Pacheco M A, Ward S J, Childers S R
Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Winston-Salem, NC 27157.
Brain Res. 1993 Feb 12;603(1):102-10. doi: 10.1016/0006-8993(93)91304-b.
G protein-linked cannabinoid receptors are present in high density in cerebellum, where they inhibit adenylyl cyclase. This study explored whether cannabinoid receptors are co-localized with GABAB receptors on cerebellar granule cells. In rat cerebellar membranes, receptor-coupled G protein function was assayed by agonist stimulation of low Km GTPase as well as agonist-inhibited adenylyl cyclase. Addition of cannabinoid agonists together with the GABAB agonist, baclofen, produced additive responses with stimulation of low Km GTPase but only partially additive responses with inhibition of adenylyl cyclase. In Weaver and Staggerer but not Nervous mutant mice, cannabinoid-inhibited adenylyl cyclase was significantly decreased in cerebellar but not striatal membranes compared to littermate controls. In primary cultures of rat cerebellar granule cells, cannabinoids inhibited forskolin-stimulated cAMP levels, with IC50 values ranging from 0.1 to 2.0 microM. Cannabinoid inhibition of intracellular cAMP levels was blocked by pretreatment of cell cultures with pertussis toxin. Addition of baclofen and cannabinoid agonists together in cultured granule cells produced no additivity in response for inhibition of intracellular cAMP levels. These data confirm that G protein-linked cannabinoid receptors are present in cerebellar granule cells and may share adenylyl cyclase catalytic units with GABAB receptors.
G蛋白偶联大麻素受体在小脑中有高密度表达,在那里它们抑制腺苷酸环化酶。本研究探讨了大麻素受体是否与小脑颗粒细胞上的GABAB受体共定位。在大鼠小脑膜中,通过低Km GTP酶的激动剂刺激以及激动剂抑制的腺苷酸环化酶来测定受体偶联的G蛋白功能。将大麻素激动剂与GABAB激动剂巴氯芬一起添加,在刺激低Km GTP酶时产生相加反应,但在抑制腺苷酸环化酶时仅产生部分相加反应。与同窝对照相比,在韦弗和蹒跚小鼠而非神经突变小鼠中,大麻素抑制的腺苷酸环化酶在小脑膜中显著降低,但在纹状体膜中未降低。在大鼠小脑颗粒细胞的原代培养物中,大麻素抑制福斯高林刺激的cAMP水平,IC50值范围为0.1至2.0 microM。用百日咳毒素预处理细胞培养物可阻断大麻素对细胞内cAMP水平的抑制作用。在培养的颗粒细胞中一起添加巴氯芬和大麻素激动剂,对抑制细胞内cAMP水平的反应未产生相加作用。这些数据证实G蛋白偶联大麻素受体存在于小脑颗粒细胞中,并且可能与GABAB受体共享腺苷酸环化酶催化单元。