Patterson T A, Eppler B, Dawson R
Department of Pharmacodynamics, College of Pharmacy, University of Florida, JHMHC, Gainesville 32610, USA.
Neurotoxicol Teratol. 1996 Nov-Dec;18(6):697-702. doi: 10.1016/s0892-0362(96)00132-8.
Trimethyltin (TMT) is a toxic alkyltin that produces neuronal necrosis in the CNS. TMT stimulates the efflux of the excitatory amino acid glutamate (GLU) from rat cortical slices. This release is concentration dependent, partially calcium dependent, but not inhibited by calcium channel blockers or a NMDA antagonist. In the present study the compounds furosemide, bumetanide, 4,4'-diisothiocy-anatostilbene-2,2'-disulfonic acid (DIDS), and DL-threo-beta-hydroxyaspartic acid (HAA) were tested for their ability to attenuate TMT-stimulated GLU efflux from rat cortical and hippocampal slices. Furosemide (1 mM) reduced the TMT-induced GLU efflux in cortical slices and hippocampal slices, but bumetanide (0.1 mM) had no effect on TMT-induced GLU efflux. DIDS (1 mM) demonstrated a trend toward decreasing GLU efflux from TMT stimulation in both the cortex and hippocampus, but this reduction was not significant. However, DIDS was able to prevent the decrease in intracellular GLU content produced by TMT in both the cortical and hippocampal slices. HAA (1 mM) increased the net GLU efflux in both cortical slices and hippocampal slices, and produced a significant depletion of the glutamate content of the slices. Taurine efflux was stimulated by TMT treatment but was not blocked by the chloride transport inhibitors. These data suggest that cell swelling-induced release of GLU may not be directly involved in TMT-induced GLU efflux, and that TMT does not appear to elicit GLU efflux by a mechanism involving reversal of the GLU transporter.
三甲基锡(TMT)是一种有毒的烷基锡,可在中枢神经系统中导致神经元坏死。TMT可刺激大鼠皮质切片中兴奋性氨基酸谷氨酸(GLU)的外流。这种释放是浓度依赖性的,部分依赖于钙,但不受钙通道阻滞剂或NMDA拮抗剂的抑制。在本研究中,测试了呋塞米、布美他尼、4,4'-二异硫氰酸根合芪-2,2'-二磺酸(DIDS)和DL-苏式-β-羟基天冬氨酸(HAA)减弱TMT刺激大鼠皮质和海马切片中GLU外流的能力。呋塞米(1 mM)可减少皮质切片和海马切片中TMT诱导的GLU外流,但布美他尼(0.1 mM)对TMT诱导的GLU外流无影响。DIDS(1 mM)在皮质和海马中均显示出降低TMT刺激引起的GLU外流的趋势,但这种降低并不显著。然而,DIDS能够防止TMT在皮质和海马切片中引起的细胞内GLU含量的降低。HAA(1 mM)增加了皮质切片和海马切片中的净GLU外流,并导致切片中谷氨酸含量显著减少。TMT处理可刺激牛磺酸外流,但不受氯离子转运抑制剂的阻断。这些数据表明,细胞肿胀诱导的GLU释放可能不直接参与TMT诱导的GLU外流,并且TMT似乎不是通过涉及GLU转运体逆转的机制引发GLU外流。