Abstract
A series of benzolactam derivatives has been evaluated for their affinity for alpha 1 and alpha 2-adrenoreceptors. The influence of terminal amine and amide fragments on the affinity and selectivity has been investigated. It has been found that derivatives containing 1,2,3,4-tetrahydroisoquinoline (THIQ) as the basic component can form potent alpha 1 and/or alpha 2 ligands, and that their alpha 1/alpha 2 selectivity depends on the benzolactam fragment.
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