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An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN. Thorneloe KS, et al. Among authors: davenport ea. Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276. Sci Transl Med. 2012. PMID: 23136043
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore.
Washburn DG, Holt DA, Dodson J, McAtee JJ, Terrell LR, Barton L, Manns S, Waszkiewicz A, Pritchard C, Gillie DJ, Morrow DM, Davenport EA, Lozinskaya IM, Guss J, Basilla JB, Negron LK, Klein M, Willette RN, Fries RE, Jensen TC, Xu X, Schnackenberg CG, Marino JP Jr. Washburn DG, et al. Among authors: davenport ea. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4979-84. doi: 10.1016/j.bmcl.2013.06.047. Epub 2013 Jun 26. Bioorg Med Chem Lett. 2013. PMID: 23886683
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Morales-Ramos AI, Mecom JS, Kiesow TJ, Graybill TL, Brown GD, Aiyar NV, Davenport EA, Kallal LA, Knapp-Reed BA, Li P, Londregan AT, Morrow DM, Senadhi S, Thalji RK, Zhao S, Burns-Kurtis CL, Marino JP Jr. Morales-Ramos AI, et al. Among authors: davenport ea. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6222-6. doi: 10.1016/j.bmcl.2008.09.102. Epub 2008 Oct 2. Bioorg Med Chem Lett. 2008. PMID: 18926700
Evidence for allosteric interactions of antagonist binding to the smoothened receptor.
Rominger CM, Bee WL, Copeland RA, Davenport EA, Gilmartin A, Gontarek R, Hornberger KR, Kallal LA, Lai Z, Lawrie K, Lu Q, McMillan L, Truong M, Tummino PJ, Turunen B, Will M, Zuercher WJ, Rominger DH. Rominger CM, et al. Among authors: davenport ea. J Pharmacol Exp Ther. 2009 Jun;329(3):995-1005. doi: 10.1124/jpet.109.152090. Epub 2009 Mar 20. J Pharmacol Exp Ther. 2009. PMID: 19304771
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.
Thalji RK, Aiyar N, Davenport EA, Erhardt JA, Kallal LA, Morrow DM, Senadhi S, Burns-Kurtis CL, Marino JP Jr. Thalji RK, et al. Among authors: davenport ea. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4104-7. doi: 10.1016/j.bmcl.2010.05.072. Epub 2010 Jun 9. Bioorg Med Chem Lett. 2010. PMID: 20542694
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