AD 6, a coronary dilating agent, stimulates PGI2 production in rat aorta ex vivo and in human endothelial cells in culture

E. Dejana; C. de Castellarnau; G. Balconi; D. Rotilio; A. Pietra; G. de Gaetano

doi:10.1016/S0031-6989(82)80077-5

AD 6, a coronary dilating agent, stimulates PGI2 production in rat aorta ex vivo and in human endothelial cells in culture

E. Dejana, C. de Castellarnau, G. Balconi, D. Rotilio, A. Pietra, G. de Gaetano

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Abstract

AD6(8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carbonyl-methoxy-coumarin) reportedly exerts specific coronary vasodilatory activity and reduces platelet aggregation in laboratory animals. We investigated whether AD6 stimulates prostacyclin (PGI₂) synthesis by vascular cells. AD6 treatment of rats induced a dose dependent enhancement of prostacyclin (PGI2) synthesis by rings of thoracic aorta measured by bioassay and confirmed by thin layer radio-chromatography of the products of ¹⁴C arachidonic acid(¹⁴CAA) metabolism. In vitro incubation of the drug with cultured human endothelial cells caused a concentration dependent stimulation of PGI2 production measured by radioimmunoassay of 6keto PGF1_α. It is proposed that the previously described vasodilatory activity of the drug might be mediated through the stimulation of PGI2 release.

Original language	English
Pages (from-to)	719-724
Number of pages	6
Journal	Pharmacological Research Communications
Volume	14
Issue number	8
DOIs	https://doi.org/10.1016/S0031-6989(82)80077-5
Publication status	Published - 1982

ASJC Scopus subject areas

Pharmacology

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10.1016/S0031-6989(82)80077-5

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title = "AD 6, a coronary dilating agent, stimulates PGI2 production in rat aorta ex vivo and in human endothelial cells in culture",

abstract = "AD6(8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carbonyl-methoxy-coumarin) reportedly exerts specific coronary vasodilatory activity and reduces platelet aggregation in laboratory animals. We investigated whether AD6 stimulates prostacyclin (PGI2) synthesis by vascular cells. AD6 treatment of rats induced a dose dependent enhancement of prostacyclin (PGI2) synthesis by rings of thoracic aorta measured by bioassay and confirmed by thin layer radio-chromatography of the products of 14C arachidonic acid(14CAA) metabolism. In vitro incubation of the drug with cultured human endothelial cells caused a concentration dependent stimulation of PGI2 production measured by radioimmunoassay of 6keto PGF1α. It is proposed that the previously described vasodilatory activity of the drug might be mediated through the stimulation of PGI2 release.",

author = "E. Dejana and {de Castellarnau}, C. and G. Balconi and D. Rotilio and A. Pietra and {de Gaetano}, G.",

year = "1982",

doi = "10.1016/S0031-6989(82)80077-5",

language = "English",

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pages = "719--724",

journal = "Pharmacological Research",

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T1 - AD 6, a coronary dilating agent, stimulates PGI2 production in rat aorta ex vivo and in human endothelial cells in culture

AU - Dejana, E.

AU - de Castellarnau, C.

AU - Balconi, G.

AU - Rotilio, D.

AU - Pietra, A.

AU - de Gaetano, G.

PY - 1982

Y1 - 1982

N2 - AD6(8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carbonyl-methoxy-coumarin) reportedly exerts specific coronary vasodilatory activity and reduces platelet aggregation in laboratory animals. We investigated whether AD6 stimulates prostacyclin (PGI2) synthesis by vascular cells. AD6 treatment of rats induced a dose dependent enhancement of prostacyclin (PGI2) synthesis by rings of thoracic aorta measured by bioassay and confirmed by thin layer radio-chromatography of the products of 14C arachidonic acid(14CAA) metabolism. In vitro incubation of the drug with cultured human endothelial cells caused a concentration dependent stimulation of PGI2 production measured by radioimmunoassay of 6keto PGF1α. It is proposed that the previously described vasodilatory activity of the drug might be mediated through the stimulation of PGI2 release.

AB - AD6(8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carbonyl-methoxy-coumarin) reportedly exerts specific coronary vasodilatory activity and reduces platelet aggregation in laboratory animals. We investigated whether AD6 stimulates prostacyclin (PGI2) synthesis by vascular cells. AD6 treatment of rats induced a dose dependent enhancement of prostacyclin (PGI2) synthesis by rings of thoracic aorta measured by bioassay and confirmed by thin layer radio-chromatography of the products of 14C arachidonic acid(14CAA) metabolism. In vitro incubation of the drug with cultured human endothelial cells caused a concentration dependent stimulation of PGI2 production measured by radioimmunoassay of 6keto PGF1α. It is proposed that the previously described vasodilatory activity of the drug might be mediated through the stimulation of PGI2 release.

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JO - Pharmacological Research

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ER -

AD 6, a coronary dilating agent, stimulates PGI2 production in rat aorta ex vivo and in human endothelial cells in culture

Abstract

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