苯并噻二嗪TAG对哺乳动物甘氨酸受体通道激活的影响。

Effects of the benzothiadiazine TAG on channel activation at mammalian glycine receptors.

作者信息

Mathers D A

机构信息

Department of Physiology, University of British Columbia, Vancouver, Canada.

出版信息

Neurosci Lett. 1993 Jan 4;149(1):23-6. doi: 10.1016/0304-3940(93)90338-l.

DOI:10.1016/0304-3940(93)90338-l

PMID:8385751

Abstract

The effects of the benzothiadiazine TAG on membrane channels activated by taurine and glycine were investigated in dissociated spinal cord neurons from embryonic mice. TAG (100-200 microM) dose-dependently and reversibly antagonized the ability of glycine and taurine to activate chloride permeable ionic channels in these patches. This effect of TAG was due to shortening of the mean open time of the glycine and taurine activated channels. In addition, TAG significantly increased the mean shut time of taurine activated channels. The mean amplitude single channel currents activated by either agonist was unaltered by TAG. Single channel currents activated by taurine were significantly more sensitive to the blocking action of TAG than currents activated by glycine.

摘要

在来自胚胎小鼠的离体脊髓神经元中，研究了苯并噻二嗪TAG对由牛磺酸和甘氨酸激活的膜通道的影响。TAG（100 - 200微摩尔）以剂量依赖性和可逆的方式拮抗甘氨酸和牛磺酸在这些膜片中激活氯离子通透离子通道的能力。TAG的这种作用是由于缩短了甘氨酸和牛磺酸激活通道的平均开放时间。此外，TAG显著增加了牛磺酸激活通道的平均关闭时间。两种激动剂激活的单通道电流的平均幅度未被TAG改变。牛磺酸激活的单通道电流比甘氨酸激活的电流对TAG的阻断作用更敏感。