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Adrenomedullin receptor binding sites in rat brain and peripheral tissues


, : Adrenomedullin receptor binding sites in rat brain and peripheral tissues. European Journal of Pharmacology 474(2-3): 165-174, 8 August

The existence of specific adrenomedullin receptor binding sites was investigated using the agonist peptide a (125I) human adrenomedullin-(13-52) in rat brain, lung and vas deferens homogenates. Saturation-binding experiments suggest that (125I)human adrenomedullin-(13-52) binds to an apparent single population of sites with similar affinities (KD of 0.3 to 0.6 nM) but with different maximal binding capacity in the rat brain, lung and vas deferens homogenates (Bmax of 73, 1760 and 144 fmol/mg protein, respectively). Competition-binding experiments using various analogues and fragments of calcitonin gene-related peptide (CGRP) and adrenomedullin were also performed using this radioligand. Competition-binding profiles suggest the possible existence of heterogeneous populations of adrenomedullin receptor binding sites. For example, in rat brain, human adrenomedullin-(1-52) and human adrenomedullin-(13-52) competed against specific (125I)human adrenomedullin-(13-52) sites with competition curves best fitted to a two-site model. Additionally, human calcitonin gene-related peptide alpha (hCGRPalpha), (Cys(Et)2,7)hCGRPalpha and ((R-(R,(R*,S*))-N-(2-((5-amino-1-((4-(4-pyridinyl)-1-piperazinyl)carbonyl)pentyl)amino)-1-((3,5-dibromo-4-hydroxyphenyl)methyl)-2-oxoethyl)-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-,1-Piperidinecarboxamide) (BIBN4096BS) competed against specific (125I)human adrenomedullin-(13-52) binding with profiles that were also best fitted to a two-site model. Furthermore, binding assays performed in the presence of GTPgammaS (100 muM) revealed that this compound inhibited 20% of specific (125I)human adrenomedullin-(13-52) sites in rat brain homogenates and competition curves of human adrenomedullin-(1-52) and (Cys(Et)2,7)hCGRPalpha against specific (125I)human adrenomedullin-(13-52) sites remained best fitted to a two-site model. Moreover, the existence of specific (125I)human adrenomedullin-(13-52) binding sites that are resistant to human adrenomedullin-(22-52) and human CGRP-(8-37) is suggested in the rat brain and vas deferens. Taken together, these data provide evidence for the possible existence of heterogeneous populations of adrenomedullin binding sites in rat brain and peripheral tissues.

US$19.90

PMID: 12921858

DOI: 10.1016/s0014-2999(03)02042-9


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Christakis, G., 1979: How to make a nutritional diagnosis without really trying. A. Adult nutritional diagnosis. A. Many nutritional deficiency states are common and are easily missed by the diagnosing physician, particularly in their early stage. It is necessary to probe for signs, including biochemical signs, and symptoms in adult persons.

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Filippov, D.; Hilkova, O., 1965: Improving varietal composition in the fields. The following recommended potato varieties have all been recently bred at the White Russian Institute of Horticulture, Vegetables and Potato: Skorospelka 1 and 2, Losice, Razvaristyj and Temp; they have high tuber yields and are resistant to wart....

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Ring, E.F.; Engel, J.M.; Page-Thomas, D.P., 1984: Thermologic methods in clinical pharmacology-skin temperature measurement in drug trials. With the increasing availability of thermographic equipment the definition of "thermography" and "thermologic methods" is important, since differing techniques and standards may be applied. Recommendations are given for optimum...

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Dreyfus, R., 1972: Problems and solutions. Reaction or flu?. Dental Survey 48(1): 37-37

Khomentovsky, P.A., 1981: Insects-xylophages in an isolated habitat of Larix kurilensis on the Kamchatka Peninsula. The endemic fauna of insects-xylophages of the Kurile larch in the Storozh river valley isolated by mountain ridges from its main range on the Kamchatka Peninsula is extremely poor (2--3 species). With respect to the Tolbachik volcano eruption in...

Hood, E.G., 1931: The cause and prevention of mould in pasteurized butter. An address based on known information of standard character, designed to inform local buttermakers as to sources of yeasts and molds in butter, with very little new information.