining significantly lower than baseline 1 hour post-injection.
Did not prevent clonidine from inducing further decreases in blood pressure and heart rate that were not significantly different from changes seen in control dogs treated with clonidine alone.
化学情報
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CAS 番号 146-36-1
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分子量 235.32
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分子式 C17H17N
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SMILES
C=CCN1CC2=C(C3=C(C1)C=CC=C3)C=CC=C2
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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]. Ishida Y, et al. Alpha-adrenolytic properties of apogalanthamine and azapetine analogs. Journal of pharmacobio-dynamics. 1985 Nov;8(11):917-23. [Content Brief]
[4]. Timmermans PB, et al. Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. Journal of medicinal chemistry. 1984 Apr;27(4):495-503. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Azapetine 関連分類
HY-181635 関連分類
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