Bucumolol
Bucumolol is an orally active β-adrenergic receptor blocker. Bucumolol inhibits Renin release. Bucumolol exhibits activities including local anesthesia, antiarrhythmia, antihypertension, heart rate reduction, negative inotropy, cardiac action potential inhibition, and action potential duration shortening. Bucumolol does not increase cardiac electrical threshold, prolong atrial refractory period, or affect body weight in rodents. Bucumolol can be used in research related to arrhythmia and hypertension.
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- CAS 番号: 58409-59-9
- 分子式: C17H23NO4
- 分子量:305.37
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
β adrenergic receptor |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Bucumolol (50 mg/kg; p.o.; once daily; 6 weeks) suppresses hypertension development, lowers heart rate, and reduces plasma renin concentration in 5-week-old male spontaneously hypertensive rats, with no significant effect on body weight or plasma aldosterone concentration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SHR (male, 15 weeks of age)[2]
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Dosage:50 mg/kg
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Administration:p.o.; single dose
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Result:Decreased mean blood pressure from 163.8 mmHg to 149.4 mmHg (8.4% reduction, p < 0.01, N=8).
Lowered heart rate from 343.8 beats/min to 303.8 beats/min (p < 0.01, N=8).
Reduced plasma renin concentration from 4.23 ng/mL/h to 2.53 ng/mL/h (43.7% reduction, p < 0.01, N=8).
Showed a significant positive correlation (r=0.716, p < 0.05) between percent changes in plasma renin concentration and mean blood pressure.
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Animal Model:SHR (male, 5 weeks of age)[2]
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Dosage:50 mg/kg
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Administration:p.o.; once daily; 6 weeks
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Result:Produced significantly lower systolic blood pressure compared to controls as early as 1 week after dosing, with the difference sustained for 6 weeks.
Lowered heart rate throughout the 6-week period.
Reduced plasma renin concentration to 1.9 ng/mL/h (p < 0.05, final N=6) compared to control 4.4 ng/mL/h.
Tended to lower plasma aldosterone concentration to 226.8 pg/mL, with no statistically significant difference relative to control 304.4 pg/mL.
Showed no statistically significant difference in body weight compared to controls.
化学情報
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CAS 番号 58409-59-9
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分子量 305.37
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分子式 C17H23NO4
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SMILES
O=C1OC2=C(C=CC(C)=C2C=C1)OCC(CNC(C)(C)C)O
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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]. Nakayama K, et al. Antiarrhythmic activity of dextro- and levo-isomers of 5-methyl-8-(2-hydroxy-3-t-butylamino-propoxy) coumarin hydrocholoride (bucumolol), a beta-adrenergic blocking agent, on aconitine-induced atrial and ouabain-induced ventricular arrhythmias in dogs. Jpn J Pharmacol. 1979 Dec;29(6):935-45. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Bucumolol 関連分類
HY-184751 関連分類
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Keywords
- Bucumolol
- 58409-59-9
- Adrenergic Receptor
- Renin
- Beta Receptor
- ouabain-induced ventricular arrhythmia
- spontaneously hypertensive rats
- cardiac fast sodium channel
- guinea pig papillary muscles
- guinea-pig right atria
- aconitine-induced atrial arrhythmia
- frog sciatic nerves
- guinea pig left atrial muscles
- β-adrenergic receptor
- hypertensive rodents
- Inhibitor
- inhibitor
- inhibit