Iwamura S, Kambegawa A
J Pharmacobiodyn. 1981 Apr;4(4):275-81. doi: 10.1248/bpb1978.4.275.
New hapten-carrier conjugates were prepared from 9,10-dihydro-N-[1-(hydroxymethyl)propyl]-6-methylergoline-8-carboxamide 1-hemisuccinate (dihydromethylergometrine hemisuccinate) by coupling with bovine serum albumin employing the mixed anhydride technique. The specificity of anti-dihydromethylergometrine antiserum elicited in the rabbits by immunization with this antigen was tested by cross-reaction studies with methylergometrine, dihydroergotoxine, dihydroergocristine and dihydroergotamine employing [9,10-3H]-dihydromethylergometrine and [9,10-3H]-dihydroergocryptine in the radioimmunoassay procedure. These cross reactivities were observed 100% for methylergometrine, 48.3% for dihydroergotamine, 16.6% for dihydroergotoxine and 6.6% for dihydroergocristine using labeled dihydromethylergometrine. When labeled dihydroergocriptine was the results were 18.3%, 112.1%, 100% and 63.8%, respectively. Methylergometrine concentrations in the postpartal plasma and milk at 2 hr after oral administration of methylergometrine maleate (0.75 mg) to woman were 5.1 ng/ml and 1.3 ng/ml, respectively. Dihydroergotoxine concentrations in the rabbit sera after oral administration of dihydroergotoxine methanesulfonate (4 mg) were studied. The assay was satisfactory to permit the measurement of ergot alkaloid levels in the biological fluids.
采用混合酸酐技术，将9,10 - 二氢 - N - [1 - (羟甲基)丙基] - 6 - 甲基麦角灵 - 8 - 甲酰胺1 - 半琥珀酸酯（二氢甲基麦角新碱半琥珀酸酯）与牛血清白蛋白偶联，制备了新的半抗原 - 载体缀合物。用该抗原免疫家兔产生的抗二氢甲基麦角新碱抗血清的特异性，通过在放射免疫分析程序中使用[9,10 - 3H] - 二氢甲基麦角新碱和[9,10 - 3H] - 二氢麦角隐亭，与甲基麦角新碱、二氢麦角毒碱、二氢麦角克碱和二氢麦角胺进行交叉反应研究来测试。使用标记的二氢甲基麦角新碱时，甲基麦角新碱的交叉反应率为100%，二氢麦角胺为48.3%，二氢麦角毒碱为16.6%，二氢麦角克碱为6.6%。当标记的是二氢麦角隐亭时，结果分别为18.3%、112.1%、100%和63.8%。给女性口服马来酸甲基麦角新碱（0.75mg）后2小时，产后血浆和乳汁中甲基麦角新碱的浓度分别为5.1ng/ml和1.3ng/ml。研究了给家兔口服甲磺酸二氢麦角毒碱（4mg）后血清中二氢麦角毒碱的浓度。该分析方法足以用于测量生物体液中的麦角生物碱水平。
