Antagonistic action of AA-2414 on thromboxane A2/prostaglandin endoperoxide receptor in platelets and blood vessels.

Imura, Yoshimi; Terashita, Zen‐ichi; Shibouta, Yumiko; Inada, Yuji; Nishikawa, Kohei

doi:10.1254/jjp.52.35

Cited by 16 publications

(6 citation statements)

References 18 publications

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“…22) The COX inhibitors aspirin and indomethacin, TXA 2 synthesis inhibitor ozagrel, and TXA 2 receptor antagonist seratrodast have been used for the treatment of these diseases. 13,14,23) In the present study, we showed for the first time that the extract from Piper longum L. had an inhibitory effect on platelet aggregation as a TXA 2 receptor antagonist. These…”

Section: Discussionsupporting

confidence: 53%

Inhibitory Effect of Ethanol Extract of Piper longum L. on Rabbit Platelet Aggregation through Antagonizing Thromboxane A2 Receptor

Iwashita

Saito

Yamaguchi³

et al. 2007

Biological & Pharmaceutical Bulletin

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Section: Discussionsupporting

confidence: 53%

Inhibitory Effect of Ethanol Extract of Piper longum L. on Rabbit Platelet Aggregation through Antagonizing Thromboxane A2 Receptor

Iwashita

Saito

Yamaguchi³

et al. 2007

Biological & Pharmaceutical Bulletin

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“…The affinities of TXA2-R antagonists to the receptor may differ (13,14,19,20,31). For picotamide, seratrodast, and L-655,240, different K i values for competition of TXA2-R ligands have been reported, based on studies performed in thrombocytes, vessels, or other models (13,14,19,20,31).…”

Section: Discussionmentioning

confidence: 99%

“…For picotamide, seratrodast, and L-655,240, different K i values for competition of TXA2-R ligands have been reported, based on studies performed in thrombocytes, vessels, or other models (13,14,19,20,31). Therefore, we used higher concentrations of picotamide, as of seratrodast and L-655,240.…”

Section: Discussionmentioning

confidence: 99%

“…U46619, picotamide, and L-665,240 were obtained from Enzo Life Sciences (Lörrach, Germany), seratrodast was obtained from Tocris (Bristol, UK), and phenylephrine and norepinephrine were obtained from Sigma (Munich, Germany). Concentrations of picotamide, L-665,240, and seratrodast were based on data from studies of platelets and vessels (13,14,19,20,31).…”

Section: Methodsmentioning

confidence: 99%

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The receptor antagonist picotamide inhibits adrenergic and thromboxane-induced contraction of hyperplastic human prostate smooth muscle

Hennenberg

Miljak

Herrmann

et al. 2013

American Journal of Physiology-Renal Physiology

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Inhibition of prostate smooth muscle contraction is an important strategy for medical treatment of lower urinary tract symptoms (LUTS). Besides α1-adrenoceptors, prostate smooth muscle contraction is induced by activation of thromboxane (TXA2) receptors (TXA2-R). Here, we examined the effects of the TXA2-R antagonist picotamide on contraction of human prostate tissue. Prostate tissues were obtained from radical prostatectomy. The effects of picotamide (300 μM), L-665,240 (3 μM), and seratrodast (3 μM) on U46619-, electric field stimulation- (EFS-), phenylephrine-, and norepinephrine-induced contractions were studied in organ baths. Expression of TXA2-R and TXA2 synthase (TXS) was examined by fluorescence stainings. Picotamide, seratrodast, and L-655,240 inhibited concentration-dependent contractions induced by the TXA2 analog U46619. Picotamide, but not seratrodast or L-655,240, inhibited frequency-dependent contractions induced by EFS. Picotamide inhibited concentration-dependent contractions induced by norepinephrine or by the selective α1-adrenoceptor agonist phenylephrine. In prostate strips, where only submaximal contraction by a low dose of phenylephrine was induced, application of U46619 raised tone to maximum phenylephrine-induced tension. Immunoreactivity for TXA2-R and TXS was observed in the stroma and in epithelial cells of glands. Colocalization of both immunoreactivites was observed with the smooth muscle markers calponin and α-smooth muscle actin, with the epithelial marker pan-cytokeratin, and with prostate-specific antigen in the stroma and glands. The receptor antagonist picotamide inhibits α1-adrenergic, TXA2-mediated, and EFS-induced contractions in the human prostate. To the best of our knowledge, this is the first antagonist able to inhibit two different contraction systems in the prostate.

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“…Combined TP antagonism/thromboxane synthase inhibition usually requires the presence of a (N)-imidazole (dazoxiben; Randall et al, 1981) or a pyridin-3-yl group (isbogrel; Imura et al, 1990;ridogrel, Hoet et al, 1990;Fig. 11) to combine with the heme site of the synthase (see Hsu et al, 1999).…”

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confidence: 99%

International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress

Woodward

Jones

Narumiya³

2011

Pharmacological Reviews

396

414

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Antagonistic action of AA-2414 on thromboxane A2/prostaglandin endoperoxide receptor in platelets and blood vessels.

Cited by 16 publications

References 18 publications

Inhibitory Effect of Ethanol Extract of Piper longum L. on Rabbit Platelet Aggregation through Antagonizing Thromboxane A2 Receptor

Inhibitory Effect of Ethanol Extract of Piper longum L. on Rabbit Platelet Aggregation through Antagonizing Thromboxane A2 Receptor

The receptor antagonist picotamide inhibits adrenergic and thromboxane-induced contraction of hyperplastic human prostate smooth muscle

International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress

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