Synthesis, binding affinity and selectivity of new beta 1- and beta 2-adrenoceptor blockers

Farmaco. 1999 Nov-Dec;54(11-12):713-20. doi: 10.1016/s0014-827x(99)00077-4.

Abstract

The synthesis of a new series of sesamol derivatives with beta-adrenergic blocking activity is described. The affinity and selectivity of these compounds for beta 1- and beta 2-adrenoceptors were studied in comparison with those of ICI-118551 and propranolol. Some of the synthesized compounds show very good affinity for the beta 2-receptors of rat lung membranes and two of them provide interesting selectivity.

MeSH terms

  • Adrenergic beta-1 Receptor Antagonists*
  • Adrenergic beta-2 Receptor Antagonists*
  • Adrenergic beta-Antagonists / chemical synthesis*
  • Adrenergic beta-Antagonists / metabolism
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Lung / metabolism
  • Magnetic Resonance Spectroscopy
  • Male
  • Propanolamines / metabolism
  • Propanolamines / pharmacology
  • Protein Binding
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adrenergic, beta-1 / metabolism
  • Receptors, Adrenergic, beta-2 / metabolism
  • Spectrophotometry, Infrared

Substances

  • Adrenergic beta-1 Receptor Antagonists
  • Adrenergic beta-2 Receptor Antagonists
  • Adrenergic beta-Antagonists
  • Propanolamines
  • Receptors, Adrenergic, beta-1
  • Receptors, Adrenergic, beta-2
  • ICI 118551