Pfam box Symbol Endothelin Name Endothelin family image 1EDN human endothelin1 02.png width caption Pfam ... PDB3 1srb 150 170 protein Name Endothelin 1 caption image width HGNCid 3176 Symbol EDN1 AltSymbols ... LocusSupplementaryData p24 protein Name Endothelin 2 image width caption Symbol Endothelin 2 EDN2 AltSymbols ... protein Name Endothelin 3 image width caption Symbol EDN3 AltSymbols ATC prefix ... cite journal author Agapitov AV, Haynes WG title Role of endothelin in cardiovascular disease ... S title Pharmacology and physiopathology of the brain endothelin system an overview journal Curr. Med ... and two key Receptor biochemistry receptor types, Endothelin receptor ET sub A sub and ET sub B sub see Endothelin 1 EDN1 , Endothelin 2 EDN2 , Endothelin 3 EDN3 . ET sub A sub receptors are found in the smooth muscle tissue of blood vessel s, and binding of endothelin to ET sub A sub increases ... endothelin system in hypertension recent patents and discoveries journal Recent Pat Cardiovasc ... cells that line the interior of the blood vessels. When endothelin binds to ET sub B sub receptors ... and vascular functions. ref name pmid9239759 cite journal author Barnes K, Turner AJ title The endothelin system and endothelin converting enzyme in the brain molecular and cellular studies journal ... s for endothelin are present in blood vessels and cells of the brain, choroid plexus and peripheral ... of stroke , endothelin 1 caused severe metabolic stimulation and seizures with substantial decreases ... Intraventricular endothelin 1 uncouples the blood flow metabolism relationship in periventricular ... A similar strong vasoconstrictor action of endothelin 1 was demonstrated in a peripheral neuropathy ... ischemia induced by epineurial endothelin in the rat sciatic nerve journal Am. J. Physiol ... individual, a delicate balance between vasoconstriction and vasodilation is maintained by endothelin ... on the other. Overproduction of endothelin in the lungs may cause pulmonary hypertension , which ... more details
PBB geneid 1906 Endothelin 1 , also known as EDN1 , is a human gene and the corresponding peptide, one of three isoform s of human endothelin . The PBB Summary template is automatically maintained by Protein Box Bot. See Template PBB Controls to Stop updates. PBB Summary section title summary text Further reading refbegin 2 PBB Further reading citations cite journal author Bruno CM, Neri S, Di Prima P, Sciacca C title Pathophysiology of endothelin and medical emergencies. journal Panminerva medica volume 45 issue 2 pages 151 4 year 2003 pmid 12855940 doi cite journal author Doggrell SA title The endothelin system and its role in acute myocardial infarction. journal Expert Opin. Ther. Targets volume 8 issue 3 pages 191 201 year 2006 pmid 15161426 doi 10.1517 14728222.8.3.191 cite journal author Beghetti M, Black SM, Fineman JR title Endothelin 1 in congenital heart disease. journal Pediatr. Res. volume 57 issue 5 Pt 2 pages 16R 20R year 2005 pmid 15817494 doi 10.1203 01.PDR.0000160447.83332.13 cite journal author Cazaubon S, Deshayes F, Couraud PO, Nahmias C title Endothelin 1, angiotensin II and cancer journal Med Sci Paris volume 22 issue 4 pages 416 22 year 2006 pmid 16597412 doi 10.1051 medsci 2006224416 cite journal author Ariza AC, Bobadilla NA, Halhali A title Endothelin 1 and angiotensin II in preeeclampsia journal Rev. Invest. Clin. volume 59 issue 1 pages 48 56 year 2007 pmid 17569300 doi refend gene 6 stub The PBB Controls template provides controls for Protein Box Bot, please see Template PBB Controls for details. PBB Controls update page yes require manual inspection no update protein box yes update summary yes update citations yes ... more details
protein Name endothelin receptor type A caption image width HGNCid 3179 Symbol EDNRA AltSymbols EntrezGene 1909 OMIM 131243 RefSeq NM 001957 UniProt P25101 PDB ECnumber Chromosome 4 Arm q Band 31.2 LocusSupplementaryData protein Name endothelin receptor type B caption image width HGNCid 3180 Symbol EDNRB AltSymbols HSCR2, HSCR EntrezGene 1910 OMIM 131244 RefSeq NM 000115 UniProt P24530 PDB ECnumber Chromosome 13 Arm q Band 22 LocusSupplementaryData There are at least three known endothelin receptors , ET sub A sub , ET sub B1 sub and ET sub B2 sub , all of which are G protein coupled receptor s whose activation result in elevation of intracellular free calcium . ref name pmid12037137 cite journal author Davenport AP title International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature journal Pharmacol. Rev. volume 54 issue 2 pages 219 26 year 2002 pmid 12037137 doi 10.1124 pr.54.2.219 ref Clinical significance It is associated with ABCD syndrome ref name pmid11891690 cite journal author Verheij JB, Kunze J, Osinga J, van Essen AJ, Hofstra RM title ABCD syndrome is caused by a homozygous mutation in the EDNRB gene journal Am. J. Med. Genet. volume 108 issue 3 pages 223 5 year 2002 pmid 11891690 doi 10.1002 ajmg.10172 ref and some forms of Waardenburg syndrome . ref name pmid9279758 cite journal author Read AP, Newton VE title Waardenburg syndrome journal J. Med. Genet. volume 34 issue 8 pages 656 65 year 1997 pmid 9279758 doi 10.1136 jmg.34.8.656 pmc 1051028 ref See also Endothelin receptor antagonist References Reflist External links cite web url http www.iuphar db.org GPCR ChapterMenuForward?chapterID 1283 title Endothelin Receptors accessdate author authorlink coauthors date format work IUPHAR Database of Receptors and Ion Channels publisher International Union of Basic and Clinical Pharmacology pages language archiveurl archivedate quote MeshName Endothelin receptor transmembranereceptor stub G protein coupled receptors Category G protein coupled ... more details
PBB geneid 1908 Endothelin 3 is a protein that in humans is encoded by the EDN3 gene . ref name entrez cite web title Entrez Gene EDN3 endothelin 3 url http www.ncbi.nlm.nih.gov sites entrez?Db gene&Cmd ... text The protein encoded by this gene is a member of the endothelin family. Endothelins are endothelium ... for endothelin receptor type B EDNRB . The interaction of this endothelin with EDNRB is essential ... cite web title Entrez Gene EDN3 endothelin 3 url http www.ncbi.nlm.nih.gov sites entrez?Db gene&Cmd ... AP, et al. title Presence of messenger ribonucleic acid for endothelin 1, endothelin 2, and endothelin ... Solution structure of endothelin 3 determined using NMR spectroscopy. journal Biochemistry volume 31 ... C, Hansmann I title The gene for the novel vasoactive peptide endothelin 3 EDN3 is localized ... Chromosomal assignments of the human endothelin family genes the endothelin 1 gene EDN1 to 6p23 p24, the endothelin 2 gene EDN2 to 1p34, and the endothelin 3 gene EDN3 to 20q13.2 q13.3. journal Am. J ... Onda H, Ohkubo S, Ogi K, et al. title One of the endothelin gene family, endothelin 3 gene, is expressed ... of human endothelin by cathepsin E. journal FEBS Lett. volume 273 issue 1 2 pages 99 102 year ... T title cDNA cloning and chromosomal assignment of the gene encoding endothelin 3 journal ... A, Yanagisawa M, Kimura S, et al. title The human endothelin family three structurally and pharmacologically ... journal author Yu JC, Davenport AP title Secretion of endothelin 1 and endothelin 3 by human cultured ... of endothelin 3 with endothelin B receptor is essential for development of epidermal melanocytes ... 0092 8674 94 90018 3 cite journal author Edery P, Atti T, Amiel J, et al. title Mutation of the endothelin ... Hofstra RM, Osinga J, Tan Sindhunata G, et al. title A homozygous mutation in the endothelin 3 gene ... journal author Lahav R, Ziller C, Dupin E, Le Douarin NM title Endothelin 3 promotes neural crest cell ... 39455 cite journal author Bolk S, Angrist M, Xie J, et al. title Endothelin 3 frameshift mutation ... more details
PBB geneid 1907 Endothelin 2 , also known as ET 2 , is a protein that in humans is encoded by the EDN2 gene . ref name entrez cite web title Entrez Gene endothelin 2 url http www.ncbi.nlm.nih.gov sites entrez?Db gene&Cmd ShowDetailView&TermToSearch 1907 accessdate ref Function Endothelin 2 is a member of the endothelin protein family of secretory vasoconstrictive peptides. The preproprotein is processed to a short mature form which functions as a ligand for the endothelin receptor s that initiate intracellular signaling events. This gene product is involved in a wide range of biological processes, such as hypertension and ovulation . ref name entrez References reflist Further reading refbegin 2 cite journal author Arjomand Nahad F, Landt O, Stangl K, et al. title Fifteen polymorphisms in endothelin 1, endothelin 2 and endothelin receptor A genotyped by four duplex assays and seven simple assays on a LightCycler using hybridization probes. journal Clin. Chem. Lab. Med. volume 44 issue 8 pages 929 32 year 2006 pmid 16879056 doi 10.1515 CCLM.2006.180 cite journal author Ryckman KK, Morken NH, White MJ, et al. title Maternal and fetal genetic associations of PTGER3 and PON1 with preterm ... increased circulating endothelin 2 in primary biliary cirrhosis. journal Aliment. Pharmacol. Ther ... E, Saida K title Endothelin 2 vasoactive intestinal contractor regulation of expression via reactive ... 2734952 cite journal author Wiesmann F, Veeck J, Galm O, et al. title Frequent loss of endothelin 3 ... Meidan R, Levy N title The ovarian endothelin network an evolving story. journal Trends Endocrinol ... Rebourcet R, Mignot TM, Robert B, Ferr F title Endothelin 2 down regulation occurs in parallel ... author Nagai T, Ogimoto A, Okayama H, et al. title A985G polymorphism of the endothelin 2 gene ... A, et al. title A role for endothelin 2 and its receptors in breast tumor cell invasion. journal ... 10.1074 jbc.M512330200 cite journal author Sun de J, Liu Y, Lu DC, et al. title Endothelin 3 growth ... more details
A endothelin receptor antagonist ERA is a medication drug that blocks endothelin receptors. Three main kinds of ERAs exist selective ET sub A sub receptor antagonists sitaxentan , ambrisentan , atrasentan , BQ 123 , zibotentan , which affect Endothelin receptor type A endothelin A receptors . dual antagonists bosentan , tezosentan , which affect both endothelin A and Endothelin receptor type B B receptors . ref http cvpharmacology.com vasodilator ETblockers.htm Endothelin receptor antagonists Bot generated title ref selective ET sub B sub receptor antagonists BQ 788 and A192621 which affect Endothelin receptor type B endothelin B receptors are used in research but have not yet reached the clinical trial stage. Sitaxentan, ambrisentan and bosentan are mainly used for the treatment of pulmonary arterial hypertension , while atrasentan is an experimental anti cancer drug. See also Endothelin receptor References references Receptor agonists and antagonists PAH rx Antihypertensives and diuretics Category Endothelin receptor antagonists treatment stub sr Antagonist endotelinkog receptora ... more details
PBB geneid 1909 Endothelin receptor type A , also known as ET sub A sub , is a human G protein coupled receptor . ref name entrez cite web title Entrez Gene EDNRA endothelin receptor type A url http www.ncbi.nlm.nih.gov .... PBB Summary section title summary text Interactions Endothelin receptor type A has been shown ... H J authorlink coauthors Chun M, Kandror K V date May 2001 title Tip60 and HDAC7 interact with the endothelin ... and HTATIP . ref name pmid11262386 See also Endothelin receptor References reflist External links cite web url http www.iuphar db.org GPCR ReceptorDisplayForward?receptorID 2263 title Endothelin Receptors ... author Arai H, Nakao K, Hosoda K, et al. title Molecular cloning of human endothelin receptors and their expression ... the human endothelin A receptor. journal J. Biol. Chem. volume 267 issue 26 pages 18797 804 year ... of a human endothelin receptor subtype A. journal Am. J. Med. Sci. volume 304 issue 4 pages ... K, Hiroshi Arai, et al. title Cloning and expression of human endothelin 1 receptor cDNA. journal ... endothelin ETA receptor journal Biochem. Biophys. Res. Commun. volume 181 issue 1 pages 184 ... Y, Miyamoto C title Cloning and characterization of cDNA encoding human A type endothelin receptor ... and functional expression of a vascular smooth muscle endothelin 1 receptor journal Proc. Natl ... of guanine nucleotide binding regulatory proteins which couple to endothelin receptors journal Eur ... of endothelin receptor subtypes in the human prostate journal Mol. Pharmacol. volume 45 issue 2 pages ... of the human endothelin receptors journal J. Biol. Chem. volume 268 issue 6 pages 3873 ... RNA splicing of the human endothelin A receptor generates multiple transcripts journal Biochem ... A, Cramer H, Sauer T, et al. title Palmitoylation of endothelin receptor A. Differential modulation ... endothelin A and B receptors. Evidence for G protein coupled receptor kinase specificity journal J. Biol ... journal author Bourgeois C, Robert B, Rebourcet R, et al. title Endothelin 1 and ETA receptor expression ... more details
PBB geneid 1910 Endothelin receptor type B , also known as ET sub B sub is a protein that in humans is encoded ... R title Cloning and chromosomal localization of a human endothelin ETA receptor journal Biochem. Biophys ... 291X 05 81399 3 url issn ref Function Endothelin receptor type B is a G protein coupled receptor which activates a phosphatidylinositol calcium second messenger system. Its ligand, endothelin , consists .... ref cite web title Entrez Gene EDNRB endothelin receptor type B url http www.ncbi.nlm.nih.gov ... transcription factor and endothelin signaling in Waardenburg syndrome and other pigmentary ... 2, is due to mutation in endothelin receptor type B gene. ref name pmid9556633 cite journal author ... M, Sekiya S, Kimura S title Novel mutations of the endothelin B receptor gene in patients with Hirschsprung ... mutation in the endothelin B receptor gene is associated with lethal white foal syndrome LWFS ... Endothelin receptor type B has been shown to Protein protein interaction interact with Caveolin 1 ..., Fujiyoshi Yoshinori, Doi Tomoko date April 2003 title Regulated interaction of endothelin B receptor ... laydate quote doi 10.1046 j.1432 1033.2003.03544.x ref See also Endothelin receptor References reflist ... title Endothelin Receptors ET sub B sub accessdate author authorlink coauthors date format work IUPHAR ... cloning of human endothelin ET receptors ETA and ETB. journal J. Cardiovasc. Pharmacol. volume ... K, et al. title Molecular cloning of human endothelin receptors and their expression in vascular endothelial ... of a non isopeptide selective human endothelin receptor. journal Biochem. Biophys. Res. Commun. volume ... author Cyr C, Huebner K, Druck T, Kris R title Cloning and chromosomal localization of a human endothelin ... Y, et al. title Cloning and sequence analysis of a cDNA encoding human non selective type of endothelin ... al. title Cloning and functional expression of human cDNA for the ETB endothelin receptor. journal Biochem ..., Hosoda K, Washington SS, et al. title A missense mutation of the endothelin B receptor gene in multigenic ... more details
PBB geneid 1889 Endothelin converting enzyme 1 , also known as ECE1 , is a enzyme which in humans is encoded by the ECE1 gene . ref name entrez cite web title Entrez Gene ECE1 endothelin converting enzyme ... endothelin converting enzyme ECE 1 journal FEBS Lett. volume 356 issue 2 3 pages 238 43 year 1994 month ... endothelin converting enzyme cDNA journal Biochem. Biophys. Res. Commun. volume 207 issue 2 pages 807 12 year 1995 month February pmid 7864876 doi 10.1006 bbrc.1995.1258 url ref Function Endothelin converting enzyme 1 is involved in the proteolytic processing of endothelin 1 endothelin 1 EDN1 , 2 endothelin 2 EDN2 , and 3 endothelin 3 EDN3 to biologically active peptides. ref name entrez References ... K, Moroi K, Inagaki N, et al. title Cloning and sequencing of a human endothelin converting enzyme in renal adenocarcinoma ACHN cells producing endothelin 2 journal Biochem. Biophys. Res. Commun. volume ... Schmidt M, Kr ger B, Jacob E, et al. title Molecular characterization of human and bovine endothelin .... title Cloning and functional expression of human endothelin converting enzyme cDNA journal Biochem ... the human endothelin converting enzyme ECE 1 journal J. Biol. Chem. volume 270 issue 50 pages 29794 ... K, et al. title Human endothelin converting enzyme gene ECE1 mapped to chromosomal region 1p36.1 ... promoters directing isoform specific expression of human endothelin converting enzyme 1 .... title Human endothelin converting enzyme ECE 1 three isoforms with distinct subcellular localizations ... cite journal author Kido T, Sawamura T, Masaki T title The processing pathway of endothelin 1 production ... A loss of function mutation in the endothelin converting enzyme 1 ECE 1 associated with Hirschsprung ..., Mele A, et al. title Proteolytic processing of big endothelin 3 by the kell blood group protein journal ... O, Lepailleur Enouf D, Egidy G, et al. title A fourth isoform of endothelin converting enzyme ECE ... for the specific cleavage at the Trp 21 Val 22 bond by soluble endothelin converting enzyme ... more details
EDN may refer to Encyclop die des Nuisances, a French magazine and publisher EDN magazine , an engineering magazine Endothelin , a chemical substance Eden Park railway station , a British Railway station with the station code EDN Earth Day Network, a coordinating body for Earth Day events Enterprise Municipal Airport Alabama FAA LID EDN Equal Device Network , a device interconnection network disambig ... more details
chembox Verifiedfields changed verifiedrevid 393276085 Reference ref name Sigma http www.sigmaaldrich.com catalog ProductDetail.do?N4 B150 SIGMA&N5 SEARCH CONCAT PNO BRAND KEY&F SPEC BQ 123 at Sigma Aldrich ref ImageFile BQ 123.png ImageSize 200px IUPACName 2 3 R ,6 R ,9 S ,12 R ,15 S 6 1 H indol 3 ylmethyl 9 2 methylpropyl 2,5,8,11,14 pentaoxo 12 propan 2 yl 1,4,7,10,13 pentazabicyclo 13.3.0 octadecan 3 yl acetic acid OtherNames Cyclo small D small trp small D small asp small L small pro small D small val small L small leu Section1 Chembox Identifiers CASNo Ref cascite correct ?? CASNo 136553 81 6 PubChem 443289 ChEMBL Ref ebicite changed EBI ChEMBL 1269102 IUPHAR ligand 1003 IUPHAR ligand 997 SMILES CC C C C H 1C O N C H C O N C H C O N2CCC C H 2C O N C H C O N1 C C C CC O O CC3 CNC4 CC CC C43 Section2 Chembox Properties C 31 H 42 N 6 O 7 Appearance Density MeltingPt BoilingPt Solubility Section3 Chembox Hazards MainHazards FlashPt Autoignition RPhrases SPhrases S22 S24 25 BQ 123 is a cyclic peptide consisting of five amino acid s. The amino acid sequence is small D small tryptamine small D small aspartic acid small L small proline small D small valine small L small leucine . BQ 123 is a selective ET sub A sub endothelin receptor antagonist . ref name Sigma As such, it is used as a biochemical tool in the study of endothelin receptor function. References reflist Category peptides Category Endothelin receptor antagonists biochem stub sr BQ 123 ... more details
ETB may refer to End Transmission Block character End Transmission Block , a control code in computing EITB Euskal Telebista , the Basque Country autonomous community Basque Country public broadcast service The Economics and Trade Branch of the United Nations Electric trolleybus An exchange code for the Ethiopian birr ETB, Empresa de Telecomunicaciones de Bogot , Colombia . The former European Transaction Bank, renamed to Xchanging on July 1, 2006 Engineering and Technology Board , United Kingdom Ethanol, 2 tert butoxy Endothelin receptor type B Earned Time Benefit disambig de ETB es ETB eo ETB fr ETB it ETB ja ETB sr ETB sv ETB ... more details
antagonist of endothelin 1 at the endothelin A ET A and endothelin B ET B receptors. Under normal conditions, endothelin 1 binding of ET A or ET B receptors causes pulmonary vasoconstriction ... and diuretics Category Endothelin receptor antagonists Category Orphan drugs Category Pyrimidines Category ... more details
first AA date 1 March 2008 title Phase I II Study of Atrasentan, an Endothelin A Receptor Antagonist ... AM last7 Lush first7 R last8 Padilla first8 B last9 Burton first9 M issue 5 ref It is an endothelin receptor antagonist selective for endothelin receptor type A subtype A ET sub A sub . While other drugs of this type sitaxentan , ambrisentan exploit the vasoconstrictive properties of endothelin and are mainly used for the treatment of pulmonary arterial hypertension , atrasentan blocks endothelin ... more details
Orphan date February 2009 PBB geneid 9427 Endothelin converting enzyme like 1 is a protein that in humans is encoded by the ECEL1 gene . ref name pmid9931490 cite journal author Valdenaire O, Richards JG, Faull RL, Schweizer A title XCE, a new member of the endothelin converting enzyme and neutral endopeptidase family, is preferentially expressed in the CNS journal Brain Res Mol Brain Res volume 64 issue 2 pages 211 21 year 1999 month Mar pmid 9931490 pmc doi 10.1016 S0169 328X 98 00321 0 ref ref name pmid11352565 cite journal author Rump A, Kasper G, Hayes C, Wen G, Starke H, Liehr T, Lehmann R, Lagemann D, Rosenthal A title Complex arrangement of genes within a 220 kb region of double duplicated DNA on human 2q37.1 journal Genomics volume 73 issue 1 pages 50 5 year 2001 month May pmid 11352565 pmc doi 10.1006 geno.2000.6504 ref ref name entrez cite web title Entrez Gene ECEL1 endothelin converting enzyme like 1 url http www.ncbi.nlm.nih.gov sites entrez?Db gene&Cmd ShowDetailView&TermToSearch 9427 accessdate ref The PBB Summary template is automatically maintained by Protein Box Bot. See Template PBB Controls to Stop updates. PBB Summary section title summary text This gene encodes a member of the neutral endopeptidase NEP related family. It is expressed specifically in the nervous system. The gene disruption in mouse embryonic stem cells results in neonatal lethality due to respiratory failure shortly after birth. Based on the specific expression of this gene and the phenotype of the gene deficiency in mouse embryos, it is suggested that the protein encoded by this gene play a critical role in the nervous regulation of the respiratory system. ref name entrez cite web title Entrez Gene ECEL1 endothelin converting enzyme like 1 url http www.ncbi.nlm.nih.gov sites entrez ... author Kawamoto T, Ohira M, Hamano S, et al. title High expression of the novel endothelin converting ... Endothelin converting enzyme like 1 ECEL1 is present both in the plasma membrane and in the endoplasmic ... more details
ref Mechanism of action Sitaxentan is a small molecule that Endothelin receptor antagonist blocks the action of endothelin ET on the endothelin A ET sub A sub receptor selectively by a factor of 6000 ... pmc 2111639 doi 10.1136 ard.2007.069609 ref It is a sulfonamide class endothelin receptor antagonist ... effects of endothelin receptor antagonists, and include liver enzyme abnormalities increased Alanine ... of Pulmonary Arterial Hypertension Benefits from Endothelin Receptor Subtype Selectivity? Clinical ... cgi content abstract 121 6 1860 Clinical Efficacy of Sitaxsentan, an Endothelin A Receptor ... Hypertension PAH rx Antihypertensives and diuretics Category Endothelin receptor antagonists ... more details
Drugbox Verifiedfields changed Watchedfields changed verifiedrevid 384091933 IUPAC name 2 S 2 4,6 Dimethoxypyrimidin 2 yl oxy 3 methoxy 3,3 di phenyl propanoic acid image Darusentan.png Clinical data tradename pregnancy category legal status routes of administration Oral Pharmacokinetic data bioavailability protein bound metabolism Liver Hepatic elimination half life 12.5 hours Identifiers CAS number Ref cascite correct ?? CAS number 171714 84 4 ATC prefix none ATC suffix ATC supplemental PubChem 177236 DrugBank Ref drugbankcite correct drugbank DrugBank UNII Ref fdacite changed FDA UNII 33JD57L6RW ChEMBL Ref ebicite changed EBI ChEMBL 23261 ChemSpiderID 154336 InChI 1 C22H22N2O6 c1 27 17 14 18 28 2 24 21 23 17 30 19 20 25 26 22 29 3,15 10 6 4 7 11 15 16 12 8 5 9 13 16 h4 14,19H,1 3H3, H,25,26 t19 m1 s1 InChIKey FEJVSJIALLTFRP LJQANCHMBS StdInChI 1S C22H22N2O6 c1 27 17 14 18 28 2 24 21 23 17 30 19 20 25 26 22 29 3,15 10 6 4 7 11 15 16 12 8 5 9 13 16 h4 14,19H,1 3H3, H,25,26 t19 m1 s1 StdInChIKey FEJVSJIALLTFRP LJQANCHMSA N Chemical data C 22 H 22 N 2 O 6 molecular weight 410.42 g mol smiles COC1 CC NC N1 O C H C O O C C2 CC CC C2 C3 CC CC C3 OC OC Darusentan LU 135252 HMR 4005 is a endothelin receptor antagonist . Gilead Colorado, a subsidiary of Gilead Sciences , ref http www.gilead.com pdf Gilead Sciences Company Overview.pdf Gilead Sciences ref under license from Abbott Laboratories , is developing darusentan for the potential treatment of uncontrolled hypertension . In June 2003, Myogen licensed the compound from Abbott for its application in the cancer field. ref https www.thomson pharma.com Thomson Pharma ref In May 2007, a randomized, double blind, active control, parallel assignment, safety and efficacy phase III trial was initiated in subjects who had completed the maintenance period of the DAR 312 study. References reflist pharma stub Category Endothelin receptor antagonists Category Pyrimidines Category Phenol ethers ... more details
Orphan date February 2009 refimprove date March 2009 Burantashi literally penis get up is a native Hausa people Hausa Fulani powder derived from the bark of the African tree Pausinystalia yohimbe . Burantashi is used as a food additive to barbecued meat suya in Nigeria , especially the Northern parts. The extracts contain the alkaloid yohimbine , an Alpha 2 adrenergic receptor alpha sub 2 sub receptor antagonist antagonist that has been used widely with variable success in erectile dysfunction , but the whole bark of the tree was not studied until recently. In one recent study, pure Burantashi powder obtained from a local suya vendor in Lagos, Nigeria was extracted aqueously and studied on the renal circulation of Sprague Dawley rat s. ref name Ajayi Ajayi AA, Newaz M, Hercule H, Saleh M, Bode CO, Oyekan AO. Endothelin like action of Pausinystalia yohimbe aqueous extract on vascular and renal regional hemodynamics in Sprague Dawley rats. Methods. Find. Expt. Clin. Pharmacol . 2003, 25 10 817 22. ref In the in vivo study, the extract code named CCD X , caused a rise in mean arterial pressure MAP , and a rise in renal medullary blood flow MBF . This systemic vasoconstrictor and renal medullary dilator action was attenuated separately by the endothelin A receptor blocker BMS 182874, ET B blocker BQ788, but blocked by their combination ref name Ajayi . Further, the nitric oxide inhibitor NO , L Nomega nitro Arginine Methyl Ester L NAME 10 mg kg totally inhibited the rise in medullary blood flow due to CCD X. In vitro studies in isolated perfused kidneys IPK and in pressurised microvessels PMV confirmed the in vivo effect to cause vasoconstriction , which was inhibited by endothelin A and B antagonists. The pressor dose response characteristic of CCD X on PMV was similar to that of endothelin 1 with EC sub 50 sub close to 100ng. It was concluded from these studies that, the aqueous extract exhibited a vasoconstrictor effect possibly alpha sub 2 sub mediated like yohimbin ... more details
Chemotaxis Receptor biochemistry receptors are expressed in the surface membrane with diverse dynamics, some of them have long term characteristics as they are determined genetically, others have short term moiety as their assembly is induced ad hoc in the presence of the ligand. The diverse feature of the chemotaxis receptors and ligands provides the possibility to select chemotactic responder cells with a simple chemotaxis assay . By chemotactic selection we can determine whether a still not characterized molecule acts via the long or the short term receptor pathway. Recent results proved that chemokines e.g. IL 8 , RANTES are working on long term chemotaxis receptors, while vasoactive peptides e.g. endothelin act more on the short term ones. Term chemotactic selection is also used to design a technique which separates eukaryotic or prokaryotic cells upon their chemotactic responsiveness to selector ligands. Image chtxsel.png center 300 px div style text align center border none Chemotactic selection div References cite journal author Kohidai L and Csaba G title Chemotaxis and chemotactic selection induced with cytokines IL 8, RANTES and TNF alpha in the unicellular Tetrahymena pyriformis. journal Cytokine year 1988 volume 10 pages 481 6 doi 10.1006 cyto.1997.0328 pmid 9702410 issue 7 External links http www.chemotaxis.usn.hu Chemotaxis Category Cell biology Category Perception Category Signal transduction es Selecci n quimiot ctica hu Kemotaktikus szelekci ... more details
PBB geneid 168667 BMP binding endothelial regulator is a protein that in humans is encoded by the BMPER gene . ref name entrez cite web title Entrez Gene BMP binding endothelial regulator url http www.ncbi.nlm.nih.gov sites entrez?db gene&cmd retrieve&list uids 168667 accessdate 2011 09 29T21 37 01.388 07 00 ref Transcription KLF15 is a strong and direct activator of BMPER expression which is inhibited by Sp1 transcription factor SP1 . BMPER is inhibited by endothelin 1 , which may be mediated by endothelin inhibition of KLF15. ref name pmid19767294 cite journal author Helbing T, Volkmar F, Goebel U, Heinke J, Diehl P, Pahl HL, Bode C, Patterson C, Moser M title Kr ppel like factor 15 regulates BMPER in endothelial cells journal Cardiovasc. Res. volume 85 issue 3 pages 551 9 year 2010 month February pmid 19767294 doi 10.1093 cvr cvp314 ref References reflist Further reading refbegin 2 Cite pmid 11853319 Cite pmid 12897139 Cite pmid 14766204 Cite pmid 18787191 Cite pmid 20869035 refend gene 7 stub ... more details
Autacoids or autocoids are biological factors which act like local hormones , have a brief duration, act near the site of synthesis, ref name Ahrens1996 cite book author Franklin A. Ahrens title Pharmacology url http books.google.com books?id JgtQHQY7VJQC&pg PA45 accessdate 25 November 2010 date 1 October 1996 publisher Wiley Blackwell isbn 9780683000856 pages 45 ref . The word autacoids comes from the Greek Autos self and Acos relief, i.e. drug . The effect of autacoids are mostly localized but large amounts can be produced and moved into circulation. Autocoids may thus have systemic effect by being transported via circulation. These regulating molecules are also metabolised locally. So the compounds are produced locally, they act locally and are metabolised locally. Autacoids can have many different biological actions including modulation of the activity of smooth muscles, glands, nerves, platelets and other tissues. Some autacoids for instance are primarily characterized by the effect they have upon smooth muscle . ref MeshName Autacoids ref With respect to vascular smooth muscle , there are both vasoconstrictor and vasodilator autacoids. Vasodilator autacoids can be released during periods of exercise. Their main effect is seen in the skin, allowing for heat loss. These are local hormones and therefore have a paracrine effect. Some notable autacoids are eicosanoid s, angiotensin , neurotensin , NO nitric oxide , kinin s, histamine , serotonin , endothelin s, palmitoylethanolamide , etc. References reflist Category Biomolecules biochem stub Autacoids ca Autacoide de Autakoid gl Autacoide it Autacoide ja pl Autakoidy sr Autakoid ... more details
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