aorta

Talibegron hydrochloride (ZD2079 hydrochloride) is a β3 adrenergic receptor agonist with a pD2 of 3.72 on phenylephrine-preconstricted rat mesenteric artery. It relaxes rat mesenteric artery and isolated aorta in vitro, and inhibits ob gene expression and circulating leptin levels in lean mice in vivo.

Acitemate(Chinoin 123) has an inhibitory effect on atherosclerosis and reduces the permeability of the aorta in rabbits fed a hyperlipidemic diet, which can be used to study atherosclerosis.

Valsartan (CGP 48933) is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension.

Selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-induced relaxation. Behav

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

Aorta, EC50: 4.88 nM

trans-Ned 19 is a NAADP antagonist and TPC blocker and inhibits the calcium signal in human umbilical vein endothelial cells and the rat aorta relaxation in response to low histamine concentrations.

FCE 28654 is a water-soluble acyl-CoA inhibitor.

Win-62005 is an inhibitor of cyclic AMP phosphodiesterase III (PDE III)(Kis: 25 and 26 nM for rat heart and canine aorta).

Piclamilast (RP 73401) is a PDE4 inhibitor.

AS604872 is a selective antagonist of the FP receptor.. AS604872 significantly accelerated degeneration of the media in both cerebral artery and aorta as evidenced by thinning of the media and disruption of the elastic lamina and promoted IA and aortic di

DHP-218 is a calcium channel antagonist. DHP-218 inhibits Calcium-induced contraction of the rat aorta in high K+ solution with the pA2 value of 9.11. The IC50 value for the inhibitory effects of DHP-218 in high K+-induced and phenylephrine-induced contra

GS 389 is a novel tetrahydroisoquinoline analog with vasorelaxant properties. GS-389 significantly inhibited cGMP phosphodiesterase from the rabbit brain and increased cGMP levels in the rat aorta.

ICI 169369, a 5-HT2/5-HT1C antagonist, can evoke endothelium-dependent relaxation in rabbit aorta.

PF-9404C is the S-S diesteroisomer of a beta adrenergic receptors blocker with vasodilatory properties. PF9404C increased the formation of cyclic GMP from 3 pmol mg−1 protein in basal conditions, to 53 pmol mg−1 protein in 10 μM in rat aorta smooth muscle

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

(±)12-HEPE is produced by non-enzymatic oxidation of EPA, resulting in equal amounts of 12(S)-HEPE and 12(R)-HEPE. The biological activity of (±)12-HEPE is likely mediated by one of the individual isomers, primarily the 12(S) isomer in mammalian systems. 12-HEPE inhibits platelet aggregation with an IC50 of 24 μM, similar to 12-HETE (IC50 = 25 μM), and both compounds also inhibit U46619-induced contraction of rat aorta with IC50 values between 8.6-8.8 μM. [1][2]

The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity. The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits. CAY10487 also exhibits antioxidant activity, inhibiting copper-mediated oxidation of low-density lipoprotein by about 75% at a concentration of 2 μM.

8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a metabolite of the isoprostane 8-iso PGF2α in rabbits, monkeys, and humans. 8-iso PGF2α is a prostaglandin-like product of non-specific lipid peroxidation. In humans and monkeys, exogenously infused 8-iso PGF2α is converted to metabolites with 2 or 4 carbon atoms removed from the top side chain by β-oxidation, with a similar pattern observed in tritiated 8-iso PGF2α-infused rabbits. Early in the infusion (within 1-2 minutes), 8-iso-15-keto PGF2α is a major component of the metabolite profile, primarily comprising unmetabolized 8-iso PGF2α. 8-iso-15-keto PGF2α is a vasoconstrictor when tested on the rat isolated thoracic aorta, acting via the TP (thromboxane) receptor.

Prostaglandin A1 (PGA1) was first isolated as a dehydration product of the PGE1 compounds found in human semen. 15-keto PGA1 is a metabolite of PGA1, produced by 15-hydroxy PG dehydrogenase. It can be produced from PGA1 in pig lung, trachea, aorta, and pulmonary artery tissue preparations. 15-keto PGA1, given at a concentration of 6 μM, causes vasoconstriction of rabbit lung that is comparable to that induced by angiotensin II.

Adrenomedullin (13-52) is a truncated form of adrenomedullin (1-52) . It induces nitric oxide-dependent relaxation of and inhibits release of angiotensin II and endothelin-1 from isolated rat aorta. In vivo, adrenomedullin (13-52) decreases mean arterial pressure (MAP) in spontaneously and renal hypertensive rats in a dose-dependent manner. Adrenomedullin (13-52) (10-3,000 ng per animal) reverses increases in lobar arterial pressure induced by U-46619 in a dose-dependent manner in cats but has no effect on basal lobar arterial pressure or systemic arterial pressure. It also potentiates inflammatory edema and neutrophil accumulation in rats.

9(R)-HODE is one of several monohydroxylated products of linoleic acid. All known mammalian lipoxygenases appear to catalyze the oxygenation of arachidonic and linoleic acid to give products having strictly the (S) configuration at the site of oxygen insertion. However, both human umbilical vein endothelial cells and bovine aorta endothelial cells have been shown to produce 9(R)-HODE when incubated with linoleic acid. The physiological function of 9(R)-HODE and the enzyme that catalyzes its formation have not been determined.

Etozolin HCl is a safe and effective diuretic agent in the treatment of acute cardiac failure. In isolated rings of guinea-pig aorta not responding to acetylcholine, the diuretic dexetozoline did not influence basal vascular tone but inhibited noradrenaline- and histamine-induced contractions. Dexetozoline has a very high bioavailability after oral administration and is fairly lipohilic. The half-life of etozolin is 2.5 h. Dexetozoline accumulates in cirrhosis.

ASM-IN-1 is a potent, orally active inhibitor of acid sphingomyelinase (ASM) with an IC50 of 1.5 µM, demonstrating antiatherosclerotic and anti-inflammatory activity. It effectively reduces lipid plaques in the aortic arch and aorta, along with decreasing plasma ceramide concentrations and oxidized LDL (Ox-LDL) levels [1].