Bunolol
Bunolol ((Rac)-Bunolol) is a β-adrenergic receptor blocker. Bunolol antagonizes the β-receptor agonist activity induced by Isoproterenol (HY-B0468) and Dichloroisoproterenol. Bunolol reduces the heart rate and mean blood pressure of anesthetized dogs. Bunolol decreases spontaneous motor activity and Amphetamine-induced hyperactivity in rats, potentiates Pentobarbital-induced hypnosis in mice, and protects rats from extensor tonic convulsions induced by maximal electroshock.
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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: 27591-01-1
- 分子式: C17H25NO3
- 分子量:291.39
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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
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β-adrenoceptor |
Bunolol (0.1-3.2 mg/kg; i.v.; cumulative increments at 10-minute intervals; 1-3 mg/kg; i.v.; single dose, 15 minutes before alprenolol) does not significantly alter pulmonary resistance in healthy anesthetized dogs, but a 3 mg/kg dose blocks the resistance-lowering effect of low-dose alprenolol[2].
Bunolol (1 mg/kg; i.p.; single dose) does not exhibit inherent sedative or hypnotic effects in normal albino mice, but significantly potentiates pentobarbitone-induced hypnosis at 1 mg/kg[3].
Bunolol (10 mg/kg; i.p.; single dose) provides 20% protection against maximal electroshock-induced seizures in albino rats, reduces mean extensor tonic spasm duration to 2.6 seconds, and increases mean stupor duration to 27.0 minutes without causing mortality[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs (anesthetized with barbiturate)[1]
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Dosage:0.1 mg/kg
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Administration:i.v.; single dose
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Result:Produced 100% β-adrenergic blockade of the heart rate, contractile force, and blood pressure effects induced by isoproterenol.
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Animal Model:Mongrel dogs (either sex, 9-13 kg)[2]
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Dosage:0.1-3.2 mg/kg (cumulative i.v. doses); 1 mg/kg (single i.v. pre-alprenolol); 3 mg/kg (single i.v. pre-alprenolol)
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Administration:i.v. (cumulative increments at 10-minute intervals); i.v. (single dose, 15 minutes before alprenolol)
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Result:Did not cause any significant change in pulmonary resistance compared to control levels.
Increased the alprenolol dose required to reduce pulmonary resistance when given at 3 mg/kg.
Did not affect the alprenolol-induced resistance decrease when given at 1 mg/kg.
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Animal Model:Mongrel dogs (either sex, 9-13 kg)[2]
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Dosage:0.1-3.0 mg/kg
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Administration:i.v. (5-minute intervals)
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Result:Caused a significant increase in pulmonary resistance following administration during pilocarpine-induced bronchospasm.
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Animal Model:Albino mice (both sexes, 25-35 g)[3]
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Dosage:1 mg/kg
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Administration:i.p.; single dose; administered 15 minutes before pentobarbitone sodium
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Result:Exhibited no sedative or hypnotic action on its own.
Significantly potentiated the hypnotic action of pentobarbitone sodium.
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Animal Model:Albino rats (both sexes, 100-150 g)[3]
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Dosage:10 mg/kg
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Administration:i.p.; single dose; administered 30 minutes before electroshock
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Result:Provided 20% protection against extensor tonic spasm (8 out of 10 rats showed spasm).
Reduced mean extensor tonic spasm duration to 2.6 seconds.
Increased mean stupor duration to 27.0 minutes.
Caused no deaths within 24 hours.
化学情報
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CAS 番号 27591-01-1
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分子量 291.39
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分子式 C17H25NO3
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SMILES
O=C1C=2C=CC=C(OCC(O)CNC(C)(C)C)C2CCC1
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別名
(Rac)-Bunolol; dl-Bunolol
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)