Increased affinity of histamine H1 binding to membranes of human myometrium at the end of pregnancy.

1. The characterization of H1 binding sites in membrane preparations of human myometrium obtained from pregnant and non-pregnant women was performed by using 3H-mepyramine as the radioactive ligand. 2. Saturation curve analysis revealed that 3H-mepyramine is bound to a single class of binding sites. Changes in the H1 site binding parameters were observed at the end of pregnancy, resulting in an increased affinity relative to non-pregnant tissue (Kd: 131.0 +/- 8.8 (non-pregnant) and 72.5 +/- 7.5 (pregnant) nM, n = 6, P < 0.01). 3. A reduction in receptor concentration at the end of pregnancy was also observed, [Bmax: 565.2 +/- 43.7 (non-pregnant) and 309.6 +/- 25.9 (pregnant) fmol/mg prot, n = 6, P < 0.01]. It is possible that this reduction in Bmax could be attributed to a dilution factor due to the increase in membraneous proteins that occurs during gestation.