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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >In-vitro characterization of the pharmacological effects induced by (-)-α-bisabolol in rat smooth muscle preparations
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In-vitro characterization of the pharmacological effects induced by (-)-α-bisabolol in rat smooth muscle preparations

机译：（-）-α-bisabolol在大鼠平滑肌制剂中诱导的药理作用的体外表征

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摘要

The present study deals with the pharmacological effects of the sesquiterpene alcohol (-)-a-bisabolol on various smooth-muscle preparations from rats. Under resting tonus, (-)-α-bisabolol (30-300 μmol/L) relaxed duodenal strips, whereas it showed biphasic effects in other preparations, contracting endothelium-intact aortic rings and urinary bladder strips, and relaxing these tissues at higher concentrations (600-1000 μmol/L). In preparations precontracted either electromechanically (by 60 mmol/L K +) or pharmacomechanically (by phenylephrine or carbachol), (-)-α-bisabolol showed only relaxing properties. The pharmacological potency of (-)-α-bisabolol was variable, being higher in mesenteric vessels, whereas it exerted relaxing activity with a lesser potency on tracheal or colonic tissues. In tissues possessing spontaneous activity, (-)-α-bisabolol completely decreased spontaneous contractions in duodenum, whereas it increased their amplitude in urinary bladder tissue. Administered in vivo, (-)-α-bisabolol attenuated the increased responses of carbachol in tracheal rings of ovalbumin-sensitized rats challenged with ovalbumin, but was without effect in the decreased responsiveness of urinary bladder strips in mice treated with ifosfamide. In summary, (-)-α-bisabolol is biologically active in smooth muscle. In some tissues, (-)-α-bisabolol preferentially relaxed contractions induced electromechanically, especially in tracheal smooth muscle. The findings from tracheal rings reveal that (-)-α-bisabolol may be an inhibitor of voltage-dependent Ca 2+ channels.
机译：本研究涉及倍半萜醇（-）-α-bisabolol对大鼠各种平滑肌制剂的药理作用。在静息张力下，（-）-α-bisabolol（30-300μmol/ L）舒张十二指肠条带，而在其他制剂中则显示双相效应，收缩内皮完整的主动脉环和膀胱条带，并在较高浓度下放松这些组织（600-1000μmol/ L）。在机电（通过60 mmol / L K +）或药理（通过去氧肾上腺素或卡巴胆碱）进行预收缩的制剂中，（-）-α-bisabolol仅显示松弛特性。 （-）-α-bisabolol的药理作用是可变的，在肠系膜血管中较高，而在气管或结肠组织上则表现出松弛作用，但效力较低。在具有自发活性的组织中，（-）-α-bisabolol完全减少了十二指肠的自发收缩，而在膀胱组织中却增加了其幅度。在体内给药时，（-）-α-bisabolol减弱了用卵白蛋白攻击的卵白蛋白致敏大鼠的气管环中卡巴胆碱的增加反应，但对异环磷酰胺治疗的小鼠尿路膀胱条的反应性降低没有影响。总之，（-）-α-bisabolol在平滑肌中具有生物活性。在某些组织中，（-）-α-bisabolol优先以机电方式放松收缩，特别是在气管平滑肌中。气管环的发现表明（-）-α-bisabolol可能是电压依赖性Ca 2+通道的抑制剂。

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