Stereospecificity of the anti-inflammatory actions of terbutaline.

D E Dobbins, M J Buehn, J M Dabney
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Abstract

Intra-arterial infusion of a racemic mixture of the beta 2-agonist terbutaline blocks histamine-mediated increases in lymph flow and protein concentration in the canine forelimb. In the current study we have assessed the relative anti-inflammatory potencies of the purified stereoisomers of terbutaline. Infusion of histamine (4 micrograms base/min) increased lymph flow, protein concentration and protein transport. The intra-arterial infusion of 1-terbutaline (1 microgram/min) significantly decreased forelimb arterial pressures and prevented any changes in lymph parameters due to subsequent histamine infusion. Intra-arterial infusion of d-terbutaline (1 microgram/min) did not significantly affect forelimb vascular pressures but subsequent to histamine administration, lymph parameters increased similar to that seen with histamine alone. Infusion of a high dose of d-terbutaline (100 micrograms/min) slightly decreased forelimb arterial pressures but failed to inhibit histamine-mediated increases in lymph parameters. Infusion of 1-terbutaline alone (1 microgram/min) significantly decreased forelimb arterial pressures, lymph flow and protein transport and slightly but significantly increased lymph protein concentration. These data indicate that the beta 2-agonistic and anti-inflammatory properties of terbutaline are confined solely to the levorotatory enantiomer.

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特布他林抗炎作用的立体特异性。
动脉内输注β 2-激动剂特布他林外消旋混合物阻断组胺介导的犬前肢淋巴流量和蛋白质浓度的增加。在目前的研究中,我们已经评估了纯化的特布他林立体异构体的相对抗炎能力。输注组胺(4微克碱基/分钟)增加淋巴流量、蛋白质浓度和蛋白质运输。动脉内输注1-特布他林(1微克/分钟)可显著降低前肢动脉压,并防止后续组胺输注引起的淋巴参数变化。动脉内输注d-特布他林(1微克/分钟)对前肢血管压力没有显著影响,但组胺给药后,淋巴参数增加,与单独使用组胺相似。输注高剂量d-特布他林(100微克/分钟)可轻微降低前肢动脉压,但无法抑制组胺介导的淋巴参数升高。单独输注1-特布他林(1微克/分钟)可显著降低前肢动脉压、淋巴流量和蛋白转运,并可显著升高淋巴蛋白浓度。这些数据表明,特布他林的β 2激动和抗炎特性仅限于左旋对映体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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