Sewell R D, Tan K S, Roth S H
Eur J Pharmacol. 1984 Jun 15;102(1):71-8. doi: 10.1016/0014-2999(84)90339-x.
On the stretch-induced discharge activity of the isolated crayfish sensory neuron flurazepam (less than or equal to 3 X 10(-4) M) and Ro 15-1788 (less than or equal to 10(-3) M) produced reversible concentration-dependent excitation, but oxazepam only produced depression (less than or equal to 5 X 10(-4) M). Similar divergent effects on the membrane properties were observed. Oxazepam increased the threshold to firing without changing resting potential, membrane resistance or the GABA-mediated IPSP. In contrast flurazepam and Ro 15-1788 produced a concentration-dependent decrease in threshold. Flurazepam did not alter membrane resistance or resting potential but facilitated GABA transmission. Ro 15-1788 had the opposite effect on the GABA synapse, and also depolarized the resting potential but did not alter membrane resistance. The change in spike threshold appeared to be an important component in producing discharge excitation or depression. These results not only demonstrate the capability of the sensory neuron to discriminate between structures of benzodiazepines, but also that these agents can produce divergent effects on synaptic and non-synaptic properties of a single neuron.
关于离体小龙虾感觉神经元的牵张诱导放电活动,氟硝西泮(≤3×10⁻⁴ M)和Ro 15 - 1788(≤10⁻³ M)产生可逆的浓度依赖性兴奋,但奥沙西泮仅产生抑制作用(≤5×10⁻⁴ M)。在膜特性方面也观察到类似的不同效应。奥沙西泮提高了放电阈值,而不改变静息电位、膜电阻或GABA介导的抑制性突触后电位(IPSP)。相比之下,氟硝西泮和Ro 15 - 1788使阈值呈浓度依赖性降低。氟硝西泮不改变膜电阻或静息电位,但促进GABA传递。Ro 15 - 1788对GABA突触有相反的作用,并且使静息电位去极化,但不改变膜电阻。动作电位阈值的变化似乎是产生放电兴奋或抑制的一个重要因素。这些结果不仅证明了感觉神经元区分苯二氮䓬类结构的能力,还表明这些药物可对单个神经元的突触和非突触特性产生不同的影响。