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• W2077580886 abstract "Dopamine receptors include the D 1 - (D 1 and D 5 subtypes) and D 2 -like (D 2 , D 3 , and D 4 subtypes) families. D 1 -like receptors are positively and D 2 -like receptors negatively coupled to the adenylyl cyclase. Dopamine D 2 -like (D 4 subtype) receptors have been identified in human and rat hearts. However the presence of D 2 and D 3 receptor subtypes is unclear. Furthermore, their role in cardiac functions is unknown. By autoradiographic studies of guinea pig hearts, we identified D 3 and D 4 receptors, using the selective radioligands [ 3 H]-7-OH-DPAT and [ 3 H]emonapride (YM-09151-2 plus raclopride). Western blot analysis confirmed D 3 and D 4 receptors in the right and left ventricle of the same species. Selective agonists of D 3 and D 4 receptors (±)-7-OH-DPAT and PD 168 077 (10 –9 to 10 –5 M, respectively) induced a significant negative chronotropic and inotropic effect in the isolated guinea pig heart preparation. Negative inotropic effect induced by PD 168 077 was associated with an inhibition in cyclase activity. No changes in cyclase activity were found with (±)-7-OH-DPAT. The aim of this study is to support the presence of D 3 and D 4 receptors in the heart. Although our results suggest that D 3 and D 4 receptors are functionally active in the heart, we need additional information with an antagonist and an agonist of improved potency and selectivity to understand the respective roles of D 3 and D 4 receptors in the cardiac functions.Key words: Dopamine receptors (D 2 , D 3 , D 4 subtypes), autoradiography, Western blot, cAMP, heart." @default.
• W2077580886 created "2016-06-24" @default.
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• W2077580886 date "2002-06-01" @default.
• W2077580886 modified "2023-09-28" @default.
• W2077580886 title "Functional and autoradiographic characterization of dopamine D₂-like receptors in the guinea pig heart" @default.
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• W2077580886 doi "https://doi.org/10.1139/y02-081" @default.
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