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【结 构 式】 
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【药物名称】Iobenguane[131I], MIBG, PheoMIBG-I(131) Injection 【化学名称】m-131-Iodobenzylguanidine 【CA登记号】77679-27-7, 139755-80-9 (123I-labeled sulfate(2:1)), 87862-25-7 (non-labeled sulfate (2:1)), 149210-33-3 (sulfate (2:1)) 【 分 子 式 】C8H10IN3 【 分 子 量 】279.189 |
【开发单位】University of Michigan (Originator), CIS Bio International (Licensee), Daiichi Radioisotope (Licensee), Neoprobe (Licensee) 【药理作用】Diagnostic Agents, ONCOLYTIC DRUGS |
合成路线1
MIBG is synthesized as follows: A mixture of m-iodobenzylamine (I) hydrochloride and cyanamide (II) is stirred and heated at 100 C for 4h. The resulting m-iodobenzylguanidine is converted to the bicarbonate salt by treatment with aqueous potassium bicarbonate. Addition of dilute sulfuric acid gives the guanidine sulfate. To prepare the labeled compound, the unlabeled m-iodobenzylguanidinium sulfate is dissolved in water and treated with carrier-free Na[131]I. Refluxing for 72h and passage through Cellex D anion exchange cellulose gives [131]iodobenzylguanidine sulfate. Another more efficient method of carrying out the exchange-labeling step has been reported.
| 【1】 Eastland, G. Jr.; Iobenguane (131I). Drugs Fut 1989, 14, 5, 427. |
| 【2】 Wieland, D.M.; Wu, J.-L.; Brown, L.E.; Mengner, T.J.; Swanson, D.P.; Beierwaltes, W.H.; Radiolabeled adrenergic neuron-blocking agents: Adrenomedullary imaging with [131]iodobenzylguanidine. J Nucl Med 1980, 21, 349-53. |
| 【3】 Shapiro, B.; Copp, J.E.; Sisson, J.C.; Eyres, P.L.; Wallis, J.; Beierwaltes, W.H.; Iodine-131-m-iodobenzylguanidine for the locating of suspected pheochromocytoma: Experience in 400 cases. J Nucl Med 1985, 26, 576-85. |