Structure‐Activity Relationship Studies of CNS Agents, Part 22: A Search for New Trazodone‐Like Antidepressants: Synthesis and Preliminary Receptor Binding Studies | Zendy

Mokrosz Jerzy L. | Zendy; Duszynska Beata | Zendy; Paluchowska Maria H. | Zendy; CharakchievaMinol S. | Zendy; Mokrosz Maria J. | Zendy

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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.

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