Comparison of the characteristics and density of dopamine-1 receptors in membranes from different arteries using [3H]SCH23390 binding.
By using radioreceptor binding techniques and [3H]SCH23390 as a ligand, a comparative study was performed on the pharmacological properties and the density of dopamine-1 (D1) receptors in different vascular systems. [3H]SCH23390 was specifically bound to membranes from rabbit renal, mesenteric and pulmonary, but not femoral, arteries. The binding was saturable and in a manner consistent with the labeling of D1 receptors. The Kd value and Hill coefficient (nH) were similar in all three arteries with no statistically significant differences (p > 0.05) among them, indicating a homogenous binding site with a single class of high affinity. In competitive binding tests, the selective D1 antagonist and agonist inhibited the binding much more potently than the D2 antagonist, indicating a pharmacological characteristic of D1 receptors. The Bmax values, however, differed considerably among these arteries, with the value being the largest in the renal artery and smallest in the pulmonary artery. These findings are indicative of the existence of D1 receptor sites with identical properties but diverse density in different vascular beds, which underlies the relative functional importance of the receptors in regulating local blood flow in distinct vessels.
Jin
X H
XH
Department of Physiology, Shanxi Medical College, Taiyuan, Peoples Republic of China.
Wang
W Z
WZ
Zhao
R R
RR
D000818:Animals; D001552:Benzazepines / Q000378:metabolism*; D001667:Binding, Competitive; D004294:Domperidone / Q000494:pharmacology; D018491:Dopamine Agonists / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D018818:Fenoldopam / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D008638:Mesenteric Arteries / Q000187:drug effects / Q000378:metabolism; D011651:Pulmonary Artery / Q000187:drug effects / Q000378:metabolism; D011817:Rabbits; D011869:Radioligand Assay; D017447:Receptors, Dopamine D1 / Q000187:drug effects / Q000378:metabolism*; D012039:Regional Blood Flow / Q000187:drug effects; D012077:Renal Artery / Q000187:drug effects / Q000378:metabolism; D014316:Tritium / Q000378:metabolism
D001552:Benzazepines; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D017447:Receptors, Dopamine D1; D014316:Tritium; D004294:Domperidone; D018818:Fenoldopam