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D 2 Dopaminergic and 5‐HT 1A Serotonergic Activity of 2‐(1‐Naphthyl)ethyl‐ and 2‐(2‐Naphthyl)ethyl Amines
Author(s) -
Šukalović V.,
Roglić G.,
Husinec S.,
KostićRajaćić S.,
Andrić D.,
Šošakić Vukić
Publication year - 2003
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.200300776
Subject(s) - serotonergic , chemistry , dopaminergic , radioligand , receptor , serotonin , 5 ht receptor , ligand binding assay , stereochemistry , ligand (biochemistry) , radioligand assay , dopamine , affinities , chemical synthesis , binding affinities , dopamine receptor , biochemistry , biology , in vitro , endocrinology
Several tertiary 2‐phenylethyl, 2‐(1‐naphthyl)ethyl and 2‐(2‐naphthyl)ethyl amines were synthesized and their binding affinities for dopamine D 1 , D 2 and serotonin 5‐HT 1A receptors evaluated in radioligand binding assays. All compounds were inactive in D 1 dopamine radioligand binding assay. The 2‐(1‐naphthyl)ethyl analogues expressed a low but significant binding affinity for the D 2 and moderate one for the 5‐HT 1A receptor subtypes. Most of the remaining compounds expressed binding affinity at the 5‐HT 1A receptor subtype but were inactive in D 2 receptor binding assay. Based on these results and considering the chemical characteristics of the compounds synthesized and evaluated for dopaminergic and serotonergic activity throughout the present study it can be concluded that hydrophobic type of interaction (stacking or edge‐to‐face) plays a significant role in the formation of receptor‐ligand complexes of 2‐(1‐naphthyl)ethyl amines. This structural motive can be applied to design and synthesize new, more potent dopaminergic/serotonergic ligands by slight chemical modifications.