Broggini M, Rossi C, Colombo T, D'Incalci M
Cancer Treat Rep. 1982 Jan;66(1):127-33.
The distribution of hexamethylmelamine (HMM), pentamethylmelamine (PMM), and their metabolites N2,N2,N4,N6-tetramethylmelamine (TMM) and N2,N4,N6-trimethylmelamine (TriMM) was investigated in different tissues of M5076/73A ovarian cancer-bearing mice given 100 mg/kg ip of either drug. The area-under-the-curve (AUC) values of HMM and PMM, expressed in microgram/g x min after these drug treatments, were 2432 and 1296 in tumor, 6290 and 8141 in liver, 9779 and 21,294 in spleen, 6840 and 10,800 in kidney, 4003 and 4295 in heart, 1569 and 1327 in brain, 163,689 and 50,809 in adipose tissue, 88,725 and 45,070 in lymph nodes, 15,033 and 18,992 in small intestine, and 393 and 351 in plasma, respectively. The elimination rate of HMM for the different organs was similar, with a half-life of 37-48 mins; PMM disappeared with more variability, the half-life being 19-46 mins. While TMM concentrations were not very different from those of HMM or PMM, TriMM was much higher in all organs evaluated, particularly the brain, where AUC values were 21-24 times those of the administered drug.
在给荷M5076/73A卵巢癌小鼠腹腔注射100 mg/kg的六甲基三聚氰胺（HMM）或五甲基三聚氰胺（PMM）后，研究了这两种药物及其代谢产物N2,N2,N4,N6-四甲基三聚氰胺（TMM）和N2,N4,N6-三甲基三聚氰胺（TriMM）在不同组织中的分布情况。经这些药物处理后，以微克/克×分钟表示的HMM和PMM的曲线下面积（AUC）值，在肿瘤中分别为2432和1296，在肝脏中为6290和8141，在脾脏中为9779和21294，在肾脏中为6840和10800，在心脏中为4003和4295，在大脑中为1569和1327，在脂肪组织中为163689和50809，在淋巴结中为88725和45070，在小肠中为15033和18992，在血浆中为393和351。HMM在不同器官中的消除速率相似，半衰期为37 - 48分钟；PMM的消除存在较大差异，半衰期为19 - 46分钟。虽然TMM的浓度与HMM或PMM的浓度差异不大，但在所有评估器官中，TriMM的浓度要高得多，尤其是在大脑中，其AUC值是给药药物的21 - 24倍。
