Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells
Autor: | H. S. Odes, R. Muallem, R. Reimer, H.K. Heim, K.F. Sewing |
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Rok vydání: | 1992 |
Předmět: |
Male
Agonist endocrine system medicine.medical_specialty Duodenum medicine.drug_class medicine.medical_treatment Guinea Pigs Receptors Prostaglandin Adenylate kinase Prostaglandin In Vitro Techniques Biology Biochemistry Cyclase chemistry.chemical_compound Endocrinology Internal medicine medicine Animals Receptors Prostaglandin E Intestinal Mucosa Receptor Dibenz(b f)(1 4)oxazepine-10(11H)-carboxylic acid 8-chloro- 2-acetylhydrazide Prostaglandins E Prostanoid chemistry Prostaglandins lipids (amino acids peptides and proteins) Cyclase activity Adenylyl Cyclases Prostaglandin E |
Zdroj: | Prostaglandins. 44:485-493 |
ISSN: | 0090-6980 |
Popis: | Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2 alpha, PGD2, the stable PGI2 analogue iloprost, and the TXA2 mimetic U 46619, provides evidence for the existence of a distinct PGE-receptor on guinea-pig duodenal enterocytes. The PGE-receptor is likely to be of the EP2-subtype since the specific EP2-agonist 11-deoxy-PGE1 stimulated adenylate cyclase activity with a 20-fold higher potency than the EP1-agonist 17-phenyltrinor-PGE2 and the EP3-agonists MB 28767 and GR 63799. In addition, sulprostone (acting on both EP1- and EP3-receptors) was ineffective. Since the specific EP1-antagonist SC 19220 did not inhibit PGE2-stimulated adenylate cyclase activity, the involvement of EP1-receptors could be further excluded. The synthetic prostaglandin E-analogues misoprostol and nocloprost stimulated adenylate cyclase almost identically, though they were about 10-fold less potent than the natural PGE2. |
Databáze: | OpenAIRE |
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