Balmforth A J, Ball S G, Freshney R I, Graham D I, McNamee H B, Vaughan P F
J Neurochem. 1986 Sep;47(3):715-9. doi: 10.1111/j.1471-4159.1986.tb00670.x.
Clones have been isolated from the human astrocytoma cell line G-CCM. Homogenates of clone D384 contain an adenylate cyclase that is stimulated by 3,4-dihydroxyphenylethylamine (dopamine), noradrenaline, and isoprenaline with Ka apparent values of 4, 56, and 2.7 microM, respectively. The Ka apparent value for dopamine was increased by the D-1 antagonist cis-flupenthixol, 25 and 100 nM, to 23 and 190 microM, respectively, but was unaffected by propranolol (1 microM). Noradrenaline stimulation of adenylate cyclase was only partially inhibited by either propranolol (10 microM) or cis-flupenthixol (1 microM). Propranolol (10 microM), but not cis-flupenthixol (1 microM), prevented stimulation by isoprenaline. The stimulation of adenylate cyclase by dopamine and noradrenaline remained unchanged in the presence of phentolamine (1 microM) and sulpiride (1 microM). These results suggest that clone D384 contains both D-1 dopaminergic and beta-adrenergic receptors coupled to adenylate cyclase. Dopamine stimulates D384 adenylate cyclase through D-1 receptors, isoprenaline via beta-receptors, and noradrenaline through both receptors.
已从人星形细胞瘤细胞系G - CCM中分离出克隆。克隆D384的匀浆含有一种腺苷酸环化酶,该酶受3,4 - 二羟基苯乙胺(多巴胺)、去甲肾上腺素和异丙肾上腺素刺激,其表观解离常数(Ka)值分别为4、56和2.7微摩尔。多巴胺的表观解离常数(Ka)值在加入D - 1拮抗剂顺式氟哌噻吨(25和100纳摩尔)后分别增加到23和190微摩尔,但不受普萘洛尔(1微摩尔)影响。去甲肾上腺素对腺苷酸环化酶的刺激仅被普萘洛尔(10微摩尔)或顺式氟哌噻吨(1微摩尔)部分抑制。普萘洛尔(10微摩尔)而非顺式氟哌噻吨(1微摩尔)可阻止异丙肾上腺素的刺激作用。在酚妥拉明(1微摩尔)和舒必利(1微摩尔)存在的情况下,多巴胺和去甲肾上腺素对腺苷酸环化酶的刺激作用保持不变。这些结果表明,克隆D384含有与腺苷酸环化酶偶联的D - 1多巴胺能受体和β - 肾上腺素能受体。多巴胺通过D - 1受体刺激D384腺苷酸环化酶,异丙肾上腺素通过β受体,而去甲肾上腺素则通过两种受体。