Pocchiari F, Pataccini R, Castelnovo P, Longo A, Paro M, Casagrande C
Arzneimittelforschung. 1986 Feb;36(2A):341-4.
Ibopamine (SB-7505), the 3,4-diisobutyryl ester of N-methyldopamine (epinine), exerts, on oral administration, cardiovascular effects similar to those of intravenously infused dopamine. Plasma levels and urinary excretion of metabolites were investigated in dogs after oral administration of 4 mg/kg of ibopamine hydrochloride. Epinine, which was readily formed from ibopamine by esterases hydrolysis, was present in plasma in free and sulphate-conjugated form. The urinary metabolites after 6 h from the administration amounted to 62% of the dose, as a sum of 37% of epinine 3-O-sulphate, and 15 and 10% of 4-hydroxy-3-methoxyphenylacetic acid and 3,4-dihydroxyphenylacetic acid, respectively, both in free and conjugated form. When the main metabolite, epinine 3-O-sulphate, was administered intravenously it appeared to be excreted in urine without being deconjugated to any detectable extent, while it appeared to be partially deconjugated on oral administration.
异波帕明（SB - 7505），即N - 甲基多巴胺（去甲肾上腺素）的3,4 - 二异丁酰酯，口服时产生的心血管效应与静脉输注多巴胺相似。给犬口服4mg/kg盐酸异波帕明后，研究了其代谢产物的血浆水平和尿排泄情况。由酯酶水解异波帕明容易形成的去甲肾上腺素，以游离和硫酸结合形式存在于血浆中。给药6小时后的尿代谢产物占剂量的62%，其中3 - O - 硫酸去甲肾上腺素占37%，4 - 羟基 - 3 - 甲氧基苯乙酸和3,4 - 二羟基苯乙酸分别占15%和10%，均以游离和结合形式存在。当主要代谢产物3 - O - 硫酸去甲肾上腺素静脉给药时，它似乎以未结合的形式排泄到尿液中，未检测到任何程度的去结合，而口服给药时似乎部分去结合。
