vanderbilt medical center


  • Thomsen, M.; Lindsley, C.W.; Conn, P.J.; Wessell, J.; Fulton, B.S.; Wess, J.; Caine, S.B. ‘Evidence of contribution of both M1 and M4 receptors to muscarinic agonist attenuation of cocaine’s discriminative stimulus’ Psychopharmacology, submitted. (Grant: MH077606-01)
  • Wang, H-R.; Wu, M.; Yu, H.; Long, S.; Stevens, A.; Engers, D.W.; Sakin, H.; Daniels, J.S.; Dawson, E.S.; Hopkins, C.R.; Lindsley, C.W.; Li, M.; McManus, O.B. ‘Selective inhibition of the Kir2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR and pharmacological characterization of ML133’ ACS Chem. Bio. submitted (Grant: DA026212-01)
  • Reid, P.R.; Bridges, T.M.; Sheffler, D.A.; Cho, H.P.; Lewis, L.M.; Days, E.; Daniels, J.S.; Jones, C.K.; Niswender, C.M.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W.; Wood, M.R. ‘Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN Probe’ Bioorg. Med. Chem. Lett., 2011, (WEB ASAP doi:10.1016/j.bmcl.2010.12.015)  (Grant: MH077606-01)
  • Cheung, Y.Y.; Zamorano, R.; Blobaum, A.L.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W.; Niswender, C.M.; Hopkins, C.R. ‘Solution-phase parallel synthesis and SAR of homopiperazinyl  analogs as positive allosteric modulators of mGlu4’ ACS Combi. Sci. 2011, 13, 159-165. (Grant: NS053536-01)
  • Engers, D.W.; Field, J.R.; Le, U.; Zhou, S.; Bolinger, J.D.; Zamorano, R.; Blobaum, A.L.; Jones, C.K.; Jadhav, S.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W.; Niswender, C.M.; Hopkins, C.R. ‘Discovery, Synthesis, and SAR Development of a Series of N-(4-acetamido)-phenylpicolinamides as Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (mGlu4) with CNS Exposure in Rats’ J. Med. Chem. 2011, 54, 1106-1110.  (Grant: NS053536-01)
  • Gautam Bhave, Brian A. Chauder, Wen Liu, Eric S. Dawson, Rishin Kadakia, Thuy, T. Nguyen, L. Michelle Lewis, Jens Meiler, C. David Weaver, Lisa M. Satlin, Craig W. Lindsley, and Jerod S. Denton. “Development of a Selective Small-Molecule Inhibitor of Kir1.1, the Renal Outer Medullary Potassium Channel” Mol. Pharmacol. 2011, 79, 42-50. (Grant: NS057041-01)

Davis, A.A.; Heilman, C.J.; Brady, A.E.; Miller, N.R.; Fuerstenau-Sharpo, M.; Hanson, B.J.;  Lindsley, C.W.; Conn, P.J.; Lah, J.J.; Levey, A.I. ‘Differential effects of allosteric M1 muscarinic acetylcholine receptor agonists on receptor activation, arrestin 3 recruitment, and receptor downregulation’ ACS Chem. Neurosci. 2010, 1, 542-551. (Grant: MH077606-01)


Engers, D.W.; Gentry, P.R.; Williams, R.; Bolinger, D.L.; Weaver, C.D.; Menon, U.N.; Conn, P.J.  Lindsley, C.W.; Niswender, C.M.; Hopkins, C.R. ‘Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGluR4 PAMs identified by functional HTS’ Bioorg. Med. Chem. Lett. 2010, 20, 5175-5178. (Grant: NS053536-01)

  • Miller, N.R.; Daniels, R.N.; Conn, P.J.; Lindsley, C.W. ‘Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarnic acetylcholine subtype 1 (M1) antagonists’ Bioorg. Med. Chem. Lett. 2010, 20, 2174-2177. (Grant: MH077606-01)
  • Salovich, J.A.; Lindsley, C.W.; Hopkins, C.R. ‘Synthesis of 2,3-diarylsubstituted indazole utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence’ Tetrahedron Lett. 2010, 51, 3796-3799. (Grant: MH085683-01)
  • Bridges, T. M.; Kennedy, J. P.; Hopkins, C. R.; Conn, P. J.; Lindsley, C. W. ‘Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators’ Bioorg. Med. Chem. Lett. 2010, 20, 5617-5622 (Grant: MH077606-01)

Gautam Bhave, Daniel Lonergan, Brian A. Chauder and Jerod S. Denton.  “Small-Molecule Modulators of Inward Rectifier Potassium Channels: Recent Advances and Future Possibilities.”  Future Med. Chem. 2010, 2, 757-774. (Grant: NS057041-01)

  • Lindsley, C.W.Screening and Beyond: New Opportunities to Advance Neuroscience Discovery’ ACS Chem. Neurosci. 2010, 1, 84. (Grant: 1U54MH084659-01)
  • Digby, G.J.; Conn, P.J.; Lindsley, C.W. ‘Orthosteric- and allosteric-induced ligand-directed trafficking at G protein-coupled receptors’ Curr. Opin. Drug Disc. & Dev. 2010, 13, 577-586. (Grant: MH077606-01)
  • Bridges, T.M.; Kennedy, J.P.; Cho, H.P.; Conn, P.J.; Lindsley, C.W. ‘Chemical optimization of an M1, M3, M5 positive allosteric modulator (PAM) lead. Part II. Development of a highly selective M1 PAM’ Bioorg. Med. Chem. Lett. 2010, 20, 1972-1975. (Grant: MH077606-01)
  • Lebois, E.P.; Bridges, T.M.; Dawson, E.S.; Kennedy, J.P.; Xiang, Z.; Jadhav, S.B.; Yin, H.; Meiler, J.; Jones, C.K.; Conn, P.J.; Weaver, C.D.; Lindsley, C.W. ‘Discovery and development of novel subtype-selective M1 allosteric agonists for the investigation of M1 receptor function’ ACS Chemical Neurosci. 2010, 1, 104-121. (Grant: MH077606-01)
  • Bridges, T.M.; Kennedy, J.P.; Cho, H.P.; Conn, P.J.; Lindsley, C.W. ‘Chemical optimization of an M1, M3, M5 positive allosteric modulator (PAM) lead. Part I. Development of a highly selective M5 PAM’ Bioorg. Med. Chem. Lett. 2010, 20, 558-562. (Grant: MH077606-01)
  • Lewis, L.M.; Bhave, G.; Chauder, B.A.; Banerjee, S.; Lornsen, K.A.; Fallen, K.; Lindsley, C.W. Weaver, C.D.; Denton, J.S. ‘High-throughput screening reveals a small-molecule inhibitor of ROMK and Kir7.1’ Mol. Pharm. 2009, 76, 1094-1103. (Grant: NS057041-01)
  • Shirey, J.K.; Brady, A.E.; Jones, P.J.; Davis, A.A.; Bridges, T.M.; Jadhav, S.B.; Menon, U.; Christain, E.P.; Doherty, J.J.; Quirk, M.C.; Snyder, D.H.; Levey, A.I.; Watson, M.L.; Nicolle, M.M.; Lindsley, C.W.; Conn, P.J. ‘A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and can restore impairments of reversal learning’ J. Neurosci. 2009, 29, 14271-14286.  (Grant: MH077606-01)
  • Engers, D.W.; Niswender, C.M.; Weaver, C.D.; Jadhav, S.; Menon, U.; Conn, P.J.; Lindsley, C.W.; Hopkins, C.R. ‘Synthesis and Evaluation of a Series of Heterobiaryl Amides that are Centrally Penetrant Metabotropic Glutamate Receptor 4 (mGluR4) Positive Allosteric Modulators (PAMs)’ J. Med. Chem. 2009, 52, 4115-4118. (Grant: NS053536-01)
  • Bridges, T.M.; Marlo, J.E.; Niswender, C.M.; Jones, J.K.; Jadhav, S.B.; Gentry, P.R.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W. ‘Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N benzyl isatins’ J. Med. Chem. 2009, 52, 3445-3448. (Grant: MH077606-01)
  • Kennedy, J.P.; Bridges, T.M.; Gentry, P.R.; Brogan, J.T.; Brady, A.E.; Shirey, J.K.; Jones, C.K.; Conn, P.J.; Lindsley,C.W. ‘Synthesis and structure-activity-relationships of allosteric potentiators of the M4 muscarinic acetylcholine receptor’ ChemMedChem. 2009, 4, 1600-1607. (Grant:MH077607-01)
  • Marlo, J.E.; Niswender, C.M.; Luo, Q.; Brady, A.E.; Shirey, J.K.; Rodriguez, A.L.; Bridges, T.M.; Williams, R.; Days, E.; Nalywajko, N.T.; Austin, C.; Williams, M.; Xiang, Y.; Orton, D.; Brown, H.A.; Kim, K.; Lindsley, C.W.; Weaver, C.D.; Conn, P.J. ‘Identification and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity’ Mol. Pharm. 2009, 75(3), 577-588.  (Grant: MH077606-01)
  • Sheffler, D.J; Williams, R.; Bridges, T.M.; Lewis, L.M.; Xiang, Z.; Zheng, F.; Kane, A.S.; Byum, N.E.;   Jadhav, S.; Mock, M.M.; Zheng, F.; Lewis, L.M.; Jones, C.K.; Niswender, C.M.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W.; Conn, P.J. ‘Novel Selective Muscarinic Acetylcholine Receptor Subtype 1 (M1 mAChR) Antagonist Reduces Seizures without Impairing Hippocampal-Dependent Learning’ Mol. Pharmacol. 2009, 76, 356-368. (Grant: MH077606-01)
3. Delpire, E.; Days, E.; Mi, D.; Lewis, M.; Lindsley, C.W.; Weaver, C.D. Small molecule screen identifies novel inhibitors of the neuronal K-Cl cotransporter KCC2’ Proc. Natl. Acad Sci. USA, 2009, 106, 5383-5388. (Grant: NS053658-01)

Aldrich, L.; LeBois, E.P.; Lewis, L.M.; Nalywajko, N.T.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W. ‘MAOS protocols for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyradazines’ Tetrahedron Lett. 2009, 50, 212-216. (Grant: MH077606-01)


Lewis, L.M.; Sheffler, D.; Williams, R.; Bridges, T.A.; Kennedy, J.P.; Brogan, J.T.; Mulder, M.J.; Williams, L.; Nalywajko, N.T.; Niswender, C.; Weaver, C.D.; Conn, P.J.; Lindsley, C.W. 'Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists' Bioorg. Med. Chem. Lett., 2009, 18, 885. (Grant: MH077606-01)