Abstract
S-Activated sulfhydryldihydromorphine analogs 1 and 2 were synthesized. In the rat brain receptor binding assays, both 1 and 2 exhibited considerably high affinities for μ opioid receptors (IC 50; 1= 31.1 nM, 2= 10.7 nM). However, when each analog was incubated with membranes for the purpose of getting disulfide bridgings, 1 ( EC 50 = 58 nM) was found to affinity-label the μ receptors about 30 times more effectively than 2 ( EC 50 = 1700 nM).
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