scholarly journals Phase I Trial of Pyragrel, a Novel Thromboxane Synthetase Inhibitor, to Evaluate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers

2019 ◽  
Vol 10 ◽  
Author(s):  
Chan Zou ◽  
Xiaocong Zuo ◽  
Jie Huang ◽  
Ye Hua ◽  
Shuang Yang ◽  
...  
Keyword(s):  
Phase I ◽  
Healthy Volunteers ◽  
Phase I Trial ◽  
Synthetase Inhibitor ◽  
Thromboxane Synthetase Inhibitor ◽  
Thromboxane Synthetase

Phase I Study of Y-20811, a New Long-Acting Thromboxane Synthetase Inhibitor by Oral Administration

1989 ◽  
Vol 29 (6) ◽  
pp. 568-576 ◽  
Author(s):  
Mitsuyoshi Nakashima ◽  
Toshihiko Uematsu ◽  
Yoshiharu Takiguchi ◽  
Atsuhiro Mizuno ◽  
Mitsutaka Kanamaru
Keyword(s):  
Oral Administration ◽  
Phase I ◽  
Phase I Study ◽  
Synthetase Inhibitor ◽  
Thromboxane Synthetase Inhibitor ◽  
Thromboxane Synthetase ◽  
Long Acting

Platelet changes after a saturated fat meal and their prevention by dazmegrel, a thromboxane synthetase inhibitor

Lipids ◽  
1987 ◽  
Vol 22 (3) ◽  
pp. 159-162 ◽  
Author(s):  
J. J. F. Belch ◽  
A. R. Saniabadi ◽  
K. McLaughlin ◽  
C. D. Forbes
Keyword(s):  
Saturated Fat ◽  
Synthetase Inhibitor ◽  
Thromboxane Synthetase Inhibitor ◽  
Thromboxane Synthetase ◽  
Fat Meal

Prevention of cerebral vasospasm after SAH with a thromboxane synthetase inhibitor, OKY-1581

1982 ◽  
Vol 57 (1) ◽  
pp. 74-82 ◽  
Author(s):  
Tomio Sasaki ◽  
Susumu Wakai ◽  
Takao Asano ◽  
Kintomo Takakura ◽  
Keiji Sano
Keyword(s):  
Cerebral Vasospasm ◽  
Morphological Changes ◽  
Content Type ◽  
Synthetase Inhibitor ◽  
Thromboxane Synthetase Inhibitor ◽  
Thromboxane Synthetase ◽  
Basilar Arteries ◽  
Blood Injection ◽  
Subarachnoid Blood ◽  
Fine Print

✓ The efficacy of thromboxane synthetase inhibitor in the prevention of cerebral vasospasm after subarachnoid hemorrhage (SAH) was evaluated in a prolonged experiment using dogs. Changes in the diameter of the basilar artery were followed by angiography, and morphological changes were studied by photomicroscopy and electron microscopy. As a thromboxane synthetase inhibitor, OKY-1581 (sodium-(E)-3-(4(-3-pyridylmethyl)phenyl)-2-methylacrylate)was used. Dogs received intravenous injections of 160 mg of OKY-1581 dissolved in 2 ml of physiological saline immediately after subarachnoid blood injection. Subsequently, the animals received continuous intravenous infusion of the drug at the rate of 4 gm/50 ml/24 hours until sacrifice 4 days after induction of SAH. Control dogs received subarachnoid blood injection without treatment with OKY-1581. Angiographic examination revealed that the late spasm was almost completely abolished by the treatment with OKY-1581. Early spasm was also prevented, but the drug's effect was less prominent than it was on the late spasm. Morphological study revealed degenerative changes in the endothelium and myonecrotic changes in the tunica media following SAH in the basilar arteries of the treated as well as the untreated dogs. However, corrugation of the internal elastic lamina was almost completely absent in the treated dogs. The above results indicate that a disproportionate synthesis of thromboxane A2 plays an important role in the evolution of chronic cerebral vasospasm following SAH, and that drugs such as OKY-1581 that selectively inhibit thromboxane synthetase might be useful in the prevention of vasospasm.

Attenuation of noradrenergic neurotransmission by the thromboxane synthetase inhibitor, UK 38,485

Life Sciences ◽  
1984 ◽  
Vol 35 (2) ◽  
pp. 221-228 ◽  
Author(s):  
Edwin K. Jackson ◽  
Howard D. Uderman ◽  
William A. Herzer ◽  
Robert A. Branch
Keyword(s):  
Synthetase Inhibitor ◽  
Thromboxane Synthetase Inhibitor ◽  
Thromboxane Synthetase
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