thromboxane b2

Thromboxane B2 (a prostaglandin derivative released during anaphylaxis) induces platelet aggregation and arterial contraction.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

Thromboxane B2 (TXB2) is a compound significantly released from aggregating platelets and undergoes metabolic transformation during circulation into 11-dehydro TXB2 and 2,3-dinor TXB2. The latter, 2,3-dinor TXB2, serves as a prevalent urinary metabolite of TXB2 and acts as an indicator for in vivo TXA2 synthesis. Studies have shown that in healthy male volunteers, the median excretion rate of 2,3-dinor TXB2 is measured at 10.3 ng/hour, equivalent to 138 pg/mg of creatinine.

11-Dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite derived from the inactive TXA2 metabolite, TXB2. Its formation involves the action of cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation processes. Remarkably, levels of 11-dehydro-2,3-dinor TXB2 have been observed to increase by 5.2-fold in a surgery-induced rat model of tendon overuse, highlighting its potential role in physiological stress responses.

p-Hydroxycinnamic acid (NSC-59260) can inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

CI-949 is an allergic mediator release inhibitor that inhibits the release of leukotriene C4 D4 (LTC4 LTD4), histamine, and thromboxane B2 (TXB2) with IC50 values of 0.5 μM, 11.4 μM, and 0.1 μM, respectively.

Thromboxane B2 (TXB2) is released in substantial quantities from aggregating platelets and metabolized during circulation to 11-dehydro TXB2 and 2,3-dinor TXB2. In rats and rabbits, 2,3-dinor TXB1 has been identified as another urinary metabolite of TXB2. However in human urine, only trace amounts of 2,3-dinor TXB1 have been identified. In rats, 2,3-dinor TXB1 is excreted at a much higher rate than 2,3-dinor TXB2 (19.2 ± 4.9 ng/24 hr and 1.6 ± 0.3 ng/24 hr, respectively). Therefore, urinary 2,3-dinor TXB1 is a suitable marker of thromboxane biosynthesis in rats.

Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously express COX-2. Lornoxicam reduces LPS-induced production of nitric oxide and IL-6 in cell-based assays with IC50 values of 65 and 54 µM, respectively. It reduces carrageenan-induced paw edema in rats when administered intravenously at doses ranging from 0.1 to 9 mg kg. Formulations containing lornoxicam have been used in the management of postoperative pain.

KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.

2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside (Astragalus polyphenols) is a compound isolated from the roots of Polygonum species, which inhibits the formation of 5-HETE, HHT, and thromboxane B2.

Mulberrofuran Q is an active compound that inhibits the formation of 12-hydroxy-5,8,10-heptadecatrienoic acid (HHT) and thromboxane B2 (cyclooxygenase product) , which protects neuronal cells from hypoxia-glycorrhoea-deficiency (OGD)-induced oxidative stress.

Mulberrofuran A can inhibit the formations of 12-hydroxy-, 8, 10-heptadecatrienoic acid (HHT) and thromboxane B2, but it can increase the formation of 12-hydroxy-5, 8, 10, 14-eicosatetraenoic acid (12-HETE).

2,3-Dinor-8-iso Prostaglandin F1α (2,3-dinor-8-iso PGF1α), an isoprostane and active metabolite of arachidonic acid deriving its formation from non-enzymatic free radical peroxidation, acts as an active metabolite of the platelet aggregation inhibitor 8-iso PGF2α. This compound exhibits vasoconstrictive properties in isolated porcine retinal and brain microvessels with EC50 values of 12.8 and 18.5 nM, respectively, yet it does not cause contraction in isolated rat aortic rings at a concentration of 31 µM. Further, at a concentration of 1 µM, it raises thromboxane B2 (TXB2) levels in isolated porcine brain slices, an effect reversible by thromboxane A synthase inhibitor CGS 12970, voltage-gated calcium channel inhibitor SKF 96365, or the nicotinic acetylcholine receptor (nAChR) antagonist α-conotoxin.

1,2,3-Trilinoelaidoyl-rac-glycerol is a triacylglycerol that contains linoelaidic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trilinoelaidoyl-rac-glycerol (0.6-6.3% w/w) lowers serum levels of thromboxane B2 , prostaglandin F2 (PGF2), and PGE in rats.1 |1. Bruckner, G., Goswami, S., and Kinsella, J.E. Dietary trilinoelaidate: Effects on organ fatty acid composition, prostanoid biosynthesis and platelet function in rats. J. Nutr. 114(1), 58-67 (1984).

9-Oxononanoic Acid is an oxidized fatty acid, formed by the autoxidation of linoleic acid, which enhances phospholipase A2 (PLA2) activity and increases the production of thromboxane B2 in isolated human plasma.9-Oxononanoic Acid reduces hepatic neofatty acid synthesis and enhances the activity of rat hepatic carnitine palmitoyltransferase, a marker of β-oxidation. Activity.

Labdane F2 is an antagonist of thromboxane B2 and leukotriene B4 isolated from the Spanish herb Sideritis javalambrensis.

Thromboxane A2, as an unstable intermediate between the prostaglandin endoperoxides and thromboxane B2, is a potent inducer of platelet aggregation and causes vasoconstriction.

Glutinone (IC50=24 microM) shows a significant effect on thromboxane B2 (TXB2)-release induced by calcium ionophore in human platelets.