Abstract
AbstractA series of structurally rigid compounds (2‐amino‐2, 3‐dihydro‐3H‐phenalenes) has been synthesized for dopamine (DA) agonist activities. One member (U‐66444B) in the series has been reported as a potent and selective agonist for presynaptic DA receptors. Among close analogues of U‐66444B, we have identified two compounds with DA antagonist activities by behavioral and biochemical endpoints. The distinguishing chemical features of these two antagonists are methyl substitutions on the amino nitrogen and a phenolic hydroxy group having a most proximal position to the amino group. The structure‐activity relationship in this series of compounds may contribute to future design of DA agonists and antagonists.
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