scholarly journals Comparison of the Binding and Functional Properties of Two Structurally Different D2 Dopamine Receptor Subtype Selective Compounds

2012 ◽  
Vol 3 (12) ◽  
pp. 1050-1062 ◽  
Author(s):  
Robert R. Luedtke ◽  
Yogesh Mishra ◽  
Qi Wang ◽  
Suzy A. Griffin ◽  
Cathy Bell-Horner ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Functional Properties ◽  
Receptor Subtype ◽  
D2 Dopamine Receptor ◽  
Subtype Selective

scholarly journals Evaluation of Substituted N-Phenylpiperazine Analogs as D3 vs. D2 Dopamine Receptor Subtype Selective Ligands

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3182
Author(s):  
Boeun Lee ◽  
Michelle Taylor ◽  
Suzy A. Griffin ◽  
Tamara McInnis ◽  
Nathalie Sumien ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Involuntary Movement ◽  
Receptor Subtype ◽  
Receptor Subtypes ◽  
Inhibition Assay ◽  
D2 Dopamine Receptor ◽  
Selective Ligand ◽  
6 Hydroxydopamine ◽  
Subtype Selective

N-phenylpiperazine analogs can bind selectively to the D3 versus the D2 dopamine receptor subtype despite the fact that these two D2-like dopamine receptor subtypes exhibit substantial amino acid sequence homology. The binding for a number of these receptor subtype selective compounds was found to be consistent with their ability to bind at the D3 dopamine receptor subtype in a bitopic manner. In this study, a series of the 3-thiophenephenyl and 4-thiazolylphenyl fluoride substituted N-phenylpiperazine analogs were evaluated. Compound 6a was found to bind at the human D3 receptor with nanomolar affinity with substantial D3 vs. D2 binding selectivity (approximately 500-fold). Compound 6a was also tested for activity in two in-vivo assays: (1) a hallucinogenic-dependent head twitch response inhibition assay using DBA/2J mice and (2) an L-dopa-dependent abnormal involuntary movement (AIM) inhibition assay using unilateral 6-hydroxydopamine lesioned (hemiparkinsonian) rats. Compound 6a was found to be active in both assays. This compound could lead to a better understanding of how a bitopic D3 dopamine receptor selective ligand might lead to the development of pharmacotherapeutics for the treatment of levodopa-induced dyskinesia (LID) in patients with Parkinson’s disease.

D2 Dopamine receptor subtype mediates the inhibitory effect of dopamine on TRH-induced prolactin release from the bullfrog pituitary

2010 ◽  
Vol 168 (2) ◽  
pp. 287-292 ◽  
Author(s):  
Masaki Nakano ◽  
Atsuko Minagawa ◽  
Itaru Hasunuma ◽  
Reiko Okada ◽  
Marie-Christine Tonon ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Inhibitory Effect ◽  
Receptor Subtype ◽  
D2 Dopamine Receptor ◽  
Prolactin Release

scholarly journals Cloning of ligand-specific cell lines via gene transfer: identification of a D2 dopamine receptor subtype.

1989 ◽  
Vol 86 (24) ◽  
pp. 10134-10138 ◽  
Author(s):  
R. D. Todd ◽  
T. S. Khurana ◽  
P. Sajovic ◽  
K. R. Stone ◽  
K. L. O'Malley
Keyword(s):  
Gene Transfer ◽  
Dopamine Receptor ◽  
Cell Lines ◽  
Receptor Subtype ◽  
Specific Cell ◽  
D2 Dopamine Receptor
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