Abstract:
:Sixteen new 1-(2-methoxyphenyl)-4-(1-phenethylpiperidin-4-yl)piperazines and 1-(2-methoxyphenyl)-4-[(1-phenethylpiperidin-4-yl)methyl]piperazines were synthesized to be used as probes for mapping the dopamine D2 receptor (D2 DAR) arylpiperazine binding site. All compounds were evaluated for their affinity toward D2 DAR in an in vitro competitive displacement assay. The most active one was 1-(2-methoxyphenyl)-4-{[1-(3-nitrophenethyl)piperidin-4-yl]methyl}piperazine (25) with an affinity of Ki = 54 nM. Docking analysis was conducted on all herein described compounds, whereas molecular dynamic simulation was performed on ligand 25 to establish its mode of interaction with D2 DAR. Two possible docking orientations are proposed; the one with a salt bridge between the piperidine moiety and Asp114 of D2 DAR is more stable.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Penjišević JZ,Šukalović VV,Andrić DB,Roglić GM,Šoškić V,Kostić-Rajačić SVdoi
10.1002/ardp.201600081subject
Has Abstractpub_date
2016-08-01 00:00:00pages
614-26issue
8eissn
0365-6233issn
1521-4184journal_volume
349pub_type
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