Arylpiperazine derivatives – new agents affecting mood disorders

personАвтори: Al. Zlatkov, L. Andonova, M. Georgieva

Abstract. Disorders of the central nervous system currently affect over 1.5 billion people worldwide and account for about a third of the global disease burden.

The prevalence in recent years and the variety of mood disorders stimulate the development of new agents for their treatment. 1-Arylpiperazines are well known 5-HT receptor ligands with 5-HT1A and/or 5-HT2A affinity. The inclusion of a complex heterocyclic fragment through a polymethylene spacer at piperazine position N4 often leads to more potent ligands in both 5-HT1A and 5-HT2A affinities. The results described in literature permit an assumption that the structure of the substituent in positions 1 and 7 of purine-2,6-dione may be regarded as important factor involved in the control of 5HT1A affinity. From the presented investigations may be concluded, that the modification within the aryl fragment had typical influence on 5-HT1A receptor activity. Substitutents at the ortho position of the phenyl ring are well accepted, and the respective analogues always display higher 5-HT1A affinity than the unsubstituted phenylpiperazines.

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