Miyamoto A, Kowatch M A, Roth G S
Department of Pharmacology, Sapporo Medical College, Japan.
Exp Gerontol. 1993 Jul-Oct;28(4-5):349-59. doi: 10.1016/0531-5565(93)90062-i.
The effects of the nonionic detergent saponin on alpha 1-adrenergic signal transduction were investigated using rat parotid cells and membrane preparations. Fifty microM epinephrine-stimulated 45Ca2+ efflux and inositol 1,4,5-triphosphate (Ins[1,4,5]P3) production in adult parotid cells were significantly decreased after saponin treatment. Saponin did not alter the concentration of alpha 1-adrenergic receptors labeled by [3H]prazosin, but significantly reduced the guanosine imido diphosphate (GppNHp)-induced shift from high to low affinity sites. Fifty microM epinephrine-stimulated high affinity GTPase activity was also reduced by saponin treatment. These data suggest that reduced alpha 1-adrenergic receptor-stimulated functional responsiveness following saponin treatment may be due to impaired uncoupling of receptor-G-protein complexes.
使用大鼠腮腺细胞和膜制剂研究了非离子去污剂皂角苷对α1-肾上腺素能信号转导的影响。皂角苷处理后,50微摩尔肾上腺素刺激的成年腮腺细胞中45Ca2+外流和肌醇1,4,5-三磷酸(Ins[1,4,5]P3)生成显著降低。皂角苷未改变[3H]哌唑嗪标记的α1-肾上腺素能受体浓度,但显著降低了鸟苷亚氨基二磷酸(GppNHp)诱导的从高亲和力位点到低亲和力位点的转变。50微摩尔肾上腺素刺激的高亲和力GTP酶活性也因皂角苷处理而降低。这些数据表明,皂角苷处理后α1-肾上腺素能受体刺激的功能反应性降低可能是由于受体-G蛋白复合物解偶联受损所致。