Synthesis and SAR of an mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaff...

Por Sharma, Sameer, Rodriguez, Alice L., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2008

3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators

Por Lowe, Edward W., Ferrebee, Alysia, Rodriguez, Alice L., Conn, P. Jeffrey, Meiler, Jens
Publicado em 2010

Structure-Activity Relationships in a Novel Series of 7-Substituted-Aryl Quinolines and 5-Substituted-Aryl Benzothiazoles at the Metabotropic Glutamate Receptor Subtype 5

Por Zhang, Peng, Zou, Mu-Fa, Rodriguez, Alice L., Conn, P. Jeffrey, Newman, Amy Hauck
Publicado em 2010

Design and Synthesis of Substituted N-(1,3-Diphenyl-1H-pyrazol-5-yl)benzamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5

Por Zou, Mu-Fa, Cao, Jianjing, Rodriguez, Alice L., Conn, P. Jeffrey, Newman, Amy Hauck
Publicado em 2010

Synthesis and SAR of Novel, Non-MPEP Chemotype mGluR5 NAMs Identified by Functional HTS

Por Zhou, Ya, Rodriguez, Alice L., Williams, Richard, Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

Structure–Activity Relationships Comparing N-(6-Methylpyridin-yl)-Substituted Aryl Amides to 2-Methyl-6-(substituted-arylethynyl)pyridines or 2-Methyl-4-(substituted-arylethynyl)th...

Por Kulkarni, Santosh S., Zou, Mu-Fa, Cao, Jianjing, Deschamps, Jeffrey R., Rodriguez, Alice L., Conn, P. Jeffrey, Newman, Amy Hauck
Publicado em 2009

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

Por Hammond, Alexis S., Rodriguez, Alice L., Townsend, Steven D., Niswender, Colleen M., Gregory, Karen J., Lindsley, Craig W., Conn, P. Jeffrey
Publicado em 2010

Discovery of Molecular Switches within the ADX-47273 mGlu(5) PAM scaffold that modulate modes of pharmacology to afford potent mGlu(5) NAMs, PAMs and partial antagonists

Por Lamb, Jeffrey P., Engers, Darren W., Niswender, Colleen M., Rodriguez, Alice L., Venable, Daryl F., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2010

Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu(5)

Por Felts, Andrew S., Saleh, Sam A., Le, Uyen, Rodriguez, Alice L., Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.
Publicado em 2009

Discovery of Molecular Switches that Modulate Modes of mGlu(5) Pharmacology In Vitro and In Vivo Within a Series of Functionalized, Regioisomeric 2- and 5-(Phenylethynyl) Pyrimidin...

Por Sharma, Sameer, Kedrowski, Jeffrey, Rook, Jerri M., Smith, Randy L., Jones, Carrie K., Rodriguez, Alice L., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogs of the mGluR5 Ago-potentiator ADX-47273

Por Engers, Darren W., Rodriguez, Alice L., Williams, Richard, Hammond, Alexis A., Venable, Daryl, Oluwatola, Oluwatomi, Sulikowski, Gary A., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

Discovery and SAR of Novel mGluR5 Non-Competitive Antagonists Not Based on an MPEP Chemotype

Por Rodriguez, Alice L., Williams, Richard, Zhou, Ya, Lindsley, Stacey R., Le, Uyen, Grier, Mark D., Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

A Novel Class of Succinimide-Derived Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Provides Insight into a Disconnect in Activity between the Rat and...

Por Cho, Hyekyung P., Engers, Darren W., Venable, Daryl F., Niswender, Colleen M., Lindsley, Craig W., Conn, P. Jeffrey, Emmitte, Kyle A., Rodriguez, Alice L.
Publicado em 2014

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening

Por Mueller, Ralf, Rodriguez, Alice L., Dawson, Eric S., Butkiewicz, Mariusz, Nguyen, Thuy T., Oleszkiewicz, Stephen, Bleckmann, Annalen, Weaver, C. David, Lindsley, Craig W., Conn, P. Jeffrey, Meiler, Jens
Publicado em 2010

3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats

Por Felts, Andrew S., Lindsley, Stacey R., Lamb, Jeffrey P., Rodriguez, Alice L., Menon, Usha N., Jadhav, Satyawan, Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.
Publicado em 2010

Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

Por Williams, Richard, Manka, Jason T., Rodriguez, Alice L., Vinson, Paige N., Niswender, Colleen M., Weaver, C. David, Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado em 2011

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Por Felts, Andrew S., Rodriguez, Alice L., Morrison, Ryan D., Blobaum, Anna L., Byers, Frank W., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.
Publicado no Bioorg Med Chem Lett (2018)

(3-Cyano-5-fluorophenyl)biaryl Negative Allosteric Modulators of mGlu(5): Discovery of a New Tool Compound with Activity in the OSS Mouse Model of Addiction

Por Lindsley, Craig W., Bates, Brittney S., Menon, Usha N., Jadhav, Satyawan B., Kane, Alexander S., Jones, Carrie K., Rodriguez, Alice L., Conn, P. Jeffrey, Olsen, Christopher M., Winder, Danny G., Emmitte, Kyle A.
Publicado em 2011

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu(1)

Por Manka, Jason T., Rodriguez, Alice L., Morrison, Ryan D., Venable, Daryl F., Cho, Hyekyung P., Blobaum, Anna L., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.
Publicado em 2013

Discovery of N-Aryl Piperazines as Selective mGluR(5) Potentiators with Improved In Vivo Utility

Por Zhou, Ya, Manka, Jason T., Rodriguez, Alice L., Weaver, C. David, Days, Emily L., Vinson, Paige N., Jadhav, Satyawan, Hermann, Elizabeth J., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Stauffer, Shaun R.
Publicado em 2010