Antioxidative Action of the β-Adrenoceptor Antagonist Bopindolol and Its Metabolite 18-502

Aniya, Yoko; Fong, Kun Fan; Naito, Akira; Sakanashi, Matao

doi:10.1254/jjp.68.323

Cited by 5 publications

(2 citation statements)

References 23 publications

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“…These results mean that landiol is able to enhance lipid peroxidation. This is supported by results from previous studies: acebutolol 23 and pindolol 24 enhanced the H 2 O 2 -induced lipid peroxidation in liver microsomes. Thus, it was speculated that landiolol itself may be able to increase ROS production directly.…”

Section: Discussionsupporting

confidence: 89%

Effects of Landiolol on Mechanical and Metabolic Changes in Rat Reperfused Ischaemic Hearts

Sakanashi¹,

Sugahara²,

Sakanashi

2006

Clin Exp Pharma Physio

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1. The aim of the present study was to clarify the effects of landiolol, a short-acting selective beta(1)-adrenoceptor blocking agent, on mechanical and metabolic changes in postischaemic perfused hearts. 2. Rat isolated hearts (n = 30) were randomly separated into non-ischaemic or ischaemic groups. The latter group was further divided into Krebs'-Henseleit solution (KHS)- and landiolol (30, 100 or 300 micromol/L)-treated groups. Ischaemic hearts were subjected to 25 min global ischaemia and 20 min reperfusion under atrial pacing. Time-course changes in left ventricular (LV) end-diastolic pressure (LVEDP), LV developed pressure (LVDP), peak positive velocity of change of LV pressure (LVdP/dt(max)) and coronary flow were observed along with tissue contents of adenosine triphosphate (ATP), creatine phosphate, inorganic phosphate (Pi), malondialdehyde (MDA) and lactate dehydrogenase (LDH) release in coronary effluent. The effects of landiolol on rat isolated aortic preparations under KCl contraction were also investigated. 3. Ischaemia-reperfusion significantly impaired cardiodynamics, such as LVEDP, LVDP and LVdP/dt(max), decreased myocardial ATP content and increased Pi and LDH release. In the 30 micromol/L landiolol-treated group, cardiovascular parameters impaired by ischaemia-reperfusion and increased LDH release were further exacerbated and myocardial MDA content was significantly increased. In the 300 micromol/L landiolol-treated group, cardiac contractile dysfunction was improved and myocardial MDA, ATP and Pi contents were preserved. All measurements in the 100 micromol/L landiolol-treated group were similar to those in the ischaemic KHS group. Furthermore, significant relaxations of isolated aortic preparations were obtained with landiolol 30-1000 micromol/L, suggesting a possible calcium antagonism with landiolol. 4. In conclusion, landiolol, at low concentrations, aggravated myocardial ischaemia-reperfusion injuries, whereas at high concentrations it ameliorated them. The former effect may be mediated by the production of reactive oxygen species, whereas the latter may involve calcium antagonist activity.

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Section: Discussionsupporting

confidence: 89%

Effects of Landiolol on Mechanical and Metabolic Changes in Rat Reperfused Ischaemic Hearts

Sakanashi¹,

Sugahara²,

Sakanashi

2006

Clin Exp Pharma Physio

Self Cite

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“…Bopindolol was found to have free radical scavenging activity; in this respect, it was more potent than propranolol (4). Aniya et al (4) suggested that this potent antioxidant activity of bopindolol may be useful in the treatment of various diseases caused by oxidative stress.…”

Section: Effects Of Bopindolol On Myocardial Ischemiamentioning

confidence: 99%

Bopindolol: Pharmacological Basis and Clinical Implications

Nagatomo

Hosohata

Ohnuki

et al. 2001

Cardiovascular Drug Reviews

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Bopindolol, a non-selective antagonist of b 1 -and b 2 -adrenoceptors (ARs), has been found by pharmacological, molecular biological techniques and molecular modeling to have several unique properties. Bopindolol produces sustained blockade of b 1 -and b 2 -ARs, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Also, our recent molecular modeling studies identified possible interaction sites between bopindolol and b-AR subtypes. The reviewed studies support our findings that bopindolol is non-selective for b 1 -and b 2 -ARs, has low affinity for b 3 -AR subtype and has pharmacological properties that are likely to be beneficial in the treatment of cardiovascular diseases.

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Vasodilating β-adrenoceptor blockers as cardiovascular therapeutics

Toda

2003

Pharmacology & Therapeutics

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Antioxidative Action of the β-Adrenoceptor Antagonist Bopindolol and Its Metabolite 18-502

Cited by 5 publications

References 23 publications

Effects of Landiolol on Mechanical and Metabolic Changes in Rat Reperfused Ischaemic Hearts

Effects of Landiolol on Mechanical and Metabolic Changes in Rat Reperfused Ischaemic Hearts

Bopindolol: Pharmacological Basis and Clinical Implications

Vasodilating β-adrenoceptor blockers as cardiovascular therapeutics

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