和漢薬作用に関する薬学的基礎研究(第12報)漢薬麝香のβ-アドレナリン増強活性因子の薬理学的探索とその臓器選択的活性

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Potentiation of β-adrenergic responses by musk, an animal-origin drug, has been studied mainly in cat papillary muscle preparations driven by electric stimulation (10 V, 0.8 msec, 0.4 Hz). In order to isolate the β-adrenergic potentiation factors, musk (20 g) was extracted and the potentiation activity of each fraction was assayed, using the cardiac muscle. The resultant fraction W_<5-a> (64 mg) was homogeneous as judged by thin-layer chromatography. Dialyzed W_<5-a> was soluble in ethanol and water but not in ether. The β-adrenergic potentiation of the cardiac muscle induced by W_<5-a> was not due to the inhibition of catechol-O-methyl transferase (COMT) from the following facts : Parallelism between the COMT-inhibition activity and the β-adrenergic potentiation activity was not observed among the lots of musk tested, a purified musk fraction was a weaker inhibitor of COMT activity than the crude, and musk induced a potentiation of isoproterenol (IsP) to the same extent even in the high doses by which the inhibitory effect of pronethalol was surmounted. On the other hand it was observed that the purified fraction did not potentiate IsP-induced relaxation of smooth muscle preparations of trachea and taenia coli in guinea pigs. The crude musk itself potentiated the effect of IsP but not that of salbutamol which is well known as a COMT-resistant β-agonist. To conclude, the β-adrenergic potentiation induced by W_<5-a> in musk was very selective to cardiac muscle, and also there may be other factors in musk which induce the β-adrenergic potentiation in tracheal muscle, at least in part due to the COMT-inhibitory activity.
公益社団法人日本薬学会の論文
1978-04-25

和漢薬作用に関する薬学的基礎研究(第12報)漢薬麝香のβ-アドレナリン増強活性因子の薬理学的探索とその臓器選択的活性

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