Histamine H1-receptor-like binding sites in the locust nervous tissue.
The histamine H1-receptor-like binding sites in the nervous tissue of the locust Locusta migratoria were investigated with a conventional radio-receptor assay using [3H]mianserin as the radio ligand. Binding of [3H]mianserin to the binding site is sensitive to proteases and heat treatment. It shows the characteristics of ligand-receptor interactions. The single binding site has high affinity for mianserin (KD = 7.05 nM) and is present in high concentrations (Bmax = 1.53 pmol/mg) in the whole nervous tissue. All tested antihistamines have a high affinity for the binding site, which suggests that it represents an insect histamine receptor. Nevertheless, it shows its peculiarities distinguishing it from vertebrate histamine H1-receptors.
Roeder
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Universität Hamburg, Zoologisches Institut, F.R.G.
D000818:Animals; D001665:Binding Sites; D006110:Grasshoppers / Q000378:metabolism*; D006633:Histamine Antagonists / Q000378:metabolism; D008803:Mianserin / Q000037:antagonists & inhibitors / Q000378:metabolism; D009417:Nerve Tissue / Q000378:metabolism*; D011869:Radioligand Assay; D011969:Receptors, Histamine H1 / Q000378:metabolism*
D006633:Histamine Antagonists; D011969:Receptors, Histamine H1; D008803:Mianserin