Olpe H R, Baudry M, Jones R S
Eur J Pharmacol. 1985 Mar 26;110(1):71-80. doi: 10.1016/0014-2999(85)90030-5.
Carbamazepine moderately depressed the input fiber volley resulting in attenuation of the dendritic epsp and the population spike in CA1 of rat hippocampal slices with a threshold concentration of 20 microM. The depressant effect on the population spike was not antagonized by the adenosine receptor blocker caffeine. Paired-pulse inhibition was not affected by carbamazepine (40 microM). Epileptic-like rhythmic discharge of CA1 neurons in medium containing low Ca2+/high Mg2+ was attenuated at even lower concentrations of carbamazepine (8 microM) indicating that there was also a postsynaptic site of action. Imipramine being significantly more potent than carbamazepine in the rabbit corneal test for local anaesthetic activity had no effect on the population spike (20 microM). In neurochemical studies, carbamazepine reduced the [22Na]- and [3H]L-glutamate efflux induced by potassium and veratridine from hippocampal slices with a threshold concentration of 10 microM. The drug (400 microM) failed to affect Na+-dependent binding of [3H]L-glutamate to hippocampal synaptic membranes. In conclusion, the present findings demonstrate pre- and postsynaptic depressant actions of carbamazepine in CAI of hippocampus.
卡马西平可适度抑制传入纤维冲动,导致大鼠海马切片CA1区树突兴奋性突触后电位(epsp)和群体峰电位衰减,阈值浓度为20微摩尔。腺苷受体阻断剂咖啡因不能拮抗卡马西平对群体峰电位的抑制作用。卡马西平(40微摩尔)对双脉冲抑制无影响。在含有低钙/高镁的培养基中,即使在更低浓度的卡马西平(8微摩尔)作用下,CA1神经元的癫痫样节律性放电也会减弱,这表明还存在一个突触后作用位点。在兔角膜局部麻醉活性试验中,丙咪嗪的效力明显强于卡马西平,但对群体峰电位(20微摩尔)无影响。在神经化学研究中,卡马西平可降低钾离子和藜芦碱诱导的海马切片中[22Na] - 和[3H]L - 谷氨酸外流,阈值浓度为10微摩尔。该药物(400微摩尔)未能影响[3H]L - 谷氨酸与海马突触膜的钠离子依赖性结合。总之,目前的研究结果表明卡马西平在海马CA1区具有突触前和突触后抑制作用。