BQ-788 (sodium salt)
BQ-788 (sodium salt) structure
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Common Name | BQ-788 (sodium salt) | ||
|---|---|---|---|---|
| CAS Number | 156161-89-6 | Molecular Weight | 663.78000 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C34H50N5NaO7 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
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Endothelin-1 induces myofibrillar disarray and contractile vector variability in hypertrophic cardiomyopathy-induced pluripotent stem cell-derived cardiomyocytes.
J. Am. Heart Assoc. 3(6) , e001263, (2014) Despite the accumulating genetic and molecular investigations into hypertrophic cardiomyopathy (HCM), it remains unclear how this condition develops and worsens pathologically and clinically in terms of the genetic-environmental interactions. Establishing a h... |
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Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.
Am. J. Pathol. 184(11) , 3040-51, (2014) Retinopathy of prematurity adversely affects premature infants because of oxygen-induced damage of the immature retinal vasculature, resulting in pathological neovascularization (NV). Our pilot studies using the mouse model of oxygen-induced retinopathy (OIR)... |
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Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B.
J. Cereb. Blood Flow Metab. 35(3) , 402-11, (2015) Obstructive sleep apnea (OSA) is associated with cerebrovascular diseases. However, little is known regarding the effects of OSA on the cerebrovascular wall. We tested the hypothesis that OSA augments endothelin-1 (ET-1) constrictions of cerebral arteries. Re... |
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Novel antagonist of endothelin ETB1 and ETB2 receptors, BQ-788: effects on blood vessel and small intestine.
Biochem. Biophys. Res. Commun. 205 , 168, (1994) The effects of a peptide, BQ-788 [N-cis-2, 6-dimethyl-piperidinocarbonyl-L-gamma-methylleucyl-D-1- methoxycarbonyltryptophanyl-D-norleucine], on isolated blood vessel and small intestine were examined. In the rat aorta, BQ-788 antagonized the endothelium-depe... |
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Dissecting the functional significance of endothelin A receptors in peripheral nociceptors in vivo via conditional gene deletion.
Pain 148 , 206-14, (2010) The peptide endothelin-1 (ET1), which was originally identified as a vasoconstrictor, has emerged as a critical regulator of a number of painful conditions, including inflammatory pain and tumor-associated pain. There is considerable pharmacological evidence ... |
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Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788.
Proc. Natl. Acad. Sci. U. S. A. 91 , 4892, (1994) We describe the characteristics of a potent and selective endothelin (ET) B-receptor antagonist, BQ-788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D -1- methoxycarbonyltryptophanyl-D-norleucine]. In vitro, this compound potently and competitiv... |
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Krüppel-like factor 15 regulates BMPER in endothelial cells.
Carcinogenesis 85 , 551-9, (2010) Bone morphogenetic proteins (BMPs) are involved in embryonic and adult blood vessel formation in health and disease. Previous studies have shown that BMP endothelial cell precursor-derived regulator (BMPER) plays an important role in endothelial cell function... |
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Minimally modified LDL upregulates endothelin type A receptors in rat coronary arterial smooth muscle cells.
Mediators Inflamm. 2013 , 656570, (2013) Minimally modified low-density lipoprotein (mmLDL) is a risk factor for cardiovascular disease. The present study investigated the effects of mmLDL on the expression of endothelin type A (ET(A)) receptors in coronary arteries. Rat coronary arteries were organ... |
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Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells.
PLoS ONE 7 , e47662, (2012) Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease involving an activated endothelin system and aberrant contraction and proliferation ... |
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Antidiuretic effects of the endothelin receptor antagonist avosentan.
Front. Physiol. 3 , 103, (2012) Several clinical studies have investigated the potential benefits of endothelin receptor antagonism in chronic pathologies such as diabetic kidney disease. However, fluid retention and edema have been identified as major side effects of endothelin receptor an... |