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Specific binding of (/sup 3/H)-1-O-octadecyl Paf-acether to washed human platelets

Journal Article · · Adv. Exp. Med. Biol.; (United States)
; ; ; ;

(/sup 3/H)-Paf-acether binds to washed human platelets in a dose-dependent manner. Scatchard analysis reveals two distinct binding sites; a high affinity site with a KD value of 0.259 +/- 0.33 nM (245 +/- 30 sites per platelet) and a lower affinity site with a KD value of 9.22 +/- 1.17 nM (1616 +/- 165 sites per platelet). Association of /sup 3/H-Paf-acether to the high affinity receptor is rapid, being maximal within two minutes and remaining constant for at least twenty minutes. Dissociation from the low affinity receptor is also rapid (t1/2: less than 10s) whereas dissociation from the high affinity site is significantly slower (t1/2 : approximately 70s). (/sup 3/H)-Paf-acether binding is inhibited by unlabelled (R)-C16-Paf (IC50: 0.08 +/- 0.01 nM) greater than (R)-C18-Paf (0.48 +/- 0.03 nM) greater than (RS)-C18-Paf (1.06 +/- 0.19 nM), but remains unchanged in the presence of lyso-C18-Paf at 3.0-300 nM. (/sup 3/H)-Paf-acether binding and its inhibition by unlabelled (R)-C18-Paf-acether is independent of buffer Ca2+ within the range 0-5.0 mM.

Research Organization:
Searle Research and Development, High Wycombe, England
OSTI ID:
5578769
Journal Information:
Adv. Exp. Med. Biol.; (United States), Journal Name: Adv. Exp. Med. Biol.; (United States); ISSN AEMBA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AFFINITY
ALKALINE EARTH METALS
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL HALF-LIFE
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BLOOD COAGULATION FACTORS
BLOOD PLATELETS
BODY FLUIDS
CALCIUM
COAGULANTS
DOSE-RESPONSE RELATIONSHIPS
DRUGS
ELEMENTS
HEMATOLOGIC AGENTS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MATERIALS
MEMBRANE PROTEINS
METALS
ORGANIC COMPOUNDS
PROTEINS
REACTION KINETICS
RECEPTORS
TRACER TECHNIQUES
TRITIUM COMPOUNDS