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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 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.
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
Bucumolol potently induces a concentration-dependent negative inotropic effect in isolated guinea pig left atrial muscles, with a log 1/ED40 value of 0.097 mM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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.
プロトコル
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
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Acute brain-slice whole-cell patch-clamp recording
Acute brain-slice whole-cell patch-clamp recording measures membrane voltage or ionic current from visually targeted cells in living brain slices; after giga-seal formation, the membrane under the pipette is ruptured to provide low-resistance electrical access to the cell interior, enabling current-clamp analysis of excitability and voltage-clamp analysis of synaptic or membrane currents. Acute slices preserve local tissue architecture better than dissociated preparations and allow visually guided recording from defined brain regions or fluorescently labeled cells; however, whole-cell access also permits exchange between pipette solution and cytoplasm, so intracellular dialysis must be considered when interpreting signaling-dependent phenomena.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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)
Keywords
- Bucumolol
- 58409-59-9
- Adrenergic Receptor
- Renin
- 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