Fowler C J, Thorell G, Ogren S O
Research and Development Laboratories, Astra Alab AB, Södertälje, Sweden.
J Pharm Pharmacol. 1987 Dec;39(12):1015-8. doi: 10.1111/j.2042-7158.1987.tb03150.x.
The effect of alaproclate in carbachol-stimulated inositol phospholipid (PI) breakdown in rat cerebral cortical miniprisms has been investigated. Carbachol-stimulated PI breakdown was greatly enhanced by increasing the assay potassium concentration from 5.88 to 18.2 mM. Alaproclate, on the other hand, did not influence carbachol-stimulated PI breakdown over the concentration range tested (0-100 microM) at either assay [K+]. The elution pattern of the inositol phosphates from the Dowex-1 columns was also unaffected by alaproclate both in the absence and presence of carbachol. Thus, the potentiation by alaproclate of tremor and salivation induced by the muscarinic agonist oxotremorine in-vivo reported previously is not seen when muscarinic function is measured in-vitro using carbachol-stimulated PI breakdown.
研究了阿扑氯氮对卡巴胆碱刺激大鼠大脑皮质微小切片中肌醇磷脂(PI)分解的影响。将测定钾浓度从5.88 mM提高到18.2 mM可极大增强卡巴胆碱刺激的PI分解。另一方面,在任一测定[K+]条件下,在所测试的浓度范围(0 - 100 μM)内,阿扑氯氮均不影响卡巴胆碱刺激的PI分解。无论有无卡巴胆碱,阿扑氯氮对从Dowex - 1柱上洗脱的肌醇磷酸的洗脱模式也没有影响。因此,当使用卡巴胆碱刺激的PI分解在体外测量毒蕈碱功能时,未观察到先前报道的阿扑氯氮对毒蕈碱激动剂氧化震颤素在体内诱导的震颤和流涎的增强作用。