Molecular properties of central and peripheral histamine H1 and H2 receptors

Abstract.

We identified and characterised histamine H1 and H2 receptor subtypes on rat cortical astrocytes in primary culture with radioligand binding studies and compared their molecular properties with peripheral (bovine vascular smooth muscle and endothelial cells) histamine H1 and H2 receptors. Our results showed the existence of a homogenous population of high affinity binding sites for ³H-mepyramine (B_max = 281 fmol/mg protein, K_D= 3.5 +/− 0.7 nM) and ³H-tiotidine (B_max = 59 fmol/mg protein, K_D = 1.9 +/− 0.7 nM) on astrocytes, which was further confirmed by competition binding studies using various H1 and H2 specific agonists/antagonists. We showed differences in the density of receptors and differences in the affinities of competing drugs for the same histamine receptor subtype (H1 and H2) between the tissues used, which indicate different molecular properties of the central and peripheral histamine receptors.