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A D1/D2 chimeric dopamine receptor mediates a D1 response to a D2‐selective agonist
Author(s) -
MacKenzie Robert G.,
Steffey Michael E.,
Manelli Arlene M.,
Pollock Nancy J.,
Frail Donald E.
Publication year - 1993
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(93)81448-9
Subject(s) - quinpirole , dopamine receptor d2 , agonist , receptor , endogenous agonist , chemistry , dopamine receptor d1 , dopamine receptor , d1 like receptor , dopamine receptor d3 , d2 like receptor , pharmacology , microbiology and biotechnology , biology , biochemistry
D1 and D2 dopamine receptors are G‐protein coupled receptors and have seven transmembrane spanning regions (TM) typical of this receptor superfamily. Although dopamine binds equally to D1 and D2 receptors, many compounds are highly selective. To probe the receptors for regions that determine subtype specificity, plasmid constructs coding for the D1 or a D1/D2 chimeric receptor were made and transfected into cells to study the binding and agonist properties of non‐selective or subtype‐selective compounds. The results suggest that the D2‐selective agonist, quinpirole, gains much of its selectivity by binding to within TM VI and VII of the D2 receptor.