Distribution and excretion in the rat and monkey of [82Br] bromocriptine

Radiolabeled bromocriptine was administered to rats and monkeys and its tissue distribution, rate of excretion and metabolism were determined. In both species, [82Br]bromocriptine is predominantly concentrated in the liver, metabolized and then excreted through bile. Extractable free drug is undetectable in blood after 30 min. After 2 hr, the estimated concentration of free drug in rat brain is 2 x 10(-8) M. Terminal phase half-lives of radiolabel excretion were 2.9 days for the rat and 27.3 days for the monkey. The retained organically bound 82Br is present in a form more polar than bromocriptine.