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- FUJITA HIRONORI
- Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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- NAKAMURA JOJI
- Pharmaceuticals Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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- HASHIZUME KAZUKO
- Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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- GOTO JOJI
- Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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- KUBO KAZUHIRO
- Pharmaceuticals Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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- SHUTO KATSUICHI
- Pharmaceuticals Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
抄録
Streptomyces gabonae KY2234 was found to produce a new compound, MY336-a, which bound to β-adrenergic receptor. The compound was isolated from the fermentation broth of KY2234. MY336-a showed a high affinity for the β-receptor, labeled with [3H]dihydroalprenolol in the membrane fractions of rat heart (β1-adrenergic receptor) or lung (β2-adrenergic receptor), whereas the compound bound very weakly to α-adrenergic receptor, labeled with [3H]dihydroergokryptine in rat brain. The inhibition constants (Ki) of the compound were 0.73 and 0.14 μM for the β-receptors of heart and lung, respectively. 5'-Guanylylimidodiphosphate (Gpp(NH)p) did not alter the affinity of the β-receptors for MY336-a. In isolated guinea-pig atria, MY336-a produced an inhibition of the positive chronotropic and inotropic effects of isoproterenol. MY336-a also antagonized the relaxation of tone induced by isoproterenol in isolated guinea-pig trachea. No partial agonistic activity was detected in MY336-a in the isolated atria and trachea. In anaesthetized dogs, MY336-a (1 mg/kg, iv) exerted negative inotropic action (left ventricular dp/dt max, -32.6%).
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 39 (3), 354-363, 1986
公益財団法人 日本感染症医薬品協会
