期刊
PHARMACEUTICALS
卷 14, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/ph14070657
关键词
G protein-coupled receptors; adenosine A(1) receptor ligands; adenosine A(2A) receptor ligands; thiazolo[5,4-d]pyrimidines; ligand-adenosine receptor modeling studies; depression
资金
- University of Florence (Fondi Ateneo Ricerca 2020)
New compounds with high affinity and antidepressant-like activity were synthesized and evaluated in vitro for their potential as A(1) and A(2A) adenosine receptor ligands.
New compounds with a 7-amino-2-arylmethyl-thiazolo[5,4-d]pyrimidine structure were synthesized and evaluated in vitro for their affinity and/or potency at the human (h) A(1), hA(2A), hA(2B), and hA(3) adenosine receptors (ARs). Several compounds (5, 8-10, 13, 18, 19) were characterized by nanomolar and subnanomolar binding affinities for the hA(1) and the hA(2A) AR, respectively. Results of molecular docking studies supported the in vitro results. The 2-(2-fluorobenzyl)-5-(furan-2yl)-thiazolo[5,4-d]pyrimidin-7-amine derivative 18 (hA(1) K-i = 1.9 nM; hA(2A) K-i = 0.06 nM) was evaluated for its antidepressant-like activity in in vivo studies, the forced swimming test (FST), the tail suspension test (TST), and the sucrose preference test (SPT) in mice, showing an effect comparable to that of the reference amitriptyline.
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