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Structure‐Activity Relationship Studies of CNS Agents, Part 22: A Search for New Trazodone‐Like Antidepressants: Synthesis and Preliminary Receptor Binding Studies
Author(s) -
Mokrosz Jerzy L.,
Duszynska Beata,
Paluchowska Maria H.,
CharakchievaMinol S.,
Mokrosz Maria J.
Publication year - 1995
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19953280711
Subject(s) - trazodone , chemistry , stereochemistry , chemical synthesis , receptor , 5 ht receptor , structure–activity relationship , pharmacology , serotonin , in vitro , biochemistry , antidepressant , medicine , hippocampus
New 1‐phenyl‐ and 1‐(3‐chlorophenyl)piperazines containing a 4‐[3‐(heterocyclic)propyl] fragment were synthesized. It was found that of all the investigated compounds 11b ( K i = 13 ± 2 nM) and 8b ( K i = 38 ± 2 nM) were the most active 5‐HT 1A and 5‐HT 2A ligands, respectively. Several derivatives ( 3a, 4a, 8b, 11b, 12b, 13a , and 13b ) were selected as good candidates for new, potential antidepressants on the basis of their 5‐HT 1A /5‐HT 2A receptor binding profiles.