Turkanis S A, Karler R
Department of Pharmacology, University of Utah School of Medicine, Salt Lake City 84132.
Neuropharmacology. 1988 Jul;27(7):737-42. doi: 10.1016/0028-3908(88)90083-4.
In vitro intracellular recording techniques were used on an excitatory neuromuscular junction of a walking-limb stretcher muscle of the lobster in order to define the synaptic pharmacology of delta-9-tetrahydrocannabinol (THC), 11-hydroxy-THC and cannabidiol. Delta-9-tetrahydrocannabinol and 11-hydroxy-THC, in relatively small concentrations, increased the amplitude of the excitatory junctional potential and the mean quantum content of a muscle fiber, whereas larger concentrations produced depression. In contrast, cannabidiol reduced the excitatory junctional potential and the mean quantum content. All three cannabinoids, however, depressed the amplitude of the spontaneous miniature junctional potential. The changes in mean quantum content point to a presynaptic site of action for the drug, while the reduction of the amplitude of the miniature junctional potential presumes a postsynaptic site. Such findings suggest synaptic mechanisms and sites of action for the central excitatory and depressant properties of the cannabinoids.
为了确定δ-9-四氢大麻酚(THC)、11-羟基-THC和大麻二酚的突触药理学,研究人员对龙虾步行肢伸展肌的兴奋性神经肌肉接头进行了体外细胞内记录技术实验。相对低浓度的δ-9-四氢大麻酚和11-羟基-THC可增加兴奋性接头电位的幅度和肌肉纤维的平均量子含量,而较高浓度则会产生抑制作用。相比之下,大麻二酚降低了兴奋性接头电位和平均量子含量。然而,所有三种大麻素都会降低自发性微小接头电位的幅度。平均量子含量的变化表明药物作用于突触前位点,而微小接头电位幅度的降低则推测作用于突触后位点。这些发现提示了大麻素中枢兴奋和抑制特性的突触机制及作用位点。