Ukai Y, Taniguchi N, Yamazaki A, Kimura K
Research Laboratories, Nippon Shinyaku Co. Ltd., Kyoto, Japan.
J Pharm Pharmacol. 1989 Apr;41(4):247-52. doi: 10.1111/j.2042-7158.1989.tb06444.x.
The effect of chronic treatment with anethole trithione (ANTT) on the phosphatidylinositol (PI) turnover and cyclic (c)AMP and cGMP accumulation in rat submaxillary glands (SMG) has been compared with the effect of chronic treatment with atropine and a cholinesterase inhibitor, diisopropylfluorophosphate (dyflos, DFP). Experiments were performed 24, 48 and 24 h after the last dose of ANTT, atropine and dyflos, respectively. ANTT and atropine enhanced carbachol-stimulated [32P] incorporation into phosphatidic acid in the SMG slices, while dyflos showed no effect. Pilocarpine-stimulated in-vivo incorporation of [3H]myoinositol into inositol phosphates was significantly enhanced by ANTT, but not by atropine or by dyflos. Phospholipase C-dependent hydrolysis of phosphatidylinositol 4,5-bisphosphate was significantly enhanced by ANTT and atropine, but not by dyflos. Pilocarpine-stimulated in-vivo accumulation of cAMP and cGMP was enhanced by ANTT and atropine, but dyflos reduced cAMP accumulation without affecting cGMP accumulation. The enhancement of PI turnover and cyclic nucleotide accumulation seems to contribute to the development of supersensitivity of the salivary gland caused by chronic treatment with ANTT and atropine, while reduction of cAMP accumulation may be responsible for the subsensitivity caused by dyflos.
已将茴香脑三硫酮(ANTT)长期治疗对大鼠颌下腺(SMG)中磷脂酰肌醇(PI)周转以及环(c)AMP和cGMP积累的影响,与阿托品和胆碱酯酶抑制剂二异丙基氟磷酸酯(敌百虫,DFP)长期治疗的影响进行了比较。分别在最后一剂ANTT、阿托品和敌百虫给药后24、48和24小时进行实验。ANTT和阿托品增强了卡巴胆碱刺激的[32P]掺入SMG切片中的磷脂酸,而敌百虫则无此作用。ANTT显著增强了毛果芸香碱刺激的[3H]肌醇在体内掺入肌醇磷酸,但阿托品和敌百虫未起此作用。ANTT和阿托品显著增强了磷脂酶C依赖性的磷脂酰肌醇4,5 - 二磷酸水解,但敌百虫未起此作用。ANTT和阿托品增强了毛果芸香碱刺激的cAMP和cGMP在体内的积累,但敌百虫降低了cAMP积累,而不影响cGMP积累。PI周转和环核苷酸积累的增强似乎有助于ANTT和阿托品长期治疗引起的唾液腺超敏反应的发展,而cAMP积累的减少可能是敌百虫引起的低敏反应的原因。