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A highly potent and selective ETA endothelin receptor antagonist (Ki values are 1 nM and 7.3 μM at ETA and ETB subtypes respectively). Active in vivo.
|Storage||Desiccate at +4°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 100 mM in 1eq. HCl and to 100 mM in DMSO|
References are publications that support the biological activity of the product.
Aramori et al (1993) Subtype selectivity of a novel endothelin antagonist, FR139317, for the two endothelin receptors in transfected Chinese hamster ovary cells. Mol.Pharmacol. 43 127 PMID: 8429819
Palacios et al (2002) Role of endothelin ETA- and ETB-receptors in haemodynamic compensation following haemorrhage in anaesthetized rats. Br.J.Pharmacol. 135 876 PMID: 11861314
Rubanyi and Polokoff (1994) Endothelins: molecular biology, biochemistry, pharmacology, physiology, and pathophysiology. Pharmacol.Rev. 46 325 PMID: 7831383
Sogabe et al (1993) Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist. J.Pharmacol.Exp.Ther. 264 1040 PMID: 8450448
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Keywords: FR 139317, FR 139317 supplier, potent, selective, ETA, antagonists, Receptors, ET, EndothelinA, FR139317, Endothelin, 1210, Tocris Bioscience
1 Citation for FR 139317
Citations are publications that use Tocris products. Selected citations for FR 139317 include:
Khodorova et al (2009) Early and late contributions of glutamate and CGRP to mechanical sensitization by endothelin-1. J Pain 10 740 PMID: 19559390
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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.