[摘要]：The prepn. of a no. of (bis)guanidine and (bis)2-aminoimidazoline derivs. as potential a2-adrenoceptor antagonists for the treatment of depression was presented. Human brain tissue was used to measure their affinity toward the a2-adrenoceptors in vitro. Several compds., including the tetrahydronaphthalenylguanidine I and the bis(imidazolinyl)ethylenedianiline II, displayed good affinity and were evaluated in in vitro functional [35S]GTPgS binding assays in human prefrontal cortex to det. their agonistic or antagonistic activity. I and II showed the expected behavior for an antagonist and were subject to in vivo microdialysis expts. in rats. Significantly, these expts. confirmed the antagonistic properties of I and II, and therefore both compds. can be considered as potential antidepressants.
