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Radioligand binding of antagonists of platelet‐activating factor to intact human platelets
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Personen und Körperschaften: | , , , , , |
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Titel: |
Radioligand binding of antagonists of platelet‐activating factor to intact human platelets |
In: | FEBS Letters, 228, 1988, 2, S. 285-289 |
veröffentlicht: |
Wiley
|
Umfang: | 285-289 |
ISSN: |
0014-5793 1873-3468 |
DOI: | 10.1016/0014-5793(88)80017-6 |
Zusammenfassung: | <jats:p>Two new antagonists of platelet‐activating factor (PAF), the pyrrolothiazole derivative 52770 RP and the triazolodiazepine WEB 2086, have been studied as radioligands in intact human platelets. [<jats:sup>3</jats:sup>H]52770 RP and [<jats:sup>3</jats:sup>H]WEB 2086 bound specifically to high‐affinity sites with dissociation constants (<jats:italic>K</jats:italic> <jats:sub>d</jats:sub>) of 14.8 and 6.1 nM, respectively. The maximal number of sites for [<jats:sup>3</jats:sup>H]52770 RP binding was approx. 15‐fold higher than for [<jats:sup>3</jats:sup>H]PAF and [<jats:sup>3</jats:sup>H]WEB 2086. In addition, C<jats:sub>16</jats:sub>‐PAF, lyso‐PAF, WEB 2086 and 52770 RP had <jats:italic>K</jats:italic> <jats:sub>i</jats:sub> values which were nearly identical for both [<jats:sup>3</jats:sup>H]PAF and [<jats:sup>3</jats:sup>H]WEB 2086, whereas only 52770 RP competed for [<jats:sup>3</jats:sup>H]52770 RP‐binding sites. These results demonstrate that in human platelets the sites of [<jats:sup>3</jats:sup>H]WEB 2086 binding are identical to [<jats:sup>3</jats:sup>H]PAF‐binding sites, whereas those of [<jats:sup>3</jats:sup>H]52770 RP are not. [<jats:sup>3</jats:sup>H]WEB 2086 appears, therefore, to be a suitable antagonist radioligand for labelling PAF receptors.</jats:p> |
Format: | E-Article |
Quelle: | Wiley (CrossRef) |
Sprache: | Englisch |