鸟苷酸对脑组织和连续细胞系中CCKB受体结合的影响：一项比较研究。

Effects of guanyl nucleotides on CCKB receptor binding in brain tissue and continuous cell lines: a comparative study.

作者信息

Kaufmann R, Schöneberg T, Henklein P, Meyer R, Martin H, Ott T

机构信息

Friedrich-Schiller-University Jena, Germany.

出版信息

Neuropeptides. 1995 Jul;29(1):63-8. doi: 10.1016/0143-4179(95)90058-6.

DOI:10.1016/0143-4179(95)90058-6

PMID:7566515

Abstract

The effects of non-hydrolyzable guanyl nucleotide analogue GTP-gamma S on CCKB receptor binding in human and guinea-pig cortex, Jurkat T-cells, rat pituitary GH3 cells, rat glioma C6 cells and human small cell lung cancer NCI-H69 cells were investigated by using [3H]CCK-8S saturation and competition binding studies. GTP-gamma S caused inhibition of specific [3H]CCK-8S binding in a concentration dependent manner with a plateau at 10-25 microM. 25 microM GTP-gamma S resulted in a small but significant increase in Kd and IC50 values with amount very similar in all CCKB receptor models tested. However, the maximal number of specific [3H]CCK-8S binding sites (Bmax) was unaffected. Results suggest that CCKB receptors are G-protein coupled in a similar way to human and guinea-pig cortex, Jurkat cells, GH3 cells, C6 cells and NCI-H69 cells.

摘要

采用[3H]CCK-8S饱和结合和竞争结合研究，考察了不可水解的鸟苷酸类似物GTP-γ-S对人及豚鼠皮层、Jurkat T细胞、大鼠垂体GH3细胞、大鼠胶质瘤C6细胞和人小细胞肺癌NCI-H69细胞中CCKB受体结合的影响。GTP-γ-S以浓度依赖的方式抑制特异性[3H]CCK-8S结合，在10 - 25μM时达到平台期。25μM GTP-γ-S导致Kd和IC50值有小幅但显著的增加，在所测试的所有CCKB受体模型中增加幅度非常相似。然而，特异性[3H]CCK-8S结合位点的最大数量（Bmax）未受影响。结果表明，CCKB受体与人类和豚鼠皮层、Jurkat细胞、GH3细胞、C6细胞和NCI-H69细胞中的G蛋白偶联方式相似。