在中国仓鼠卵巢（CHO.A2B4）细胞中表达的人脑海马区假定A2B腺苷受体的特性分析
Characterization of the human brain putative A2B adenosine receptor expressed in Chinese hamster ovary (CHO.A2B4) cells.
作者信息
Alexander S P, Cooper J, Shine J, Hill S J
机构信息
Department of Physiology & Pharmacology, University of Nottingham Medical School, Queen's Medical Centre, U.K.
出版信息
Br J Pharmacol. 1996 Nov;119(6):1286-90. doi: 10.1111/j.1476-5381.1996.tb16035.x.
Abstract
- An [3H]-adenine pre-labelling methodology was employed to assay cyclic AMP generation by adenosine analogues in Chinese hamster ovary (CHO.A2B4) cells, transfected with cDNA which has been proposed to code for the human brain A2B adenosine receptor, and in guinea-pig cerebral cortical slices. 2. Adenosine analogues showing the following rank order of potency in the CHO.A2B4 cells (pD2 value): 5'-N-ethylcarboxamidoadenosine (NECA, 5.91) > adenosine (5.69) > 2-chloroadenosine (5.27) > N6-(2-(4-aminophenyl)-ethylamino)adenosine (APNEA, 4.06). The purportedly A2A-selective agonist, CGS 21680, failed to elicit a significant stimulation of cyclic AMP generation at concentrations up to 10 microM in CHO.A2B4 cells. In the guinea-pig cerebral cortex, NECA was more potent than APNEA with pD2 values of 5.91 and 4.60, respectively. 3. Of these agents, NECA was observed to exhibit the greatest intrinsic activity in CHO.A2B4 cells (ca. 10 fold stimulation of cyclic AMP), while, in comparison, maximal responses to adenosine (32% NECA response), 2-chloroadenosine (61%), and APNEA (73%) were reduced. 4. Antagonists of NECA-evoked cyclic AMP generation showed the rank order of apparent affinity (apparent pA2 value in CHO.A2B4 cells: guinea-pig cerebral cortex): XAC (7.89: 7.46) > CGS 15943 (7.75: 7.33) > DPCPX (7.16: 6.91) > PD 115,199 (6.95: 6.39) > 8FB-PTP (6.52: 6.55) > 3-propylxanthine (4.63: 4.59). 5. We conclude that, using the agents tested, the A2B adenosine receptor cloned from human brain expressed in Chinese hamster ovary cells exhibits an identical pharmacological profile to native A2B receptors in guinea-pig brain.
摘要
- 采用[3H] - 腺嘌呤预标记方法，检测转染了据推测编码人脑A2B腺苷受体的cDNA的中国仓鼠卵巢（CHO.A2B4）细胞以及豚鼠大脑皮层切片中腺苷类似物诱导的环磷酸腺苷（cAMP）生成。2. 腺苷类似物在CHO.A2B4细胞中显示出以下效价顺序（pD2值）：5'-N - 乙基甲酰胺基腺苷（NECA，5.91）＞腺苷（5.69）＞2 - 氯腺苷（5.27）＞N6 - （2 - （4 - 氨基苯基） - 乙氨基）腺苷（APNEA，4.06）。所谓的A2A选择性激动剂CGS 21680，在CHO.A2B4细胞中浓度高达10μM时未能显著刺激cAMP生成。在豚鼠大脑皮层中，NECA比APNEA更有效，pD2值分别为5.91和4.60。。3. 在这些试剂中，观察到NECA在CHO.A2B4细胞中表现出最大的内在活性（约10倍刺激cAMP），而相比之下，对腺苷（NECA反应的32%）、2 - 氯腺苷（61%）和APNEA（73%）的最大反应降低。4. NECA诱导的cAMP生成的拮抗剂显示出明显亲和力的顺序（CHO.A2B4细胞中的表观pA2值：豚鼠大脑皮层）：XAC（7.89:7.46）＞CGS 15943（7.75:7.33）＞DPCPX（7.16:6.91）＞PD 115,199（6.95:6.39）＞8FB - PTP（6.52:6.55）＞3 - 丙基黄嘌呤（4.63:4.59）。5. 我们得出结论，使用所测试的试剂，在中国仓鼠卵巢细胞中表达的从人脑中克隆的A2B腺苷受体表现出与豚鼠脑中天然A2B受体相同的药理学特征。
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