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大鼠心脏和唾液腺中去甲肾上腺素外排的调节。

Regulation of metaraminol efflux from rat heart and salivary gland.

作者信息

Costa E, Neff N H, Ngai S H

出版信息

Br J Pharmacol. 1969 May;36(1):153-60. doi: 10.1111/j.1476-5381.1969.tb08312.x.

Abstract
  1. The turnover rate of noradrenaline (NA) in heart and submaxillary salivary gland was studied in rats exposed to 4 degrees C or maintained at room temperature (22 degrees C). Cold exposure increased the turnover of the NA store in heart but not in salivary gland.2. In another series of experiments the decline of metaraminol (M) from heart and submaxillary salivary gland was studied in rats exposed to 4 degrees C or maintained at room temperature. Cold exposure accelerated the efflux of M from heart, but not from salivary gland. It is concluded that the accelerated decline of M from heart is the consequence of selective activation of the sympathetic nerves that innervate the heart.3. The turnover of NA was studied in rat heart after the administration of M (100 mug/kg intravenously) or its precursor alpha-methyl-meta-tyrosine (200 mg/kg intraperitoneally). Turnover remained essentially normal after these drugs.4. The administration of desipramine (DMI, 20 mg/kg intraperitoneally) 1 hr after M (100 mug/kg intravenously) induced a rapid sustained efflux of M from heart and salivary gland. The results of this study suggest that the slow decline of M from heart is the result of the great affinity of the amine retrieval mechanism in sympathetic nerve endings for M. DMI inhibits the retrieval mechanism, thus accelerating the efflux of M.
摘要
  1. 研究了暴露于4℃或维持在室温(22℃)的大鼠心脏和颌下唾液腺中去甲肾上腺素(NA)的周转率。冷暴露增加了心脏中NA储备的周转率,但唾液腺中的未增加。

  2. 在另一系列实验中,研究了暴露于4℃或维持在室温的大鼠心脏和颌下唾液腺中甲胺唑啉(M)的减少情况。冷暴露加速了心脏中M的外流,但唾液腺中的未加速。得出结论,心脏中M加速减少是支配心脏的交感神经选择性激活的结果。

  3. 在静脉注射M(100μg/kg)或其前体α-甲基-间酪氨酸(200mg/kg腹腔注射)后,研究了大鼠心脏中NA的周转率。这些药物给药后周转率基本保持正常。

  4. 在静脉注射M(100μg/kg)1小时后腹腔注射地昔帕明(DMI,20mg/kg),诱导心脏和唾液腺中M快速持续外流。本研究结果表明,心脏中M缓慢减少是交感神经末梢胺摄取机制对M具有高亲和力的结果。DMI抑制摄取机制,从而加速M的外流。

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