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The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin F1 alpha in patients with ischemic cerebrovascular disease.
Stroke. 1985 Mar-Apr; 16(2):241-4.S

Abstract

Thromboxane synthetase activity is selectively inhibited by (E)-3-[4-(1-imidazolylmethyl)phenyl]-2-propenoic acid hydrochloride monohydrate (OKY-046). A single dose of 100 mg OKY-046 was orally administered to patients with ischemic cerebrovascular disease and healthy volunteers. Platelet aggregation and thromboxane B2 (TXB2) generation of intact and homogenised platelets induced by 1.0 mM sodium arachidonate were measured before and at 1, 4, 6 and 8 h after dosing. OKY-046 inhibited arachidonate-induced aggregation in platelet rich plasma from some, but not all, individuals, whereas platelet TXB2 generation was almost completely inhibited by a single dose of 100 mg OKY-046, in all of the patients and healthy volunteers. Endogenous TXA2 and prostacyclin (PGI2) biosynthesis were assessed by measurement of urinary immunoreactive TXB2 (i-TXB2) and 6-keto-PGF1 alpha (i-6-keto-PGF1 alpha) before and at 0-3, 3-6, 6-9 h after dosing. OKY-046 increased the urinary i-6-keto-PGF1 alpha coincidently with a decrease of urinary i-TXB2, both in patients and healthy volunteers. These effects of a selective thromboxane synthetase inhibitor will improve a disturbed balance between TXA2 and PGI2, associated with the development of ischemic cerebrovascular disease.

Authors

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Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

3883580

Citation

Uyama, O, et al. "The Effect of a Thromboxane Synthetase Inhibitor, OKY-046, On Urinary Excretion of Immunoreactive Thromboxane B2 and 6-keto-prostaglandin F1 Alpha in Patients With Ischemic Cerebrovascular Disease." Stroke, vol. 16, no. 2, 1985, pp. 241-4.
Uyama O, Nagatsuka K, Nakabayashi S, et al. The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin F1 alpha in patients with ischemic cerebrovascular disease. Stroke. 1985;16(2):241-4.
Uyama, O., Nagatsuka, K., Nakabayashi, S., Isaka, Y., Yoneda, S., Kimura, K., & Abe, H. (1985). The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin F1 alpha in patients with ischemic cerebrovascular disease. Stroke, 16(2), 241-4.
Uyama O, et al. The Effect of a Thromboxane Synthetase Inhibitor, OKY-046, On Urinary Excretion of Immunoreactive Thromboxane B2 and 6-keto-prostaglandin F1 Alpha in Patients With Ischemic Cerebrovascular Disease. Stroke. 1985 Mar-Apr;16(2):241-4. PubMed PMID: 3883580.
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TY - JOUR T1 - The effect of a thromboxane synthetase inhibitor, OKY-046, on urinary excretion of immunoreactive thromboxane B2 and 6-keto-prostaglandin F1 alpha in patients with ischemic cerebrovascular disease. AU - Uyama,O, AU - Nagatsuka,K, AU - Nakabayashi,S, AU - Isaka,Y, AU - Yoneda,S, AU - Kimura,K, AU - Abe,H, PY - 1985/3/1/pubmed PY - 1985/3/1/medline PY - 1985/3/1/entrez SP - 241 EP - 4 JF - Stroke JO - Stroke VL - 16 IS - 2 N2 - Thromboxane synthetase activity is selectively inhibited by (E)-3-[4-(1-imidazolylmethyl)phenyl]-2-propenoic acid hydrochloride monohydrate (OKY-046). A single dose of 100 mg OKY-046 was orally administered to patients with ischemic cerebrovascular disease and healthy volunteers. Platelet aggregation and thromboxane B2 (TXB2) generation of intact and homogenised platelets induced by 1.0 mM sodium arachidonate were measured before and at 1, 4, 6 and 8 h after dosing. OKY-046 inhibited arachidonate-induced aggregation in platelet rich plasma from some, but not all, individuals, whereas platelet TXB2 generation was almost completely inhibited by a single dose of 100 mg OKY-046, in all of the patients and healthy volunteers. Endogenous TXA2 and prostacyclin (PGI2) biosynthesis were assessed by measurement of urinary immunoreactive TXB2 (i-TXB2) and 6-keto-PGF1 alpha (i-6-keto-PGF1 alpha) before and at 0-3, 3-6, 6-9 h after dosing. OKY-046 increased the urinary i-6-keto-PGF1 alpha coincidently with a decrease of urinary i-TXB2, both in patients and healthy volunteers. These effects of a selective thromboxane synthetase inhibitor will improve a disturbed balance between TXA2 and PGI2, associated with the development of ischemic cerebrovascular disease. SN - 0039-2499 UR - https://www.unboundmedicine.com/medline/citation/3883580/The_effect_of_a_thromboxane_synthetase_inhibitor_OKY_046_on_urinary_excretion_of_immunoreactive_thromboxane_B2_and_6_keto_prostaglandin_F1_alpha_in_patients_with_ischemic_cerebrovascular_disease_ L2 - https://www.ahajournals.org/doi/10.1161/01.str.16.2.241?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -