High &bgr;1‐Selectivity and Favourable Pharmacokinetics as the Outstanding Properties of Bisoprolol

  title={High \&bgr;1‐Selectivity and Favourable Pharmacokinetics as the Outstanding Properties of Bisoprolol},
  author={Guenther Haeusler and H. J. Schliep and Pierre Schelling and K. H. Becker and Michael Dr Klockow and Klaus Minck and H. J. Enenkel and E. Schulze and R. Bergmann and Claus J. Dr. Schmitges and Christoph A. Seyfried and J{\"u}rgen Harting},
  journal={Journal of Cardiovascular Pharmacology},
&NA; Bisoprolol, (±)1‐(4‐[(2‐isopropoxyethoxy)‐methyl]‐phenoxy)‐3‐isopropyl‐amino‐2‐propanol‐hemifumarate, is a new, highly selective &bgr;1‐adrenoceptor blocking agent without intrinsic sympathomimetic activity and low to moderate local anaesthetic activity. As demonstrated in binding experiments, and in classical pharmacological studies using rats, guinea pigs, cats, and dogs, bisoprolol markedly differentiated between &bgr;1‐adrenoceptors of the heart, or the renal juxtaglomerular apparatus… 
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Radioligand binding characteristics of β2–adrenoceptors of cultured melanoma cells
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The failure of nadolol and bisoprolol to potentiate noradrenaline-evoked venoconstriction argues against the involvement of masked venodilator beta-adrenoceptors in the response.
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It is concluded that the stereoselective difference in the metabolic clearance between S(-)- and R(+)-bisoprolol caused the difference inThe disposition of bisoproll enantiomers.
Metabolic Fate of the New β-Adrenoceptor Antagonist, Bisoprolol, in Animals (1) : Absorption, Distribution and Excretion of 14C-Bisoprolol in Rats
The absorption, distribution and excretion of bisoprolol were studied in rats after oral or intravenous administration of 14C-bisoproll and whole body autoradiograms obtained with pigmented rats demonstrated that specific binding of radioactivity to melanin containing tissues was noticed.
Adverse Reactions with β-Adrenoceptor Blocking Drugs
In patients with peripheral vascular disease, β-blockers with β2-agonist activity are less likely to worsen the symptoms and signs of peripheral ischaemia, and may reduce the prevalence of peripheral coldness, a common adverse effect of β- blockers.
Metabolic Fate of the New β-Adrenoceptor Antagonist, Bisoprolol, in Animals (2) : Tissue Accumulation after Consecutive Oral Administration of 14C-Bisoprolol in Rats
There was not any accumulation of the drug and its metabolites in the organs and tissues of rats following the consecutive oral administration of 14C-bisoprolol, and radioactivity levels in most tissues decreased near the detection limit in either administration group.
Metabolic Fate of the New β-Adrenoceptor Antagonist, Bisoprolol, in Animals (3) : Foeto-placental Transfer and Excretion into Milk of 14C-Bisoprolol in Rats
Pregnant rats and lactating rats after the oral or intravenous administration of 14C-bisoprolol showed very little radioactivity was transferred to fetuses through the placenta in either route of the drug administration and the time course of radioactivity in the milk was similar to that in plasma.
Autoimmunity Against the Second Extracellular Loop of &bgr;1-Adrenergic Receptors Induces &bgr;-Adrenergic Receptor Desensitization and Myocardial Hypertrophy In Vivo
Sustained sympathomimetic-like actions of autoantibodies against the domain may be partly responsible for changes in rabbit cardiac dysfunction, and autoimmunity against the second extracellular loop of &bgr;1-ARs induced profound myocardial hypertrophy in vivo.