Histamine H1-receptor in endothelial and smooth muscle cells of guinea-pig aorta.

The location of histamine H1-receptors in the thoracic aorta of guinea-pigs was studied with a [3H]mepyramine binding assay. [3H]Mepyramine binding studies of whole and rubbed aortas, and of cultured endothelial and smooth muscle cells showed that the Kd values were all in the range 0.53-0.76 nM, but that the Bmax values were 19.1, 10.1, 63.3 and 11.6 fmol/mg protein, respectively. Thus, the whole aorta contained more H1-receptors than the rubbed one (free of endothelium), and cultured endothelial cells contained more H1-receptors than smooth muscle cells. These results indicate that more histamine H1-receptors were concentrated in the endothelial cells than in the smooth muscle cells in guinea-pig aorta.