Imidazole: A selective inhibitor of thromboxane synthetase

Salvador Moncada; Stuart Bunting; Kevin Mullane; Peter Thorogood; John R. Vane; Amiram Raz; Philip Needleman

doi:10.1016/0090-6980(77)90232-5

Imidazole: A selective inhibitor of thromboxane synthetase

Salvador Moncada^*, Stuart Bunting, Kevin Mullane, Peter Thorogood, John R. Vane, Amiram Raz, Philip Needleman

^*Corresponding author for this work

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

252 Scopus citations

Abstract

Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG₂ and PGH₂) to thromboxane A₂ by platelet microsomes (IC₅₀: 22 μg/ml; determined by bioassay). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of ¹⁴C-thromboxane B₂ from ¹⁴C-PHG₂. Several imidazole analogues and other substances were tested but only 1-methyl-imidadole was more potent that imidazole iteself. The use of imidazole of inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.

Original language	English
Pages (from-to)	611-618
Number of pages	8
Journal	Prostaglandins
Volume	13
Issue number	4
DOIs	https://doi.org/10.1016/0090-6980(77)90232-5
State	Published - Apr 1977
Externally published	Yes

Funding

Funders	Funder number
National Institutes of Health	SCOR HL-17646, HE-14397

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10.1016/0090-6980(77)90232-5

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title = "Imidazole: A selective inhibitor of thromboxane synthetase",

abstract = "Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 μg/ml; determined by bioassay). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of 14C-thromboxane B2 from 14C-PHG2. Several imidazole analogues and other substances were tested but only 1-methyl-imidadole was more potent that imidazole iteself. The use of imidazole of inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.",

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T2 - A selective inhibitor of thromboxane synthetase

AU - Moncada, Salvador

AU - Bunting, Stuart

AU - Mullane, Kevin

AU - Thorogood, Peter

AU - Vane, John R.

AU - Raz, Amiram

AU - Needleman, Philip

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AB - Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 μg/ml; determined by bioassay). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of 14C-thromboxane B2 from 14C-PHG2. Several imidazole analogues and other substances were tested but only 1-methyl-imidadole was more potent that imidazole iteself. The use of imidazole of inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.

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Imidazole: A selective inhibitor of thromboxane synthetase

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