Pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A2 receptor antagonist

Tsong Long Hwang; Yung An Yeh; Ji Wang Chern; Che Ming Teng

doi:10.1016/S0306-3623(00)00046-X

Pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A₂ receptor antagonist

Tsong Long Hwang, Yung An Yeh, Ji Wang Chern, Che Ming Teng^*

^*Corresponding author for this work

National Taiwan University

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

6 Scopus citations

Abstract

The pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A₂ receptor blocking agent, was examined in this study. EK112 was found to be a angiotensin II receptor antagonist, as revealed by its competitive antagonism of angiotensin II-induced smooth muscle contraction (pA₂ value of 7.63 ± 0.14) in rabbit aorta. It also had an angiotensin II blocking action in guinea pig ileum (pA₂ value of 7.87 ± 0.67). Additionally, EK112 also possessed thromboxane A₂ receptor blocking activity, since it competitively antagonized aortic contractile responses elicited by U46619 and PGF(2α)(pK(B) values of 6.67 ± 0.09 and 6.24 ± 0.09, respectively) in rat. In contrast, EK112 did not affect the contractile responses to many other receptor agonists. EK112 did not mimic that of the angiotensin-converting enzyme (ACE) inhibitor, captopril, to enhance the muscle contraction elicited by bradykinin in guinea pig ileum, suggesting that EK112 did not inhibit ACE. Neither cyclic AMP nor cyclic GMP content in rat aortic rings was changed by EK112. These data demonstrate that EK112 is a selective antagonist of angiotensin II and thromboxane A₂ receptor. The order of this blocking potency is angiotensin II receptor > thromboxane A₂ receptor. (C) 2000 Elsevier Science Inc.

Original language	English
Pages (from-to)	25-31
Number of pages	7
Journal	General Pharmacology
Volume	34
Issue number	1
DOIs	https://doi.org/10.1016/S0306-3623(00)00046-X
State	Published - 01 2000
Externally published	Yes

Keywords

Angiotensin II
Angiotensin- converting enzyme
EK112
Receptor antagonist
Thromboxane A

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10.1016/S0306-3623(00)00046-X

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title = "Pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A2 receptor antagonist",

abstract = "The pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A2 receptor blocking agent, was examined in this study. EK112 was found to be a angiotensin II receptor antagonist, as revealed by its competitive antagonism of angiotensin II-induced smooth muscle contraction (pA2 value of 7.63 ± 0.14) in rabbit aorta. It also had an angiotensin II blocking action in guinea pig ileum (pA2 value of 7.87 ± 0.67). Additionally, EK112 also possessed thromboxane A2 receptor blocking activity, since it competitively antagonized aortic contractile responses elicited by U46619 and PGF(2α)(pK(B) values of 6.67 ± 0.09 and 6.24 ± 0.09, respectively) in rat. In contrast, EK112 did not affect the contractile responses to many other receptor agonists. EK112 did not mimic that of the angiotensin-converting enzyme (ACE) inhibitor, captopril, to enhance the muscle contraction elicited by bradykinin in guinea pig ileum, suggesting that EK112 did not inhibit ACE. Neither cyclic AMP nor cyclic GMP content in rat aortic rings was changed by EK112. These data demonstrate that EK112 is a selective antagonist of angiotensin II and thromboxane A2 receptor. The order of this blocking potency is angiotensin II receptor > thromboxane A2 receptor. (C) 2000 Elsevier Science Inc.",

keywords = "Angiotensin II, Angiotensin- converting enzyme, EK112, Receptor antagonist, Thromboxane A",

author = "Hwang, {Tsong Long} and Yeh, {Yung An} and Chern, {Ji Wang} and Teng, {Che Ming}",

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AU - Yeh, Yung An

AU - Chern, Ji Wang

AU - Teng, Che Ming

PY - 2000/1

Y1 - 2000/1

N2 - The pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A2 receptor blocking agent, was examined in this study. EK112 was found to be a angiotensin II receptor antagonist, as revealed by its competitive antagonism of angiotensin II-induced smooth muscle contraction (pA2 value of 7.63 ± 0.14) in rabbit aorta. It also had an angiotensin II blocking action in guinea pig ileum (pA2 value of 7.87 ± 0.67). Additionally, EK112 also possessed thromboxane A2 receptor blocking activity, since it competitively antagonized aortic contractile responses elicited by U46619 and PGF(2α)(pK(B) values of 6.67 ± 0.09 and 6.24 ± 0.09, respectively) in rat. In contrast, EK112 did not affect the contractile responses to many other receptor agonists. EK112 did not mimic that of the angiotensin-converting enzyme (ACE) inhibitor, captopril, to enhance the muscle contraction elicited by bradykinin in guinea pig ileum, suggesting that EK112 did not inhibit ACE. Neither cyclic AMP nor cyclic GMP content in rat aortic rings was changed by EK112. These data demonstrate that EK112 is a selective antagonist of angiotensin II and thromboxane A2 receptor. The order of this blocking potency is angiotensin II receptor > thromboxane A2 receptor. (C) 2000 Elsevier Science Inc.

AB - The pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A2 receptor blocking agent, was examined in this study. EK112 was found to be a angiotensin II receptor antagonist, as revealed by its competitive antagonism of angiotensin II-induced smooth muscle contraction (pA2 value of 7.63 ± 0.14) in rabbit aorta. It also had an angiotensin II blocking action in guinea pig ileum (pA2 value of 7.87 ± 0.67). Additionally, EK112 also possessed thromboxane A2 receptor blocking activity, since it competitively antagonized aortic contractile responses elicited by U46619 and PGF(2α)(pK(B) values of 6.67 ± 0.09 and 6.24 ± 0.09, respectively) in rat. In contrast, EK112 did not affect the contractile responses to many other receptor agonists. EK112 did not mimic that of the angiotensin-converting enzyme (ACE) inhibitor, captopril, to enhance the muscle contraction elicited by bradykinin in guinea pig ileum, suggesting that EK112 did not inhibit ACE. Neither cyclic AMP nor cyclic GMP content in rat aortic rings was changed by EK112. These data demonstrate that EK112 is a selective antagonist of angiotensin II and thromboxane A2 receptor. The order of this blocking potency is angiotensin II receptor > thromboxane A2 receptor. (C) 2000 Elsevier Science Inc.

KW - Angiotensin II

KW - Angiotensin- converting enzyme

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KW - Receptor antagonist

KW - Thromboxane A

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Pharmacological characterization of EK112, a new combined angiotensin II and thromboxane A₂ receptor antagonist

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