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Page 1
Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063.
Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EL, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS. Kharade SV, et al. Among authors: blobaum al. J Pharmacol Exp Ther. 2019 Sep;370(3):350-359. doi: 10.1124/jpet.119.257204. Epub 2019 Jun 14. J Pharmacol Exp Ther. 2019. PMID: 31201216 Free PMC article.
Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.
Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS. Kharade SV, et al. Among authors: blobaum al. Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12. Mol Pharmacol. 2018. PMID: 29895592 Free PMC article.
ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels.
Swale DR, Kurata H, Kharade SV, Sheehan J, Raphemot R, Voigtritter KR, Figueroa EE, Meiler J, Blobaum AL, Lindsley CW, Hopkins CR, Denton JS. Swale DR, et al. Among authors: blobaum al. ACS Chem Neurosci. 2016 Jul 20;7(7):1013-23. doi: 10.1021/acschemneuro.6b00111. Epub 2016 May 24. ACS Chem Neurosci. 2016. PMID: 27184474 Free PMC article.
The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Jones CK, Bubser M, Thompson AD, Dickerson JW, Turle-Lorenzo N, Amalric M, Blobaum AL, Bridges TM, Morrison RD, Jadhav S, Engers DW, Italiano K, Bode J, Daniels JS, Lindsley CW, Hopkins CR, Conn PJ, Niswender CM. Jones CK, et al. Among authors: blobaum al. J Pharmacol Exp Ther. 2012 Feb;340(2):404-21. doi: 10.1124/jpet.111.187443. Epub 2011 Nov 16. J Pharmacol Exp Ther. 2012. PMID: 22088953 Free PMC article.
Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.
Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Lindsley CW. Rook JM, et al. Among authors: blobaum al. ACS Chem Neurosci. 2017 Apr 19;8(4):866-883. doi: 10.1021/acschemneuro.6b00429. Epub 2017 Jan 10. ACS Chem Neurosci. 2017. PMID: 28001356 Free PMC article.
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.
Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW. Bertron JL, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2175-2179. doi: 10.1016/j.bmcl.2018.05.009. Epub 2018 May 5. Bioorg Med Chem Lett. 2018. PMID: 29754948 Free PMC article.
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4).
Bollinger SR, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR. Bollinger SR, et al. Among authors: blobaum al. J Med Chem. 2019 Jan 10;62(1):342-358. doi: 10.1021/acs.jmedchem.8b00994. Epub 2018 Oct 10. J Med Chem. 2019. PMID: 30247901
Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model.
Kent CN, Fulton MG, Stillwell KJ, Dickerson JW, Loch MT, Rodriguez AL, Blobaum AL, Boutaud O, Rook JL, Niswender CM, Conn PJ, Lindsley CW. Kent CN, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2021 Apr 1;37:127838. doi: 10.1016/j.bmcl.2021.127838. Epub 2021 Feb 5. Bioorg Med Chem Lett. 2021. PMID: 33556572
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.
Spearing PK, Cho HP, Luscombe VB, Blobaum AL, Boutaud O, Engers DW, Rodriguez AL, Niswender CM, Jeffrey Conn P, Lindsley CW, Bender AM. Spearing PK, et al. Among authors: blobaum al. Bioorg Med Chem Lett. 2021 Sep 1;47:128193. doi: 10.1016/j.bmcl.2021.128193. Epub 2021 Jun 9. Bioorg Med Chem Lett. 2021. PMID: 34118412 Free PMC article.
103 results