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PMID: 1247563 Published · ppublish English Journal Article

Prostaglandin E1 high affinity binding sites of rat thymocytes. Specificity and blockade by non-steroidal antiinflammatory drugs and localization in a plasma membrane-enriched fraction.

Biochimica et biophysica acta ·Vol. 419 ·No. 2 ·1976-01-21 ·Pages 365-78

Grunnet I, Bojesen E

Abstract

Great specificity is demonstrated for the prostaglandin E1 high affinity binding sites of rat thymocytes. Whereas prostaglandin E2 has the same affinity as prostaglandin E1, 13 other prostaglandin derivatives and antagonists are bound with 2-1000 times smaller affinities. 50% inhibition of the high affinity binding of prostaglandin E1 to rat thymocytes is demonstrated for three non-steroidal antiinflammatory drugs, indomethacin (3.6. 10(-5) M), salicylic acid (2.9. 10(-3) M) and acetylsalicylic acid (2.10(-2) M). The low affinity binding of prostaglandin E1 is enhanced by the same concentration of indomethacin, however, to a lesser degree and more variable than the inhibition of the high affinity binding of prostaglandin E1. Like intact cells a 50-fold purified plasma membrane fraction, isolated from a homogenate of rat thymocytes, shows reversible high affinity binding of prostaglandin E1 as well as irreversible binding of unidentified tritiated compounds. The binding data are compatible with a localization in the plasma membrane of high affinity sites for reversible binding with a considerably higher dissociation constant than that found for whole cells. Their identity remains to be demonstrated.

MeSH Terms
Animals Aspirin/pharmacology Binding Sites Binding, Competitive Cell Membrane/drug effects,metabolism Female In Vitro Techniques Indomethacin/pharmacology Kinetics L-Lactate Dehydrogenase/metabolism Nucleotidases/metabolism Prostaglandins E/metabolism Prostaglandins E, Synthetic Protein Binding Rats Salicylates/pharmacology Structure-Activity Relationship Thymus Gland/drug effects,metabolism
Chemicals
Prostaglandins E Prostaglandins E, Synthetic Salicylates L-Lactate Dehydrogenase Nucleotidases Aspirin Indomethacin
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Grunnet I
Bojesen E
Article Info
Journal
Biochimica et biophysica acta
Abbr.
Biochim Biophys Acta
ISSN
0006-3002
Published
1976-01-21
Pages
365-78
Language
English
Region
Netherlands
NLM ID
0217513
Subset
IM
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