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Antileukotriene

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indomethacin (5 mg/kg) . Hyperforin turned out to be a novel type of 5-lipoxygenase inhibitor with high effectivity in vivo and suppressed oxidative bursts in polymorphonuclear cells at 1.8 μmol/L in vitro . Inhibition of IFN-γ production, strong downregulation of CXCR3 expression on activated T cells, and downregulation of matrix metalloproteinase 9 expression caused Cabrelle et al. to test the effectivity of hyperforin in a rat model of experimental allergic encephalomyelitis (EAE). Hyperforin attenuated the symptoms significantly, and the authors discussed hyperforin as a putative therapeutic molecule for the treatment of autoimmune inflammatory diseases sustained by Th1 cells.
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effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the airways of asthmatic patients. Sulfido-peptide leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, can be measured in a number of biological fluids including bronchoalveolar lavage fluid (BALF) from asthmatic patients.
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cyclooxygenase-1 and 5-lipoxygenase . Moreover, this species attenuated the expression of iNOS in periodontal tissue, which may contribute to the attenuation of the formation of nitrotyrosine, an indication of nitrosative stress . In this context, a combination of several active constituents of Hypericum species is the carrier of their anti-inflammatory activity.
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These researches are according to an investigation of the effect of H. perforatum on the NF-κB inflammation factor, conducted by Bork et al. (1999), in which hyperforin provided a potent inhibition of TNFα-induced activation of NF-κB . Another important activity for hyperforin is a dual inhibitor of
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Anti-inflammatory mechanisms of hyperforin have been described as inhibition of cyclooxygenase-1 (but not COX-2) and 5-lipoxygenase at low concentrations of 0.3 μmol/L and 1.2 μmol/L, respectively , and of PGE2 production in vitro and in vivo with superior efficiency (ED50 = 1 mg/kg) compared to
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Zileuton is a specific inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB4, LTC4, LTD4, and LTE4) formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. Leukotrienes are substances that induce numerous biological
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Jawien, J.; Gajda, M.; Rudling, M.; Mateuszuk, L.; Olszanecki, R.; Guzik, T. J.; Cichocki, T.; Chlopicki, S.; Korbut, R. (March 2006). "Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice".
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Singh, Rakesh Kumar; Tandon, Ruchi; Dastidar, Sunanda Ghosh; Ray, Abhijit (2013). "A review on leukotrienes and their receptors with reference to asthma".
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de Melo MS, Quintans Jde S, Araújo AA, Duarte MC, Bonjardim LR, Nogueira PC, Moraes VR, de Araújo-Júnior JX, Ribeiro EA, Quintans-Júnior LJ (2014).
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These modifiers have been shown to improve asthma symptoms, reduce asthma exacerbations and limit markers of inflammation such as
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Some chemicals found in trace amounts in food, and some dietary supplements, also have been shown to inhibit 5-LOX, such as
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Antileukotrienes such as montelukast may be used in patients with asthma associated with allergic rhinitis.
138:) and consequently opposes the function of these inflammatory mediators; leukotrienes are produced by the 2235: 127: 347:
Scott JP, Peters-Golden M (September 2013). "Antileukotriene agents for the treatment of lung disease".
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Al-Ahmad, Mona; Hassab, Mohammed; Al Ansari, Ali (2020-12-21). "Allergic and Non-allergic Rhinitis".
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will inhibit the synthetic pathway of leukotriene metabolism; drugs such as
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fluid. This demonstrates that they have anti-inflammatory properties.
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Medication class that inhibits leukotriene synthesis and/or activity.
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There are two main approaches to block the actions of leukotrienes.
195:, can be used to treat these diseases. They are less effective than 2624: 2588: 2502: 2435: 2326: 2283: 1990: 1779: 1379: 1270: 905: 264: 249: 186: 41: 2561: 2364: 2218: 1567: 1092: 884: 621:"Topical application of St. John's wort (Hypericum perforatum)" 558: 292: 230: 159: 1562: 1096: 554: 552: 550: 437:. Cham: Springer International Publishing. pp. 241–252. 199:
for treating asthma, but more effective for treating certain
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Tooltip Arachidonate 5-lipoxygenase-activating protein
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Leukotriene modifier; Leukotriene receptor antagonist
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Antagonism of cysteinyl-leukotriene type 1 receptors
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Examples of 5-LOX inhibitors include drugs, such as
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Fluticasone furoate/umeclidinium bromide/vilanterol
619:Wölfle U, Seelinger G, Schempp CM (February 2014). 291:block the actions of cysteinyl leukotrienes at the 699:Frieri M (2015). "Mast Cell Activation Syndrome". 346: 1840: 1697: 342: 340: 338: 2718: 2604: 2572: 2451: 477: 475: 473: 2540: 1683: 1493:Beclometasone/formoterol/glycopyrronium bromide 790: 788: 786: 784: 782: 692: 795:Bishayee K, Khuda-Bukhsh AR (September 2013). 375: 335: 1636: 1533:Indacaterol/glycopyrronium bromide/mometasone 864: 470: 1503:Budesonide/glycopyrronium bromide/formoterol 779: 295:receptor on target cells such as bronchial 2673:5-HPETE (arachidonic acid 5-hydroperoxide) 1643: 1629: 871: 857: 745:European Journal of Clinical Investigation 735: 535:. 3.6. University of Alberta. 30 June 2013 490:United States Food and Drug Administration 173:Leukotriene receptor antagonists, such as 841:at the U.S. National Library of Medicine 812: 636: 586: 576: 2187:Tooltip Cysteinyl leukotriene receptor E 2124:Tooltip Cysteinyl leukotriene receptor 2 1951:Tooltip Cysteinyl leukotriene receptor 1 663: 215:Inhibition of the 5-lipoxygenase pathway 118:, is a medication which functions as a 2719: 1934:Tooltip Cysteinyl leukotriene receptor 1372:Arachidonate 5-lipoxygenase inhibitors 801:Acta Biochim. Biophys. Sin. (Shanghai) 698: 185:, and 5-lipoxygenase inhibitors, like 1624: 852: 657: 221:Arachidonate 5-lipoxygenase inhibitor 2522:Tooltip Leukotriene B4 ω-hydroxylase 2418:Tooltip Arachidonate 15-lipoxygenase 2380:Tooltip Arachidonate 12-lipoxygenase 1568:Theophylline/ephedrine/phenobarbital 2241:Tooltip Arachidonate 5-lipoxygenase 435:Textbook of Clinical Otolaryngology 310:counts in the peripheral blood and 13: 1563:Theophylline/ephedrine/hydroxyzine 1528:Indacaterol/glycopyrronium bromide 565:Evid Based Complement Alternat Med 14: 2738: 2653:γ-Linolenic acid (gamolenic acid) 2307:Meclofenamic acid (meclofenamate) 1848:Tooltip Leukotriene B4 receptor 2 1705:Tooltip Leukotriene B4 receptor 1 1553:Salbutamol (albuterol)/budesonide 1523:Glycopyrronium bromide/formoterol 1518:Fluticasone propionate/salmeterol 832: 664:Fanta CH (March 2009). "Asthma". 235:5-lipoxygenase activating protein 2612:Tooltip Leukotriene D4 hydrolase 2581:Tooltip Leukotriene C4 hydrolase 2460:Tooltip Leukotriene A4 hydrolase 1390:Thromboxane receptor antagonists 757:10.1111/j.1365-2362.2006.01606.x 2705:Prostanoid signaling modulators 2549:Tooltip Leukotriene C4 synthase 1688:Tooltip Leukotriene B4 receptor 1573:Umeclidinium bromide/vilanterol 136:cysteinyl leukotriene receptors 116:leukotriene receptor antagonist 1543:Ipratropium bromide/salbutamol 1513:Fluticasone furoate/vilanterol 1128:Orciprenaline (metaproterenol) 225:Drugs that inhibit the enzyme 1: 2698:Receptor/signaling modulators 1483:Aclidinium bromide/formoterol 971:Levosalbutamol (levalbuterol) 349:Am. J. Respir. Crit. Care Med 329: 206: 85: • Receptors: 1118:Isoprenaline (isoproterenol) 443:10.1007/978-3-030-54088-3_22 396:10.3109/02770903.2013.823447 7: 1093:+theophylline/phenobarbital 881:obstructive airway diseases 317: 128:arachidonate 5-lipoxygenase 75: • Enzymes: 10: 2743: 483:"Zyflo (Zileuton tablets)" 361:10.1164/rccm.201301-0023PP 218: 152:microvascular permeability 2689: 2637: 2602: 2570: 2538: 2511: 2449: 2411: 2373: 2234: 2217: 2177: 2114: 1941: 1927: 1838: 1695: 1681: 1664: 1581: 1475: 1439: 1411: 1388: 1370: 1342: 1332: 1269: 1246: 1198: 1145: 1077: 1035: 989: 913: 900: 713:10.1007/s12016-015-8487-6 533:Human Metabolome Database 97: 92: 68: 50: 40: 35: 26: 21: 1488:Beclometasone/formoterol 1097:theophylline/hydroxyzine 1037:Ultra-long-acting β 843:Medical Subject Headings 701:Clin Rev Allergy Immunol 528:Hyperforin (HMDB0030463) 2727:Leukotriene antagonists 2658:Dihomo-γ-linolenic acid 1344:Leukotriene antagonists 839:Leukotriene+antagonists 1558:Theophylline/ephedrine 1538:Indacaterol/mometasone 1299:Choline theophyllinate 1218:Glycopyrronium bromide 1180:Fluticasone propionate 967:Salbutamol (albuterol) 638:10.1055/s-0033-1351019 312:bronchoalveolar lavage 2594:Serine-borate complex 1760:CGS-23131 (LY-223982) 1548:Mometasone/formoterol 1498:Budesonide/formoterol 1248:Mast cell stabilizers 1205:muscarinic antagonist 678:10.1056/NEJMra0804579 142:and serve to promote 2530:17-Octadecynoic acid 2300:Hypericum perforatum 1476:Combination products 1238:Umeclidinium bromide 246:meclofenamate sodium 192:Hypericum perforatum 112:leukotriene modifier 2625:Ubenimex (bestatin) 2503:Ubenimex (bestatin) 1223:Ipratropium bromide 915:Short-acting β 814:10.1093/abbs/gmt064 578:10.1155/2014/960258 301:receptor antagonism 144:bronchoconstriction 132:receptor antagonist 63:Receptor antagonism 52:Mechanism of action 2393:3-Methoxytropolone 2317:N-Stearoyldopamine 1608:Never to phase III 1233:Tiotropium bromide 1228:Oxitropium bromide 1213:Aclidinium bromide 991:Long-acting β 61: • 56: • 2714: 2713: 2633: 2632: 2302:(St. John's Wort) 2228: 2213: 2212: 2209: 2208: 1923: 1922: 1675: 1618: 1617: 1435: 1434: 1141: 1140: 452:978-3-030-54087-6 384:Journal of Asthma 130:) or leukotriene 104: 103: 70:Biological target 58:Enzyme inhibition 36:Class identifiers 2734: 2668:Arachidonic acid 2613: 2609: 2582: 2578: 2550: 2546: 2523: 2519: 2461: 2457: 2419: 2415: 2381: 2377: 2341: 2337: 2242: 2238: 2232: 2231: 2222: 2188: 2184: 2125: 2121: 1952: 1948: 1939: 1938: 1935: 1931: 1849: 1845: 1706: 1702: 1693: 1692: 1689: 1685: 1679: 1678: 1669: 1645: 1638: 1631: 1622: 1621: 1340: 1339: 1200:Anticholinergics 911: 910: 873: 866: 859: 850: 849: 827: 826: 816: 792: 777: 776: 739: 733: 732: 696: 690: 689: 661: 655: 654: 640: 616: 605: 604: 590: 580: 556: 545: 544: 542: 540: 519: 506: 505: 499: 497: 487: 479: 468: 467: 430: 424: 423: 379: 373: 372: 344: 124:enzyme inhibitor 110:, also known as 83: 22:Antileukotrienes 19: 18: 2742: 2741: 2737: 2736: 2735: 2733: 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2694: 2690: 2687: 2686: 2684: 2683: 2679: 2675: 2670: 2665: 2663:Diacylglycerol 2660: 2655: 2650: 2641: 2639: 2635: 2634: 2631: 2630: 2628: 2627: 2622: 2616: 2614: 2606: 2600: 2599: 2597: 2596: 2591: 2585: 2583: 2574: 2568: 2567: 2565: 2564: 2559: 2553: 2551: 2542: 2536: 2535: 2533: 2532: 2526: 2524: 2515: 2509: 2508: 2506: 2505: 2500: 2495: 2490: 2485: 2480: 2475: 2470: 2464: 2462: 2453: 2447: 2446: 2444: 2443: 2438: 2433: 2428: 2422: 2420: 2409: 2408: 2406: 2405: 2400: 2395: 2390: 2384: 2382: 2371: 2370: 2368: 2367: 2362: 2357: 2352: 2347: 2330: 2329: 2324: 2319: 2314: 2309: 2304: 2296: 2291: 2286: 2281: 2276: 2271: 2266: 2261: 2256: 2251: 2245: 2243: 2229: 2215: 2214: 2211: 2210: 2207: 2206: 2204: 2203: 2199: 2191: 2189: 2181: 2175: 2174: 2172: 2171: 2166: 2157: 2156: 2152: 2148: 2144: 2140: 2136: 2128: 2126: 2118: 2112: 2111: 2109: 2108: 2103: 2098: 2093: 2088: 2083: 2078: 2073: 2068: 2063: 2058: 2053: 2048: 2043: 2038: 2033: 2028: 2023: 2018: 2013: 2008: 2003: 1998: 1993: 1984: 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2739: 2728: 2725: 2724: 2722: 2707: 2706: 2702: 2700: 2699: 2695: 2692: 2691: 2688: 2682: 2678:Leukotriene A 2676: 2674: 2671: 2669: 2666: 2664: 2661: 2659: 2656: 2654: 2651: 2649: 2648:Linoleic acid 2646: 2643: 2642: 2640: 2636: 2626: 2623: 2621: 2618: 2617: 2615: 2610: 2601: 2595: 2592: 2590: 2587: 2586: 2584: 2579: 2569: 2563: 2560: 2558: 2555: 2554: 2552: 2547: 2537: 2531: 2528: 2527: 2525: 2520: 2510: 2504: 2501: 2499: 2496: 2494: 2491: 2489: 2486: 2484: 2481: 2479: 2476: 2474: 2471: 2469: 2466: 2465: 2463: 2458: 2448: 2442: 2439: 2437: 2434: 2432: 2429: 2427: 2424: 2423: 2421: 2416: 2410: 2404: 2401: 2399: 2396: 2394: 2391: 2389: 2386: 2385: 2383: 2378: 2372: 2366: 2363: 2361: 2358: 2356: 2353: 2351: 2348: 2346: 2343: 2338: 2332: 2331: 2328: 2325: 2323: 2320: 2318: 2315: 2313: 2310: 2308: 2305: 2303: 2301: 2297: 2295: 2292: 2290: 2287: 2285: 2282: 2280: 2277: 2275: 2272: 2270: 2267: 2265: 2262: 2260: 2257: 2255: 2252: 2250: 2247: 2246: 2244: 2239: 2233: 2230: 2226: 2220: 2216: 2202: 2198:Leukotriene E 2196: 2193: 2192: 2190: 2185: 2176: 2170: 2167: 2165: 2162: 2159: 2158: 2155: 2151:Leukotriene E 2149: 2147: 2143:Leukotriene D 2141: 2139: 2135:Leukotriene C 2133: 2130: 2129: 2127: 2122: 2113: 2107: 2104: 2102: 2099: 2097: 2094: 2092: 2089: 2087: 2084: 2082: 2079: 2077: 2074: 2072: 2069: 2067: 2064: 2062: 2059: 2057: 2054: 2052: 2049: 2047: 2044: 2042: 2039: 2037: 2034: 2032: 2029: 2027: 2024: 2022: 2019: 2017: 2014: 2012: 2009: 2007: 2004: 2002: 1999: 1997: 1994: 1992: 1989: 1986: 1985: 1982: 1978:Leukotriene E 1976: 1974: 1970:Leukotriene D 1968: 1966: 1962:Leukotriene C 1960: 1957: 1956: 1954: 1949: 1940: 1937: 1932: 1926: 1916: 1913: 1911: 1908: 1906: 1903: 1900: 1899: 1896: 1892:Leukotriene B 1890: 1888: 1882: 1880: 1877: 1875: 1872: 1870: 1867: 1865: 1862: 1860: 1857: 1854: 1853: 1851: 1846: 1837: 1831: 1828: 1826: 1823: 1821: 1818: 1816: 1813: 1811: 1808: 1806: 1803: 1801: 1798: 1796: 1793: 1791: 1788: 1786: 1783: 1781: 1778: 1776: 1773: 1771: 1768: 1766: 1763: 1761: 1758: 1756: 1753: 1751: 1745: 1742: 1741: 1738: 1735: 1733: 1729:Leukotriene B 1727: 1725: 1719: 1717: 1714: 1711: 1710: 1708: 1703: 1694: 1691: 1686: 1680: 1677: 1673: 1667: 1663: 1659: 1656: 1653: 1646: 1641: 1639: 1634: 1632: 1627: 1626: 1623: 1607: 1605: 1602: 1601: 1599: 1596: 1593: 1590: 1588: 1585: 1584: 1580: 1574: 1571: 1569: 1566: 1564: 1561: 1559: 1556: 1554: 1551: 1549: 1546: 1544: 1541: 1539: 1536: 1534: 1531: 1529: 1526: 1524: 1521: 1519: 1516: 1514: 1511: 1509: 1506: 1504: 1501: 1499: 1496: 1494: 1491: 1489: 1486: 1484: 1481: 1480: 1478: 1474: 1468: 1465: 1463: 1460: 1458: 1455: 1453: 1450: 1448: 1445: 1444: 1442: 1438: 1428: 1425: 1423: 1420: 1419: 1417: 1415: 1412:Non-xanthine 1410: 1404: 1401: 1399: 1396: 1395: 1393: 1391: 1387: 1381: 1378: 1377: 1375: 1373: 1369: 1363: 1360: 1358: 1355: 1353: 1350: 1349: 1347: 1345: 1341: 1338: 1335: 1331: 1325: 1322: 1320: 1319:Proxyphylline 1317: 1315: 1314:Etamiphylline 1312: 1310: 1307: 1305: 1302: 1300: 1297: 1295: 1292: 1290: 1289:Aminophylline 1287: 1285: 1282: 1280: 1277: 1276: 1274: 1272: 1268: 1262: 1259: 1257: 1254: 1253: 1251: 1249: 1245: 1239: 1236: 1234: 1231: 1229: 1226: 1224: 1221: 1219: 1216: 1214: 1211: 1210: 1208: 1206: 1201: 1197: 1191: 1190:Triamcinolone 1188: 1186: 1183: 1181: 1178: 1176: 1173: 1171: 1168: 1166: 1163: 1161: 1160:Betamethasone 1158: 1156: 1155:Beclometasone 1153: 1152: 1150: 1148: 1144: 1134: 1131: 1129: 1126: 1124: 1121: 1119: 1116: 1114: 1113:Hexoprenaline 1111: 1109: 1106: 1104: 1101: 1098: 1094: 1090: 1089:+theophylline 1086: 1083: 1082: 1080: 1076: 1070: 1067: 1065: 1062: 1060: 1057: 1055: 1052: 1050: 1047: 1046: 1044: 1042: 1034: 1028: 1025: 1023: 1020: 1018: 1014: 1011: 1009: 1006: 1004: 1001: 1000: 998: 996: 988: 982: 979: 977: 974: 972: 968: 965: 963: 960: 958: 955: 953: 950: 948: 945: 943: 940: 938: 935: 933: 930: 928: 925: 924: 922: 920: 912: 909: 907: 903: 899: 894: 890: 886: 882: 874: 869: 867: 862: 860: 855: 854: 851: 844: 840: 837: 836: 824: 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2483:Fosinoprilat 2333: 2299: 2269:Caffeic acid 2194: 2161:Antagonists: 2160: 2131: 1988:Antagonists: 1987: 1958: 1902:Antagonists: 1901: 1855: 1744:Antagonists: 1743: 1712: 1452:Ensifentrine 1324:Theophylline 1309:Enprofylline 1284:Ambuphylline 1256:Cromoglicate 1133:Racephedrine 1017:Arformoterol 804: 800: 748: 744: 737: 704: 700: 694: 669: 666:N Engl J Med 665: 659: 650: 628: 624: 600: 568: 564: 537:. 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Index

Drug class
Synonyms
Mechanism of action
Enzyme inhibition
Receptor antagonism
Biological target
5-LOX
FLAP
CysLTRs
In Wikidata
leukotriene
enzyme inhibitor
arachidonate 5-lipoxygenase
receptor antagonist
cysteinyl leukotriene receptors
immune system
bronchoconstriction
inflammation
microvascular permeability
mucus
asthma
COPD
montelukast
zafirlukast
pranlukast
zileuton
Hypericum perforatum
corticosteroids
mast cell
Arachidonate 5-lipoxygenase inhibitor

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