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Selective ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively). Reduces ischemia-induced ventricular arrhythmias in a rat model.
(Modifications: Trp-1 = D-Trp, Val-4 = D-Val, Cyclized)
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solubility||Soluble to 0.10 mg/ml in water|
References are publications that support the biological activity of the product.
Agapitov and Haynes (2002) Role of endothelin in cardiovascular disease. J.Renin Angiotensin Aldosterone Syst. 3 1 PMID: 11984741
Ekelund et al (1994) Effects of selective ETB-receptor stimulation on arterial, venous and capillary functions in cat skeletal muscle. Br.J.Pharmacol. 112 887 PMID: 7921617
Makatani et al (2000) Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics. Eur.J.Pharmacol. 406 139 PMID: 11011045
Sakamoto et al (1993) Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J.Biol.Chem. 268 8547 PMID: 8473300
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Keywords: BQ-123, BQ-123 supplier, Selective, ETA, antagonists, Receptors, Endothelin, 1188, Tocris Bioscience
7 Citations for BQ-123
Citations are publications that use Tocris products. Selected citations for BQ-123 include:
Craig and Martin (2012) Dominance of flow-mediated constriction over flow-mediated dilatation in the rat carotid artery. Br J Pharmacol 167 527 PMID: 22537086
Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Am J Pathol 34 852 PMID: 24517977
Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Neurosci 184 3040 PMID: 25203536
Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol 171 5682 PMID: 25091502
Ou et al (2014) Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats. J Cell Physiol 229 489 PMID: 24105843
Mazzuca et al (2013) Enhanced endothelin receptor type B-mediated vasodilation and underlying [Ca2+]i in mesenteric microvessels of pregnant rats. Br J Pharmacol 169 1335 PMID: 23646960
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.