2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. 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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Bunolol

Bunolol Chemical Structure

CAS No. : 27591-01-1

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Description

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[1][2][3].

IC50 & Target[1]

β-adrenoceptor

 

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.
Molecular Weight

291.39

Formula

C17H25NO3
CAS No.
SMILES

O=C1C=2C=CC=C(OCC(O)CNC(C)(C)C)C2CCC1
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Keywords:

Bunolol27591-01-1(Rac)-Bunolol dl-BunololAdrenergic ReceptorBeta Receptoralprenololisoprenalinealbino miceβ-adrenergic receptordichloroisoprenalinepilocarpinealbino ratshistaminemaximal electroshock-induced seizuresanaesthetized dogsInhibitorinhibitorinhibit

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