Bräutigam M, Dreesen R, Flosbach C W, Herken H
Biochem Pharmacol. 1982 Apr 1;31(7):1279-82. doi: 10.1016/0006-2952(82)90016-8.
The DOPA-content in neuroblastoma clone N1E-115 is higher than the dopamine or noradrenaline content. Blockade of tyrosine hydroxylase by alpha-methyl-p-tyrosine (1 X 10(-3) M) resulted in a decrease of cellular DOPA-content to 24.9% after 4 hr. The accumulation of DOPA in these cells which is probably due to limited activity of l-aromatic amino acid decarboxylase led us to use DOPA-content as a measure of tyrosine hydroxylase (TH) activity. Dopamine and especially apomorphine were effective at low concentrations (dopamine IC50 1 X 10(-5) M, apomorphine 2 X 10(-7) M); lisuride had no effect on TH-activity. The low effective dose of apomorphine and the failure of lisuride to influence TH-activity are comparable to the observations in striatal synaptosomal preparations and make the N1E-115 clone a suitable model for studying the mechanism of TH-regulation. However, since haloperidol (1 X 10(-5) M) did not reverse the apomorphine-induced blockade of TH, a receptor-mediated blockade of TH seems to be improbable.
神经母细胞瘤克隆N1E-115中的多巴含量高于多巴胺或去甲肾上腺素含量。用α-甲基-对-酪氨酸(1×10⁻³M)阻断酪氨酸羟化酶后,4小时后细胞多巴含量降至24.9%。这些细胞中多巴的积累可能是由于L-芳香族氨基酸脱羧酶活性有限,这使我们将多巴含量用作酪氨酸羟化酶(TH)活性的指标。多巴胺尤其是阿扑吗啡在低浓度时有效(多巴胺IC50为1×10⁻⁵M,阿扑吗啡为2×10⁻⁷M);利苏瑞ide对TH活性没有影响。阿扑吗啡的低有效剂量以及利苏瑞ide对TH活性无影响与纹状体突触体制剂中的观察结果相似,这使得N1E-115克隆成为研究TH调节机制的合适模型。然而,由于氟哌啶醇(1×10⁻⁵M)不能逆转阿扑吗啡诱导的TH阻断,TH的受体介导阻断似乎不太可能。