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Discovery, synthesis and biological characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators.
Sharma S, Lesiak L, Aretz CD, Du Y, Kumar S, Gautam N, Alnouti Y, Dhuria NV, Chhonker YS, Weaver CD, Hopkins CR. Sharma S, et al. Among authors: hopkins cr. RSC Med Chem. 2021 Jun 21;12(8):1366-1373. doi: 10.1039/d1md00129a. eCollection 2021 Aug 18. RSC Med Chem. 2021. PMID: 34458739 Free PMC article.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Engers DW, et al. Among authors: hopkins cr. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. Epub 2010 Jul 8. Bioorg Med Chem Lett. 2010. PMID: 20667732 Free PMC article.
Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.
Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Engers DW, et al. Among authors: hopkins cr. J Med Chem. 2011 Feb 24;54(4):1106-10. doi: 10.1021/jm101271s. Epub 2011 Jan 19. J Med Chem. 2011. PMID: 21247167 Free PMC article.
Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
Miller M, Shi J, Zhu Y, Kustov M, Tian JB, Stevens A, Wu M, Xu J, Long S, Yang P, Zholos AV, Salovich JM, Weaver CD, Hopkins CR, Lindsley CW, McManus O, Li M, Zhu MX. Miller M, et al. Among authors: hopkins cr. J Biol Chem. 2011 Sep 23;286(38):33436-46. doi: 10.1074/jbc.M111.274167. Epub 2011 Jul 27. J Biol Chem. 2011. PMID: 21795696 Free PMC article.
Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.
Jones CK, Engers DW, Thompson AD, Field JR, Blobaum AL, Lindsley SR, Zhou Y, Gogliotti RD, Jadhav S, Zamorano R, Bogenpohl J, Smith Y, Morrison R, Daniels JS, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Jones CK, et al. Among authors: hopkins cr. J Med Chem. 2011 Nov 10;54(21):7639-47. doi: 10.1021/jm200956q. Epub 2011 Oct 19. J Med Chem. 2011. PMID: 21966889 Free PMC article.
Discovery, characterization, and structure-activity relationships of an inhibitor of inward rectifier potassium (Kir) channels with preference for Kir2.3, Kir3.x, and Kir7.1.
Raphemot R, Lonergan DF, Nguyen TT, Utley T, Lewis LM, Kadakia R, Weaver CD, Gogliotti R, Hopkins C, Lindsley CW, Denton JS. Raphemot R, et al. Front Pharmacol. 2011 Nov 30;2:75. doi: 10.3389/fphar.2011.00075. eCollection 2011. Front Pharmacol. 2011. PMID: 22275899 Free PMC article.
The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.
Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, Dawson ES, Li M, McManus O, Jones CK, Daniels JS, Hopkins CR, Xie XS, Conn PJ, Weaver CD, Lindsley CW. Xiang Z, et al. Among authors: hopkins cr. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742. doi: 10.1021/cn200090z. ACS Chem Neurosci. 2011. PMID: 22368764 Free PMC article.
244 results