Carswell H, Galione A G, Young J M
Br J Pharmacol. 1987 Jan;90(1):175-82. doi: 10.1111/j.1476-5381.1987.tb16838.x.
Slices of guinea-pig cerebral cortex were incubated with [3H]-inositol at 37 degrees C before exposure to histamine or carbachol at 37 degrees C or 25 degrees C. Histamine-stimulated accumulation of [3H]-inositol 1-phosphate ([3H]-IP1) at 25 degrees C was only 5-7% of that at 37 degrees C, whereas for carbachol the response at 25 degrees C was 45-49% of that at 37 degrees C. The affinity of benzilylcholine, obtained from inhibition of carbachol-induced accumulation of [3H]-IP1 was similar at 25 degrees C and 37 degrees C, but the EC50 for carbachol was lower at 25 degrees C (20 +/- 2 microM) than at 37 degrees C (42 +/- 2 microM). The IC50 for histamine inhibition of [3H]-mepyramine binding to homogenates of guinea-pig cerebral cortex did not differ significantly at 25 degrees C and 37 degrees C. Histamine-induced accumulations of [3H]-IP2 and [3H]-IP3 at 25 degrees C, expressed as a percentage of the accumulation at 37 degrees C, were also much less than the corresponding value for carbachol. These observations imply that the locus or pathway(s) of agonist-induced formation of [3H]-IP1 are not the same for histamine and carbachol.
将豚鼠大脑皮层切片在37℃下与[3H]-肌醇一起孵育,然后在37℃或25℃下暴露于组胺或卡巴胆碱。在25℃下,组胺刺激的[3H]-肌醇1-磷酸([3H]-IP1)积累量仅为37℃下的5 - 7%,而对于卡巴胆碱,25℃下的反应是37℃下的45 - 49%。从抑制卡巴胆碱诱导的[3H]-IP1积累获得的苄基胆碱亲和力在25℃和37℃下相似,但卡巴胆碱的EC50在25℃(20±2 microM)低于37℃(42±2 microM)。组胺抑制[3H]-美吡拉敏与豚鼠大脑皮层匀浆结合的IC50在25℃和37℃下无显著差异。在25℃下,组胺诱导的[3H]-IP2和[3H]-IP3积累量,以其在37℃下积累量的百分比表示,也远低于卡巴胆碱的相应值。这些观察结果表明,组胺和卡巴胆碱激动剂诱导形成[3H]-IP1的位点或途径不同。