毒理性
识别和使用：麦角克辛是一种固体。麦角克辛及其盐类属于第一类化学品。秘密实验室正在使用这种化学物质作为第一类化学品麦角胺和麦角新碱的替代品，非法制造被列为一类受控物质的麦角酸二乙基酰胺（LSD）。人体研究：在所有测试的麦角生物碱中，麦角克辛是最具细胞毒性的化合物，能从1微摩尔浓度开始诱导人肾细胞凋亡。动物研究：从挪威西南部采集的麦田草中的麦角被检查出生物碱并口服给四只大约10个月大的羊。以每天每千克体重0.12-0.75克的速度给硬壳药，持续4-27天。硬壳药中总生物碱的浓度估计约为0.4%。通过薄层色谱法鉴定出麦角辛、麦角克辛、麦角胺及其三种相应的异构体。在总生物碱中，麦角辛和麦角克辛各占35%，麦角胺占15%，异构体各占5%。在寒冷潮湿的天气中，三只在外喂养的羊都生病了，表现出食欲不振和脉搏率增加。在室内喂养的那只羊没有出现症状，也没有尸检病变。对三只表现出症状的羊进行尸检时，在消化道，尤其是瘤胃和盲肠中，发现了粘膜充血、出血、糜烂和坏死。其中两只羊的一些肢体和尾巴远端发现了轻微水肿，但没有观察到坏疽的迹象。五种麦角生物碱，即d-麦角酸衍生物，在培养的中国仓鼠卵巢细胞中测试了诱导姐妹染色单体交换（SCE）频率的能力。测试物质的浓度在10(-5)到10(-8) M之间。麦角胺、麦角新碱和甲基麦角新碱在所有使用的浓度下都显著增加了SCE的数量，而麦角克辛只有在最高浓度下才会出现这种情况。由于麦角克辛引起的血管收缩是通过α2-肾上腺素受体介导的，在大鼠中，麦角克辛作为α2-肾上腺素受体的激动剂，以及α1-肾上腺素受体的拮抗剂。
IDENTIFICATION AND USE: Ergocristine is a solid. Ergocristine and its salts are List I Chemicals. Clandestine laboratories are using this chemical as a substitute for the List I chemicals ergotamine and ergonovine to illicitly manufacture the schedule I controlled substance lysergic acid diethylamide (LSD). HUMAN STUDIES: Of all tested ergot alkaloids, ergocristine was the most cytotoxic compound inducing apoptosis in human kidney cells starting at a concentration of 1uM. ANIMAL STUDIES: A sample of ergot from meadow grass collected in the south-western part of Norway was examined for alkaloids and dosed orally to four lambs about 10 months old. Sclerotia were dosed at a rate of 0.12-0.75 g per kg body weight per day for 4-27 days. The concentration of total alkaloids in the sclerotia was estimated to be about 0.4%. Ergosine, ergocristine, ergotamine and the three corresponding isomers were identified by thin-layer chromatography. Of the total alkaloids, ergosine and ergocristine constituted 35% each, ergotamine 15% and the isomers 5% each. Three lambs dosed outdoors in cold and wet weather all became ill, with anorexia and increased pulse rate. No symptoms nor post mortem lesions were seen in the single lamb kept indoors. On post mortem examination of the three lambs showing symptoms, hyperemic mucosae, hemorrhages, erosions and necroses in the digestive tract, most pronounced in abomasum and cecum, were demonstrated. In two lambs, slight edema was found distally in some of the limbs and tail, but no sign of gangrene was observed. Five ergot alkaloids, d-lysergic acid derivatives, were tested for the induction of sister chromatid exchange (SCE) frequencies in cultured Chinese hamster ovary cells. The concentrations of the test substances ranged between 10(-5) and 10(-8) M. Ergotamine, ergonovine, and methylergonovine induced a significantly high number of SCEs at all the concentrations used, while with ergocristine this occurred only at the highest concentration. Vasoconstriction due to ergocristine is mediated by alpha 2-adrenoceptors and in the rat, ergocristine acts as an alpha 2-adrenoceptors agonist, and an alpha 1-adrenoceptors antagonist.
来源:Hazardous Substances Data Bank (HSDB)
