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Intravenous infusion of a selective inhibitor of thromboxane A2 synthetase in man: influence on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation.
Circulation 1984; 70(4):599-605Circ

Abstract

The effect of the selective thromboxane A2 synthetase inhibitor OKY-1581, a pyridine derivative [sodium (E)-3-(4-(3-pyridylmethyl)phenyl)-2-methyl-2-propenoate], on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation was studied in human volunteers. To clarify its effectiveness as an enzyme inhibitor, OKY-1581, at doses of 17, 83, 167, 417, 833, and 1667 micrograms/kg (n = 5 for each group), was injected intravenously, or was infused (10 micrograms/kg/min; n = 5) over 3 hr on 3 successive days. OKY-1580 (OKY-1581 free acid) was rapidly converted to its main beta-oxidized product, OKY-1565, and its reduced form, OKY-1558. During the study, plasma thromboxane B2 levels, inhibition of thromboxane B2 production in serum, and inhibition of rabbit platelet thromboxane A2 synthetase were monitored continuously. Twenty-five minutes after the injection of the above doses, plasma thromboxane B2 levels decreased by 4 +/- 7%, 40 +/- 14%, 57 +/- 7%, 68 +/- 6%, 93 +/- 5%, and 96 +/- 5% (mean +/- SD), respectively. Thromboxane B2 production in serum was decreased by 2 +/- 8%, 70 +/- 10%, 75 +/- 8%, 81 +/- 10%, and 96 +/- 8%, respectively, and rabbit platelet thromboxane A2 synthetase by 2 +/- 7%, 52 +/- 8%, 79 +/- 10%, 80 +/- 9%, 96 +/- 8%, and 95 +/- 7%. These parameters returned to the control levels 24 hr after the injection.(

ABSTRACT

TRUNCATED AT 250 WORDS)

Authors

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Pub Type(s)

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

Language

eng

PubMed ID

6434196

Citation

Yui, Y, et al. "Intravenous Infusion of a Selective Inhibitor of Thromboxane A2 Synthetase in Man: Influence On Thromboxane B2 and 6-keto-prostaglandin F1 Alpha Levels and Platelet Aggregation." Circulation, vol. 70, no. 4, 1984, pp. 599-605.
Yui Y, Hattori R, Takatsu Y, et al. Intravenous infusion of a selective inhibitor of thromboxane A2 synthetase in man: influence on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation. Circulation. 1984;70(4):599-605.
Yui, Y., Hattori, R., Takatsu, Y., Nakajima, H., Wakabayashi, A., Kawai, C., ... Tsubojima, M. (1984). Intravenous infusion of a selective inhibitor of thromboxane A2 synthetase in man: influence on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation. Circulation, 70(4), pp. 599-605.
Yui Y, et al. Intravenous Infusion of a Selective Inhibitor of Thromboxane A2 Synthetase in Man: Influence On Thromboxane B2 and 6-keto-prostaglandin F1 Alpha Levels and Platelet Aggregation. Circulation. 1984;70(4):599-605. PubMed PMID: 6434196.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Intravenous infusion of a selective inhibitor of thromboxane A2 synthetase in man: influence on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation. A1 - Yui,Y, AU - Hattori,R, AU - Takatsu,Y, AU - Nakajima,H, AU - Wakabayashi,A, AU - Kawai,C, AU - Kayama,N, AU - Hiraku,S, AU - Inagawa,T, AU - Tsubojima,M, PY - 1984/10/1/pubmed PY - 1984/10/1/medline PY - 1984/10/1/entrez SP - 599 EP - 605 JF - Circulation JO - Circulation VL - 70 IS - 4 N2 - The effect of the selective thromboxane A2 synthetase inhibitor OKY-1581, a pyridine derivative [sodium (E)-3-(4-(3-pyridylmethyl)phenyl)-2-methyl-2-propenoate], on thromboxane B2 and 6-keto-prostaglandin F1 alpha levels and platelet aggregation was studied in human volunteers. To clarify its effectiveness as an enzyme inhibitor, OKY-1581, at doses of 17, 83, 167, 417, 833, and 1667 micrograms/kg (n = 5 for each group), was injected intravenously, or was infused (10 micrograms/kg/min; n = 5) over 3 hr on 3 successive days. OKY-1580 (OKY-1581 free acid) was rapidly converted to its main beta-oxidized product, OKY-1565, and its reduced form, OKY-1558. During the study, plasma thromboxane B2 levels, inhibition of thromboxane B2 production in serum, and inhibition of rabbit platelet thromboxane A2 synthetase were monitored continuously. Twenty-five minutes after the injection of the above doses, plasma thromboxane B2 levels decreased by 4 +/- 7%, 40 +/- 14%, 57 +/- 7%, 68 +/- 6%, 93 +/- 5%, and 96 +/- 5% (mean +/- SD), respectively. Thromboxane B2 production in serum was decreased by 2 +/- 8%, 70 +/- 10%, 75 +/- 8%, 81 +/- 10%, and 96 +/- 8%, respectively, and rabbit platelet thromboxane A2 synthetase by 2 +/- 7%, 52 +/- 8%, 79 +/- 10%, 80 +/- 9%, 96 +/- 8%, and 95 +/- 7%. These parameters returned to the control levels 24 hr after the injection.(ABSTRACT TRUNCATED AT 250 WORDS) SN - 0009-7322 UR - https://www.unboundmedicine.com/medline/citation/6434196/Intravenous_infusion_of_a_selective_inhibitor_of_thromboxane_A2_synthetase_in_man:_influence_on_thromboxane_B2_and_6_keto_prostaglandin_F1_alpha_levels_and_platelet_aggregation_ L2 - http://www.ahajournals.org/doi/full/10.1161/01.cir.70.4.599?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -