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Art. -Nr.: HY-114833

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Bunolol

Name: Bunolol
Brand: MedChemExpress
SKU: HY-114833
Availability: PreOrder

(Synonyms: (Rac)-Bunolol; dl-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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CAS. Nr.: 27591-01-1
Formel: C₁₇H₂₅NO₃
Molecular Weight:291.39

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Bunolol Chemical Structure

CAS. Nr.: 27591-01-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

β-adrenoceptor

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

Bunolol (0.1 mg/kg; i.v.; single dose) exhibits potent β-adrenergic blocking activity in barbiturate-anesthetized mongrel dogs, achieving complete blockade of isoproterenol-induced cardiac effects at an intravenous dose of 0.1 mg/kg^[1].
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.

Animal Model:

Mongrel dogs (anesthetized with barbiturate)^[1]
Dosage:

0.1 mg/kg
Administration:

i.v.; single dose
Result:

Produced 100% β-adrenergic blockade of the heart rate, contractile force, and blood pressure effects induced by isoproterenol.

Animal Model:

Mongrel dogs (either sex, 9-13 kg)^[2]
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)
Administration:

i.v. (cumulative increments at 10-minute intervals); i.v. (single dose, 15 minutes before alprenolol)
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.

Animal Model:

Mongrel dogs (either sex, 9-13 kg)^[2]
Dosage:

0.1-3.0 mg/kg
Administration:

i.v. (5-minute intervals)
Result:

Caused a significant increase in pulmonary resistance following administration during pilocarpine-induced bronchospasm.

Animal Model:

Albino mice (both sexes, 25-35 g)^[3]
Dosage:

1 mg/kg
Administration:

i.p.; single dose; administered 15 minutes before pentobarbitone sodium
Result:

Exhibited no sedative or hypnotic action on its own.
Significantly potentiated the hypnotic action of pentobarbitone sodium.

Animal Model:

Albino rats (both sexes, 100-150 g)^[3]
Dosage:

10 mg/kg
Administration:

i.p.; single dose; administered 30 minutes before electroshock
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.

Chemical Information

CAS. Nr. 27591-01-1
Molecular Weight 291.39
Formel C₁₇H₂₅NO₃
SMILES

O=C1C=2C=CC=C(OCC(O)CNC(C)(C)C)C2CCC1
Synonyms

(Rac)-Bunolol; dl-Bunolol
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Schwender C F, et al. Derivatives of 3, 4-dihydro-1 (2H)-naphthalenone as. beta.-adrenergic blocking agents. 3. Carbonyl-containing analogs of bunolol[J]. Journal of Medicinal Chemistry, 1973, 16(5): 585-588.

[2]. Giles RE, et al. Effects of alprenolol, bunolol and propranolol on pulmonary resistance in the anaesthetized dog. Eur J Pharmacol. 1971 Oct;16(2):155-63. [Content Brief]

[3]. Khanna N K, et al. Neuropharmacological Actions of two New Adrenergic Beta-Receptor Antagonists, Bunolol and H 64/52[J]. The Japanese Journal of Pharmacology, 1972, 22(2): 262-264.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
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- In Vivo
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Bunolol

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen