INTRINSIC β-SYMPATHOMIMETIC ACTIVITY OF DILEVALOL, R, RISOMER OF LABETALOL
スポンサーリンク
概要
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The potency and selectivity of the intrinsic β-sympathomimetic activity (ISA) of dilevalol were studied with isolated guinea-pig trachea and pithed rat. This drug relaxed the contracture of isolated guinea-pig tracheal preparation induced by histamine in a dosedependent manner. The dose-response curves of dilevalol and labetalol were shifted to the right with propranolol pretreatment. The relaxing potency of dilevalol was approximately 4.7 times more potent than that of labetalol. Dilevalol markedly reduced the diastolic blood pressure with only a slight increase of heart rate in pithed rats, while isoproterenol and pindolol caused moderate to marked positive chronotropic effects in proportion to their hypotensive effects. These results suggest that dilevalol has more potent ISA than labetalol and shows more β_2-adrenoceptor selectivity than pindolol.
- 公益社団法人日本薬学会の論文
著者
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Ueda Motohiko
Department Of Pharmacology Shionogi Research Laboratories Shionogi & Co. Ltd.
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MATSUNAGA Kazuki
Department of Pharmacology, Shionogi Research Laboratories, Shionogi & Co., Ltd.
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NAKAMURA KIMIKO
Department of Pharmacology, Shionogi Research Laboratories, Shionogi & Co., Ltd.
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Nakamura Kimiko
Department Of Pharmacology Shionogi Research Laboratories Shionogi & Co. Ltd.
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Matsunaga Kazuki
塩野義製薬
関連論文
- EFFECTS OF d-AND I-PROPRANOLOL ON THE ACUTE HYPOTENSION INDUCED BY PINDOLOL IN CONSCIOUS SPONTANEOUSLY HYPERTENSIVE RATS (SHR)
- INTRINSIC β-SYMPATHOMIMETIC ACTIVITY OF DILEVALOL, R, RISOMER OF LABETALOL
- SUBSTANCE P IN THE CENTRAL NERVOUS SYSTEM OF RABBITS : UPTAKE SYSTEM DIFFERS FROM PUTATIVE TRANSMITTERS
- Subacute studies on hemodynamic effects of propranolol in conscious spontaneously hypertensive rats (SHR).
- Actions of a newly synthesized compound (711389-S) on various types of experimentally induced arrhythmias in mammalian species in situ.
- Acute Tolerance to the Hypotensive Effect of Pindolol in Conscious SHR