Specific binding of 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor) to the intact canine platelet

Binding of 3H-labeled 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor; PAF) to the intact, washed canine platelet has been defined and characterized as being specific and receptor-mediated. Under the conditions described, specific binding to 2 X 10(7) canine platelets reac...

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Veröffentlicht in:Thrombosis research 1988-06, Vol.50 (6), p.789-802
Hauptverfasser: JANERO, D. R, BURGHARDT, B, BURGHARDT, C
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creator JANERO, D. R
BURGHARDT, B
BURGHARDT, C
description Binding of 3H-labeled 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor; PAF) to the intact, washed canine platelet has been defined and characterized as being specific and receptor-mediated. Under the conditions described, specific binding to 2 X 10(7) canine platelets reached saturation within 10 min at a [3H]PAF concentration of approximately 0.4 nM. Non-specific binding was accountable for, at most, some 30% of the total PAF bound at equilibrium. Above approximately 0.4 nM [3H]PAF, total binding and non-specific binding increased in parallel. Since no involvement of PAF ligand in dog platelet intermediary metabolism during the binding incubation could be demonstrated, non-specific PAF binding may reflect a partitioning of the molecule into a cellular compartment (perhaps the platelet membranes). Equilibrium analysis revealed that the canine platelet has one class of specific binding sites with a Kd of 0.63 +/- 0.02 nM PAF, a Bmax of 222 +/- 10 fmol/10(7) platelets, and, at most, 1.33 +/- 0.06 X 10(3) binding sites/platelet. [3H]PAF specific binding to the canine platelet is ligand-selective and stereo-selective, as demonstrated by the relative abilities of non-labeled PAF and various PAF analogs/metabolites to inhibit [3H]PAF specific binding in a concentration-dependent manner. The extents to which PAF and PAF analogs were able to displace specifically-bound [3H]PAF from the canine platelet correlated well with their physiological (i. e., pro-aggregatory) effects. These data offer the first quantitative description of canine platelet high-affinity PAF binding sites/receptors and link receptor-mediated PAF binding to canine platelet physiology.
doi_str_mv 10.1016/0049-3848(88)90339-8
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R</creatorcontrib><creatorcontrib>BURGHARDT, B</creatorcontrib><creatorcontrib>BURGHARDT, C</creatorcontrib><title>Specific binding of 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor) to the intact canine platelet</title><title>Thrombosis research</title><addtitle>Thromb Res</addtitle><description>Binding of 3H-labeled 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor; PAF) to the intact, washed canine platelet has been defined and characterized as being specific and receptor-mediated. Under the conditions described, specific binding to 2 X 10(7) canine platelets reached saturation within 10 min at a [3H]PAF concentration of approximately 0.4 nM. Non-specific binding was accountable for, at most, some 30% of the total PAF bound at equilibrium. Above approximately 0.4 nM [3H]PAF, total binding and non-specific binding increased in parallel. Since no involvement of PAF ligand in dog platelet intermediary metabolism during the binding incubation could be demonstrated, non-specific PAF binding may reflect a partitioning of the molecule into a cellular compartment (perhaps the platelet membranes). Equilibrium analysis revealed that the canine platelet has one class of specific binding sites with a Kd of 0.63 +/- 0.02 nM PAF, a Bmax of 222 +/- 10 fmol/10(7) platelets, and, at most, 1.33 +/- 0.06 X 10(3) binding sites/platelet. [3H]PAF specific binding to the canine platelet is ligand-selective and stereo-selective, as demonstrated by the relative abilities of non-labeled PAF and various PAF analogs/metabolites to inhibit [3H]PAF specific binding in a concentration-dependent manner. The extents to which PAF and PAF analogs were able to displace specifically-bound [3H]PAF from the canine platelet correlated well with their physiological (i. e., pro-aggregatory) effects. These data offer the first quantitative description of canine platelet high-affinity PAF binding sites/receptors and link receptor-mediated PAF binding to canine platelet physiology.</description><subject>Animals</subject><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Blood coagulation. Blood cells</subject><subject>Blood Platelets - metabolism</subject><subject>Dogs</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Kinetics</subject><subject>Ligands</subject><subject>Molecular and cellular biology</subject><subject>Platelet</subject><subject>Platelet Activating Factor - antagonists &amp; inhibitors</subject><subject>Platelet Activating Factor - metabolism</subject><subject>Platelet Aggregation - drug effects</subject><issn>0049-3848</issn><issn>1879-2472</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kctOwzAQRS0EKqXwByBlgVC7MPiRxM4SVbykSl0A68iZ2K3BTULsInXBv-OK0MVoRnPPvYsZhC4puaWE5neEpAXmMpVTKWcF4bzA8giNqRQFZqlgx2h8QE7RmfcfhFBBi2yERjylXHAyRj-vnQZrLCSVbWrbrJLWJBQvsXKfO4cZVqBDHHyDV24Hum8xx9269bFg3Trb6GTaORW00yHCwX6rsI8xcW77WRLaJKx1YpsQFwmoZu_4N5yjE6Oc1xdDn6D3x4e3-TNeLJ9e5vcL3DGeBUwzXVWUQZoB5BUnhWZEF8xAVuUs14YrlQNXslZAAKQUNK1TURnKM2AiOibo5i-369uvrfah3FgP2jnV6HbrSyFTIoqMRfBqALfVRtdl19uN6nflcK-oXw-68qCc6VUD1h8wIeMXcsF_AZfRe7U</recordid><startdate>19880615</startdate><enddate>19880615</enddate><creator>JANERO, D. 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Blood cells</topic><topic>Blood Platelets - metabolism</topic><topic>Dogs</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Kinetics</topic><topic>Ligands</topic><topic>Molecular and cellular biology</topic><topic>Platelet</topic><topic>Platelet Activating Factor - antagonists &amp; inhibitors</topic><topic>Platelet Activating Factor - metabolism</topic><topic>Platelet Aggregation - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>JANERO, D. R</creatorcontrib><creatorcontrib>BURGHARDT, B</creatorcontrib><creatorcontrib>BURGHARDT, C</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Thrombosis research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>JANERO, D. R</au><au>BURGHARDT, B</au><au>BURGHARDT, C</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Specific binding of 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor) to the intact canine platelet</atitle><jtitle>Thrombosis research</jtitle><addtitle>Thromb Res</addtitle><date>1988-06-15</date><risdate>1988</risdate><volume>50</volume><issue>6</issue><spage>789</spage><epage>802</epage><pages>789-802</pages><issn>0049-3848</issn><eissn>1879-2472</eissn><coden>THBRAA</coden><abstract>Binding of 3H-labeled 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor; PAF) to the intact, washed canine platelet has been defined and characterized as being specific and receptor-mediated. Under the conditions described, specific binding to 2 X 10(7) canine platelets reached saturation within 10 min at a [3H]PAF concentration of approximately 0.4 nM. Non-specific binding was accountable for, at most, some 30% of the total PAF bound at equilibrium. Above approximately 0.4 nM [3H]PAF, total binding and non-specific binding increased in parallel. Since no involvement of PAF ligand in dog platelet intermediary metabolism during the binding incubation could be demonstrated, non-specific PAF binding may reflect a partitioning of the molecule into a cellular compartment (perhaps the platelet membranes). Equilibrium analysis revealed that the canine platelet has one class of specific binding sites with a Kd of 0.63 +/- 0.02 nM PAF, a Bmax of 222 +/- 10 fmol/10(7) platelets, and, at most, 1.33 +/- 0.06 X 10(3) binding sites/platelet. [3H]PAF specific binding to the canine platelet is ligand-selective and stereo-selective, as demonstrated by the relative abilities of non-labeled PAF and various PAF analogs/metabolites to inhibit [3H]PAF specific binding in a concentration-dependent manner. The extents to which PAF and PAF analogs were able to displace specifically-bound [3H]PAF from the canine platelet correlated well with their physiological (i. e., pro-aggregatory) effects. These data offer the first quantitative description of canine platelet high-affinity PAF binding sites/receptors and link receptor-mediated PAF binding to canine platelet physiology.</abstract><cop>New York, NY</cop><pub>Elsevier Science</pub><pmid>3413730</pmid><doi>10.1016/0049-3848(88)90339-8</doi><tpages>14</tpages></addata></record>
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subjects Animals
Binding, Competitive
Biological and medical sciences
Blood coagulation. Blood cells
Blood Platelets - metabolism
Dogs
Fundamental and applied biological sciences. Psychology
Kinetics
Ligands
Molecular and cellular biology
Platelet
Platelet Activating Factor - antagonists & inhibitors
Platelet Activating Factor - metabolism
Platelet Aggregation - drug effects
title Specific binding of 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine (platelet-activating factor) to the intact canine platelet
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