9,11-AZO-13-OXA-15-hydroxyprostanoic acid: A potent thromboxane synthetase inhibitor and a pgh2/txa2 receptor antagonist

Sheung Tsam Kam; Philip S. Portoghese; Earl W. Dunham; Jonathan M. Gerrard

doi:10.1016/0161-4630(79)90069-7

9,11-AZO-13-OXA-15-hydroxyprostanoic acid: A potent thromboxane synthetase inhibitor and a pgh2/txa2 receptor antagonist

Sheung Tsam Kam
, Philip S. Portoghese
, Earl W. Dunham
, Jonathan M. Gerrard

Medicinal Chemistry

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

11 Scopus citations

Abstract

9,11-Azo-13-oxa-15-hydroxyprostanoic acid (AOHP) is shown to be _a potent inhibitor of thromboxane synthetase with an IC₅₀ at about 10^-6M. It also blocked the agonist actions of 9,11-epoxymethano-PGH₂ IC₅₀ 9 × 10^-7M) and TXA₂ IC₅₀ 2.4 × 10^-6M) on human platelet-rich plasma indicating that it also is a PGH₂/TxA₂ receptor blocker.

Original language	English (US)
Pages (from-to)	279-289
Number of pages	11
Journal	Prostaglandins and Medicine
Volume	3
Issue number	5
DOIs	https://doi.org/10.1016/0161-4630(79)90069-7
State	Published - Nov 1979

Bibliographical note

Funding Information:
This work was supported in part by NIH research grant HL 16524 and HL 17871 and is abstracted in part from the Ph.D. thesis submitted by S. -T. Kam to the Graduate Faculty, University of Minnesota. The authors wish to thank Dr. G. Graff, Department of Pharmacology, University of Minnesota, for the [l-14C]PGH2 sample and Dr. J. E. Pike of the Upjohn Company for the prostaglandin standards.

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@article{98186b19a8f1419d91dc7112ceab239b,

title = "9,11-AZO-13-OXA-15-hydroxyprostanoic acid: A potent thromboxane synthetase inhibitor and a pgh2/txa2 receptor antagonist",

abstract = "9,11-Azo-13-oxa-15-hydroxyprostanoic acid (AOHP) is shown to be \_a potent inhibitor of thromboxane synthetase with an IC50 at about 10-6M. It also blocked the agonist actions of 9,11-epoxymethano-PGH2 IC50 9 × 10-7M) and TXA2 IC50 2.4 × 10-6M) on human platelet-rich plasma indicating that it also is a PGH2/TxA2 receptor blocker.",

author = "Kam, \{Sheung Tsam\} and Portoghese, \{Philip S.\} and Dunham, \{Earl W.\} and Gerrard, \{Jonathan M.\}",

note = "Funding Information: This work was supported in part by NIH research grant HL 16524 and HL 17871 and is abstracted in part from the Ph.D. thesis submitted by S. -T. Kam to the Graduate Faculty, University of Minnesota. The authors wish to thank Dr. G. Graff, Department of Pharmacology, University of Minnesota, for the [l-14C]PGH2 sample and Dr. J. E. Pike of the Upjohn Company for the prostaglandin standards.",

year = "1979",

month = nov,

doi = "10.1016/0161-4630(79)90069-7",

language = "English (US)",

volume = "3",

pages = "279--289",

journal = "Prostaglandins and Medicine",

issn = "0161-4630",

publisher = "Churchill Livingstone",

number = "5",

}

TY - JOUR

T1 - 9,11-AZO-13-OXA-15-hydroxyprostanoic acid

T2 - A potent thromboxane synthetase inhibitor and a pgh2/txa2 receptor antagonist

AU - Kam, Sheung Tsam

AU - Portoghese, Philip S.

AU - Dunham, Earl W.

AU - Gerrard, Jonathan M.

N1 - Funding Information: This work was supported in part by NIH research grant HL 16524 and HL 17871 and is abstracted in part from the Ph.D. thesis submitted by S. -T. Kam to the Graduate Faculty, University of Minnesota. The authors wish to thank Dr. G. Graff, Department of Pharmacology, University of Minnesota, for the [l-14C]PGH2 sample and Dr. J. E. Pike of the Upjohn Company for the prostaglandin standards.

PY - 1979/11

Y1 - 1979/11

N2 - 9,11-Azo-13-oxa-15-hydroxyprostanoic acid (AOHP) is shown to be _a potent inhibitor of thromboxane synthetase with an IC50 at about 10-6M. It also blocked the agonist actions of 9,11-epoxymethano-PGH2 IC50 9 × 10-7M) and TXA2 IC50 2.4 × 10-6M) on human platelet-rich plasma indicating that it also is a PGH2/TxA2 receptor blocker.

AB - 9,11-Azo-13-oxa-15-hydroxyprostanoic acid (AOHP) is shown to be _a potent inhibitor of thromboxane synthetase with an IC50 at about 10-6M. It also blocked the agonist actions of 9,11-epoxymethano-PGH2 IC50 9 × 10-7M) and TXA2 IC50 2.4 × 10-6M) on human platelet-rich plasma indicating that it also is a PGH2/TxA2 receptor blocker.

UR - https://www.scopus.com/pages/publications/0018730294

UR - https://www.scopus.com/pages/publications/0018730294#tab=citedBy

U2 - 10.1016/0161-4630(79)90069-7

DO - 10.1016/0161-4630(79)90069-7

M3 - Article

C2 - 233035

AN - SCOPUS:0018730294

SN - 0161-4630

VL - 3

SP - 279

EP - 289

JO - Prostaglandins and Medicine

JF - Prostaglandins and Medicine

IS - 5

ER -

9,11-AZO-13-OXA-15-hydroxyprostanoic acid: A potent thromboxane synthetase inhibitor and a pgh2/txa2 receptor antagonist

Abstract

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