Tonini M, Frigo G M, Lecchini S, d'Angelo L, Marcoli M, Crema A
Arzneimittelforschung. 1982;32(5):518-21.
The effects of ten days' oral treatment with 200 mg/kg/d of 4-(3,4,5-trimethoxythiobenzoyl)tetrahydro-1,4-oxazine (trithiozine) on the mechanical responses of rat stomach in vitro have been studied. Gastric muscular excitation due to vagal stimulation was partially reduced in the trithiozine-pretreated animals, while the amount of acetylcholine (Ach) released both at rest conditions and in response to field stimulation was similar in both controls and drug-pretreated rats. Also muscular responses induced by dopamine (DA) and by serotonin (5-HT) were of similar degree in both groups of rats. On the contrary, the nonadrenergic and non-cholinergic inhibitory response evoked by vagal stimulation in the presence of muscarinic and alpha- and beta-adrenergic receptor blockade, respectively, was enhanced in the drug-pretreated animals. Moreover, trithiozine pretreatment caused an increase of spontaneous motor activity and a remarkable degree of potentiation of the contractile response to prostaglandins (PGs), both exogenously applied or endogenously released by ATP. Our results give further evidence that trithiozine has no anticholinergic activity and that some therapeutic properties of the molecule could be accounted for by an involvement of endogenous PGs.
研究了以200毫克/千克/天的剂量口服4-(3,4,5-三甲氧基硫代苯甲酰基)四氢-1,4-恶嗪（曲硫秦）十天对大鼠离体胃机械反应的影响。在经曲硫秦预处理的动物中，迷走神经刺激引起的胃肌兴奋部分降低，而在静息状态和电场刺激下释放的乙酰胆碱（Ach）量在对照组和药物预处理大鼠中相似。两组大鼠中，多巴胺（DA）和5-羟色胺（5-HT）诱导的肌肉反应程度也相似。相反，在分别存在毒蕈碱和α、β肾上腺素能受体阻断的情况下，迷走神经刺激引起的非肾上腺素能和非胆碱能抑制反应在药物预处理动物中增强。此外，曲硫秦预处理导致自发运动活性增加，以及对前列腺素（PGs）收缩反应的显著增强，PGs无论是外源性应用还是由ATP内源性释放。我们的结果进一步证明曲硫秦没有抗胆碱能活性，并且该分子的一些治疗特性可能与内源性PGs的参与有关。
