Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells

R. Reimer; H. K. Heim; K. F. Sewing; R. Muallem; H. S. Odes

doi:10.1016/0090-6980(92)90142-G

Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells

R. Reimer
, H. K. Heim
, K. F. Sewing
, R. Muallem
, H. S. Odes

Medical School for International Health

Research output: Contribution to journal › Article › peer-review

39 Scopus citations

Abstract

Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE₂, PGF_2α, 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. This 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.

Original language	English
Pages (from-to)	485-493
Number of pages	9
Journal	Prostaglandins
Volume	44
Issue number	5
DOIs	https://doi.org/10.1016/0090-6980(92)90142-G
State	Published - 1 Jan 1992

ASJC Scopus subject areas

Biochemistry
Endocrinology

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10.1016/0090-6980(92)90142-G

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title = "Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells",

abstract = "Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2α, 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. This 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.",

author = "R. Reimer and Heim, \{H. K.\} and Sewing, \{K. F.\} and R. Muallem and Odes, \{H. S.\}",

year = "1992",

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doi = "10.1016/0090-6980(92)90142-G",

language = "English",

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T1 - Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells

AU - Reimer, R.

AU - Heim, H. K.

AU - Sewing, K. F.

AU - Muallem, R.

AU - Odes, H. S.

PY - 1992/1/1

Y1 - 1992/1/1

N2 - Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2α, 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. This 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.

AB - Rank order of agonist potency for activation of adenylate cyclase by the naturally occurring prostanoids PGE2, PGF2α, 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. This 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.

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DO - 10.1016/0090-6980(92)90142-G

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AN - SCOPUS:0026464444

SN - 0090-6980

VL - 44

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EP - 493

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JF - Prostaglandins

IS - 5

ER -

Eefects of EP-receptor subtype specific agonists and other prostanoids on adenylate cyclase activity of duodenal epithelial cells

Abstract

ASJC Scopus subject areas

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