Radioligand binding of antagonists of platelet-activating factor to intact human platelets.
FEBS Lett
; 228(2): 285-9, 1988 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-3342883
ABSTRACT
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. [3H]52770 RP and [3H]WEB 2086 bound specifically to high-affinity sites with dissociation constants (Kd) of 14.8 and 6.1 nM, respectively. The maximal number of sites for [3H]52770 RP binding was approx. 15-fold higher than for [3H]PAF and [3H]WEB 2086. In addition, C16-PAF, lyso-PAF, WEB 2086 and 52770 RP had Ki values which were nearly identical for both [3H]PAF and [3H]WEB 2086, whereas only 52770 RP competed for [3H]52770 RP-binding sites. These results demonstrate that in human platelets the sites of [3H]WEB 2086 binding are identical to [3H]PAF-binding sites, whereas those of [3H]52770 RP are not. [3H]WEB 2086 appears, therefore, to be a suitable antagonist radioligand for labelling PAF receptors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Azepinas
/
Tiazóis
/
Triazinas
/
Triazóis
/
Plaquetas
Limite:
Humans
Idioma:
En
Revista:
FEBS Lett
Ano de publicação:
1988
Tipo de documento:
Article
País de afiliação:
Reino Unido