Corpus ID: 25735973

In vitro measurement of the beta-adrenergic blocking properties of ORF 12592, the 5-hydroxy analog of propranolol.

@article{Greenslade1978InVM,
  title={In vitro measurement of the beta-adrenergic blocking properties of ORF 12592, the 5-hydroxy analog of propranolol.},
  author={F. Greenslade and K. L. Newquist},
  journal={Archives internationales de pharmacodynamie et de therapie},
  year={1978},
  volume={233 2},
  pages={
          270-80
        }
}
ORF 12592 caused concentration-dependent inhibition of isoproterenol stimulated adenylate cyclase activity in sarcolemma-enriched membrane preparations of guinea-pig myocardium. Its potency was slightly less than that of d,l-propranolol. ORF 12592 did not stimulate basal enzyme activity, suggesting it to be devoid of intrinsic sympathomimetic activity. It produced no marked inhibition of basal activity, nor did it inhibit sodium fluoride stimulated enzyme activity, indicating that the compound… Expand
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Selective synthesis of the human drug metabolite 5’-hydroxypropranolol by an evolved self-sufficient peroxygenase
Propranolol is a widely used beta-blocker that is metabolized by human liver P450 monooxygenases into equipotent hydroxylated human drug metabolites (HDMs). It is paramount for the pharmaceuticalExpand