| 1-O-alkyl-2-N-methylcarbamyl-glycerophosphocholine: a biologically potent, non-metabolizable analog of platelet-activating factor. | |
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MedLine Citation:
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PMID: 2820395 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We prepared unlabeled and 3H-labeled analogs of platelet-activating factor (PAF) containing a N-methylcarbamyl residue at the sn-2 position. PAF and its methylcarbamyl analog competed for binding to high affinity receptors on human polymorphonuclear neutrophils; their respective dissociation constants for these receptors were 0.2 and 1.1 nM. The binding affinities of the two analogs correlated precisely with their capacities to stimulate neutrophil degranulation responses. Unlike PAF, however, the methylcarbamyl analog completely resisted metabolic inactivation by neutrophils and by human sera. Thus, these compounds' biological potencies are determined predominantly by receptor binding: cellular metabolism of the ligands neither contributes to nor appreciably limits their stimulating actions. |
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Authors:
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J T O'Flaherty; J F Redman; J D Schmitt; J M Ellis; J R Surles; M H Marx; C Piantadosi; R L Wykle |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Biochemical and biophysical research communications Volume: 147 ISSN: 0006-291X ISO Abbreviation: Biochem. Biophys. Res. Commun. Publication Date: 1987 Aug |
Date Detail:
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Created Date: 1987-10-08 Completed Date: 1987-10-08 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0372516 Medline TA: Biochem Biophys Res Commun Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 18-24 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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1-Alkyl-2-acetylglycerophosphocholine Esterase Leukotriene B4 / pharmacology Neutrophils / drug effects, metabolism Phospholipases A / metabolism Phospholipid Ethers* Platelet Activating Factor / analogs & derivatives*, pharmacology Platelet Membrane Glycoproteins* Receptors, Cell Surface / metabolism Receptors, G-Protein-Coupled* Stereoisomerism Structure-Activity Relationship |
| Grant Support | |
ID/Acronym/Agency:
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HL-26257/HL/NHLBI NIH HHS; HL-26818/HL/NHLBI NIH HHS; HL-27799/HL/NHLBI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Phospholipid Ethers; 0/Platelet Activating Factor; 0/Platelet Membrane Glycoproteins; 0/Receptors, Cell Surface; 0/Receptors, G-Protein-Coupled; 0/platelet activating factor receptor; 111057-91-1/1-O-hexadecyl-2-N-methylcarbamylphosphatidylcholine; 71160-24-2/Leukotriene B4; EC 3.1.1.-/Phospholipases A; EC 3.1.1.47/1-Alkyl-2-acetylglycerophosphocholine Esterase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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