Abstract

Combined in vivo radioreceptor binding and autoradiographic techniques were used to characterized the pharmacological profile and to study the anatomical localization of dopamine (DA) DA-1 receptor sites in sections of rabbit pulmonary artery. [3H]R-(+)-8-chloro-2,3,4,5-tetrahydro-5-phenyl-1H-3-benzazepin-7- alhemimaleate (SCH 23390), which was used as a ligand, was bound by sections of rabbit pulmonary artery in a manner consistent with the binding of DA DA-1 sites. The Kd value was 4.75 nM, whereas the Bmax value was 78.3 +/- 5.7 fmol/mg tissue. Light microscope autoradiography demonstrated specific [3H]SCH 23390 binding sites primarily in the endothelium of the rabbit pulmonary artery. Moreover, sparse receptor sites were visualized in the medial layer. Mechanical removal of endothelium caused the disappearance of [3H]SCH 23390 binding sites showing the endothelial localization, but was without effect on the receptor sites of the medial layer. The present findings suggest that differently from systemic arteries, where DA-1 receptor sites are localized in the medial layer, probably within smooth muscle, the majority of DA-1 sites in the rabbit pulmonary artery are endothelial. The possible significance of these sites visualized in the present study for the first time is discussed.