Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1990-4-26
pubmed:abstractText
The effects of polymyxin B, a cyclic polycationic peptide antibiotic, on the binding of thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor agonists and antagonists to the putative human platelet TXA2/PGH2 receptor have been determined. Crude membranes were prepared from washed human platelets and the binding of [125I]-PTA-OH, a TXA2/PGH2 receptor antagonist, was used as a ligand to characterize the effects of polymyxin B on agonist and antagonist binding. Polymyxin B produced a concentration-dependent decrease in the IC50 values for the TXA2/PGH2 agonist, U46619, in radioligand competition binding assays. Polymyxin B also decreased the IC50 values of the TXA2/PGH2 agonist ONO 11113 from 75 +/- 11 nM to 38 +/- 2.5 nM and the TXA2/PGH2 receptor antagonist SQ29548 from 60 +/- 14 nM to 20 +/- 2.3 nM. The Kd for [125I]-PTA-OH was also reduced by polymyxin B from 107 +/- 10 nM to 76 +/- 6 nM but it had no effect on the maximum number of binding sites (Bmax). Polymyxin B had no significant effect on the binding affinity of U46619 in intact washed human platelets. These results raise the possibility that polymyxin B can alter the conformational state of the TXA2/PGH2 receptor when it is in a crude membrane fraction but not in intact platelets.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/1-(5-Isoquinolinesulfonyl)-2-Methylp..., http://linkedlifedata.com/resource/pubmed/chemical/15-Hydroxy-11 alpha,9..., http://linkedlifedata.com/resource/pubmed/chemical/Hydrazines, http://linkedlifedata.com/resource/pubmed/chemical/I-PTA-OH, http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines, http://linkedlifedata.com/resource/pubmed/chemical/Piperazines, http://linkedlifedata.com/resource/pubmed/chemical/Polymyxin B, http://linkedlifedata.com/resource/pubmed/chemical/Polymyxins, http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin Endoperoxides, http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandin Endoperoxides..., http://linkedlifedata.com/resource/pubmed/chemical/Prostaglandins H, http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Prostaglandin, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Thromboxane A2..., http://linkedlifedata.com/resource/pubmed/chemical/SQ 29548, http://linkedlifedata.com/resource/pubmed/chemical/STA 2, http://linkedlifedata.com/resource/pubmed/chemical/Thromboxane A2
pubmed:status
MEDLINE
pubmed:issn
0934-9820
pubmed:author
pubmed:issnType
Print
pubmed:volume
1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
41-4
pubmed:dateRevised
2009-2-14
pubmed:meshHeading
pubmed-meshheading:2856171-1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine, pubmed-meshheading:2856171-15-Hydroxy-11 alpha,9..., pubmed-meshheading:2856171-Blood Platelets, pubmed-meshheading:2856171-Cell Membrane, pubmed-meshheading:2856171-Humans, pubmed-meshheading:2856171-Hydrazines, pubmed-meshheading:2856171-Isoquinolines, pubmed-meshheading:2856171-Piperazines, pubmed-meshheading:2856171-Polymyxin B, pubmed-meshheading:2856171-Polymyxins, pubmed-meshheading:2856171-Prostaglandin Endoperoxides, pubmed-meshheading:2856171-Prostaglandin Endoperoxides, Synthetic, pubmed-meshheading:2856171-Prostaglandins H, pubmed-meshheading:2856171-Protein Kinase Inhibitors, pubmed-meshheading:2856171-Receptors, Prostaglandin, pubmed-meshheading:2856171-Receptors, Thromboxane, pubmed-meshheading:2856171-Receptors, Thromboxane A2, Prostaglandin H2, pubmed-meshheading:2856171-Thromboxane A2
pubmed:year
1988
pubmed:articleTitle
Polymyxin B increases TXA2/PGH2 agonist and antagonist affinities in human platelet membranes.
pubmed:affiliation
Department of Cell and Molecular Pharmacology and Experimental Therapeutics, Medical University of South Carolina, Charleston 29425.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't