Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 µM the (S)-enantiomer of 16-HETE inhibits proximal tubule ATPase activity by as much as 60%, whereas the (R)-isomer has negligible effects on ATPase activity.
16-HETE is arachidonic acid metabolite through subterminal hydroxylation by cytochrome P-450. 16-HETE exhibits vasodilatory and PMN inhibitory effects and serves as biomarker for early stages of non-alcoholic fatty liver disease[1].
体外研究
16-HETE (0.01-1 μM) specifically inhibits the aggregation and adhesion of polymorphonuclear leukocytes, but has no significant effect on platelet function and blood pressure [1].
体内研究
16-HETE (1-20 μg, arterial injection) participates stereospecifically (S-enantiomer) in vasodilation, renal perfusion regulation, and tubular transport mechanisms in New Zealand white rabbits [2].
16-HETE (1 μg/kg/min) can inhibit the increase of intracranial pressure (ICP) in the thromboembolic stroke model of New Zealand white rabbits [1].
Animal Model:
New Zealand White rabbit
Dosage:
1-20 μg
Administration:
injection into artery
Result:
16S inhibited 60% ATPase activity at the concentration of 2 μM, while 16R enantiomer remained inactive.
Animal Model:
New Zealand White rabbit
Dosage:
1 μg/kg/min
Administration:
6 hours constant infusion from Hours 1 to 2 after autologous clot embolization
Result:
Reduced infarction area and less increased ICP.
分子式
C20H32O3
分子量
320.5
CAS号
128914-46-5
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bednar MM, et al., 16(R)-hydroxyeicosatetraenoic acid, a novel cytochrome P450 product of arachidonic acid, suppresses activation of human polymorphonuclear leukocyte and reduces intracranial pressure in a rabbit model of thromboembolic stroke. Neurosurgery. 2000 Dec;47(6):1410-8; discussion 1418-9.
[2]. Carroll MA, e al., Cytochrome P-450-dependent HETEs: profile of biological activity and stimulation by vasoactive peptides. Am J Physiol. 1996 Oct;271(4 Pt 2):R863-9.