吩噻嗪对激素敏感型腺苷酸环化酶的抑制作用。
Inhibition of hormone-sensitive adenyl cyclase by phenothiazines.
作者信息
Wolff J, Jones A B
出版信息
Proc Natl Acad Sci U S A. 1970 Feb;65(2):454-9. doi: 10.1073/pnas.65.2.454.
Chlorpromazine (3 x 10(-4)M) prevents the stimulation of adenyl cyclase activity in thyroid membranes produced by thyrotropin and prostaglandin, ACTH stimulation of adenyl cyclase in adrenal tissue, and glucagon- and epinephrine-stimulation of adenyl cyclase activity in liver. Baseline activity is unaffected. Parathyroid hormone stimulation of kidney preparations was not inhibited under these conditions. At chlorpromazine concentrations >3 x 10(-4)M F(-)-stimulated cyclase activity of thyroid and adrenal tissue was increased. Other phenothiazines, trifluoperazine, and prochlorperazine, have similar effects on thyrotropin and F(-)-stimulated cyclase activity of thyroid. Na(+)- K(+)-dependent ATPase of thyroid is also inhibited by chlorpromazine. Since thymol causes a similar dissociation of hormone- and F(-)-stimulated adenyl cyclase, it is concluded that the surface properties of these agents best account for their effects on adenyl cyclase.
氯丙嗪（3×10⁻⁴M）可抑制促甲状腺激素和前列腺素对甲状腺膜中腺苷酸环化酶活性的刺激、促肾上腺皮质激素对肾上腺组织中腺苷酸环化酶的刺激，以及胰高血糖素和肾上腺素对肝中腺苷酸环化酶活性的刺激。基线活性不受影响。在这些条件下，甲状旁腺激素对肾制剂的刺激未被抑制。当氯丙嗪浓度>3×10⁻⁴M时，氟离子刺激的甲状腺和肾上腺组织的环化酶活性增加。其他吩噻嗪类药物，如三氟拉嗪和丙氯拉嗪，对促甲状腺激素和氟离子刺激的甲状腺环化酶活性有类似作用。氯丙嗪还可抑制甲状腺的钠钾依赖性ATP酶。由于百里酚对激素和氟离子刺激的腺苷酸环化酶有类似的解离作用，因此得出结论，这些药物的表面性质最能解释它们对腺苷酸环化酶的作用。
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