Characterization of the inhibitory prostanoid receptors on human neutrophils
| Autor: | Alan Wheeldon, C.J. Vardey |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Agonist
Prostaglandin Antagonists Neutrophils Leukotriene B4 medicine.drug_class Xanthones Prostaglandin E2 receptor Receptors Prostaglandin Prostanoic acid In Vitro Techniques Pharmacology chemistry.chemical_compound Oxygen Consumption Superoxides medicine Humans Prostaglandin E2 Receptor Hydantoins Zymosan Prostanoic Acids Prostanoid N-Formylmethionine Leucyl-Phenylalanine Xanthenes chemistry Biochemistry Prostaglandins lipids (amino acids peptides and proteins) Misoprostol Research Article medicine.drug |
| Zdroj: | British Journal of Pharmacology. 108:1051-1054 |
| ISSN: | 0007-1188 |
| DOI: | 10.1111/j.1476-5381.1993.tb13504.x |
| Popis: | 1. We have evaluated the effects of various prostanoid agonists on the release of leukotriene B4 (LTB4) and superoxide anions (O2-) from human neutrophils stimulated with opsonized zymosan (OZ) and formyl-methionyl-leucyl-phenylalanine (FMLP), respectively. 2. Prostaglandin E2 (PGE2) and PGD2 inhibited both OZ-induced LTB4 release (EC50 0.72 microM and 0.91 microM respectively), and FMLP-induced O2- release (EC50 0.42 microM and 0.50 microM respectively). PGF2 alpha, the TP-receptor agonist, U46619, and the IP-receptor agonist, iloprost, were also active, but were all at least an order of magnitude less potent than PGE2 and PGD2. 3. The EP2/EP3-receptor agonist, misoprostol, and the selective EP2-agonist, AH13205, were both effective inhibitors of LTB4 release, being approximately equipotent with and 16-times less potent than PGE2, respectively. In contrast, the EP1/EP3-receptor agonist, sulprostone, had no inhibitory activity at concentrations of up to 10 microM. 4. The selective DP-receptor agonist, BW245C, inhibited LTB4 release, (EC50 0.006 microM) being approximately 50 times more potent than PGD2. BW245C also inhibited O2- release, and this inhibition was antagonized competitively by the DP-receptor blocking drug, AH6809 (pA2 6.6). 5. These data indicate the presence of both inhibitory EP- and DP-receptors on the human neutrophil. The rank order of potency of EP-receptor agonists suggest that the EP-receptors are of the EP2-subtype. |
| Databáze: | OpenAIRE |
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