dopamine receptor type 2 d2r  (OriGene)

Journal: Journal of Medicinal Chemistry

Article Title: Discovery, Optimization, and Characterization of Novel D 2 Dopamine Receptor Selective Antagonists

doi: 10.1021/jm500126s

Figure Lengend Snippet: Known chemical series of selective D 2 versus D 3 DAR antagonists. Superscript “a” indicates that additional information is in Table S15 in .

Article Snippet: This was accomplished by determining the K i values for the compounds using stable (HEK293 based) cell lines expressing the D 3 human dopamine receptors (Codex Biosciences, Gaithersburg, MD).

Techniques:

Journal: Journal of Medicinal Chemistry

Article Title: Discovery, Optimization, and Characterization of Novel D 2 Dopamine Receptor Selective Antagonists

doi: 10.1021/jm500126s

Figure Lengend Snippet: (A) Structure of the hit compound 1 . (B) Graphical representation of the dose–response curves of 1 in D 2 Ca 2+ assay (green, AC 50 = 0.280 ± 0.012 μM), D 2 β-arrestin assay (blue, AC 50 = 2.89 ± 0.25 μM), and D 3 β-arrestin assay (red, AC 50 = 5.76 ± 1.18 μM). (C) Graphical representation of the dose–response curves of 1 in binding assays for D 1 (black), D 2 (blue, K i = 0.30 ± 0.09 μM), D 3 (red, K i = 1.9 ± 0.9 μM), D 4 (green), and D 5 (brown).

Article Snippet: This was accomplished by determining the K i values for the compounds using stable (HEK293 based) cell lines expressing the D 3 human dopamine receptors (Codex Biosciences, Gaithersburg, MD).

Techniques: Beta-Arrestin Assay, Binding Assay