Improved scale-up synthesis and purification of clinical asthma candidate MIDD0301

Por Knutson, Daniel E., Roni, Rashid, Mian, Yeunus, Cook, James M., Stafford, Douglas C., Arnold, Leggy A.
Publicado no Org Process Res Dev (2020)

Rapid pH-dependent equilibrium of 4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate does not influence bioavailability

Por Roni, Rashid, Li, Guanguan, Mikulsky, Brandon N., Knutson, Daniel E., Mian, Yeunus, Zahn, Nicolas M., Cook, James M., Stafford, Douglas C., Arnold, Leggy A.
Publicado no Mol Pharm (2020)

Nebulized MIDD0301 Reduces Airway Hyperresponsiveness in Moderate and Severe Murine Asthma Models

Por Zahn, Nicolas M., Mikulsky, Brandon N., Roni, M. S. Rashid, Yocum, Gene T., Mian, Md Yeunus, Knutson, Daniel E., Cook, James M., Emala, Charles W., Stafford, Douglas C., Arnold, Leggy A.
Publicado no ACS Pharmacol Transl Sci (2020)

A novel GABA(A) receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo

Por Yocum, Gene T., Perez-Zoghbi, Jose F., Danielsson, Jennifer, Kuforiji, Aisha S., Zhang, Yi, Li, Guanguan, Rashid Roni, M. S., Kodali, Revathi, Stafford, Douglas C., Arnold, Leggy A., Cook, James M., Emala, Charles W.
Publicado no Am J Physiol Lung Cell Mol Physiol (2019)

A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABA(A) Receptor

Por Li, Guanguan, Nieman, Amanda N., Mian, Md Yeunus, Zahn, Nicolas M., Mikulsky, Brandon N., Poe, Michael M., Methuku, Kashi R., Liu, Yongfeng, Cook, James M., Stafford, Douglas C., Arnold, Leggy A.
Publicado no Molecules (2020)

A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model

Por Clayton, Terry, Poe, Michael M., Rallapalli, Sundari, Biawat, Poonam, Savić, Miroslav M., Rowlett, James K., Gallos, George, Emala, Charles W., Kaczorowski, Catherine C., Stafford, Douglas C., Arnold, Leggy A., Cook, James M.
Publicado no Int J Med Chem (2015)

MIDD0301 – A first-in-class anti-inflammatory asthma drug targets GABA(A) receptors without causing systemic immune suppression

Por Zahn, Nicolas M., Huber, Alec T., Mikulsky, Brandon Nicholas, Stepanski, Mae Elizabeth, Kehoe, Alexander Scott, Li, Guanguan, Schussman, Melissa, Rashid Roni, M. S., Kodali, Revathi, Cook, James M., Stafford, Douglas C., Steeber, Douglas A., Arnold, Leggy A.
Publicado no Basic Clin Pharmacol Toxicol (2019)

Targeting nitric oxide production in microglia with novel imidazodiazepines for non-sedative pain treatment

Por Nieman, Amanda N., Li, Guanguan, Zahn, Nicolas M., Mian, Md Yeunus, Mikulsky, Brandon N., Hoffman, Dylan A., Wilcox, Taylor M., Kehoe, Alexander S., Luecke, Ian W., Poe, Michael M., Alvarez-Carbonell, David, Cook, James M., Stafford, Douglas C., Arnold, Leggy A.
Publicado no ACS Chem Neurosci (2020)

Optimization of Substituted Imidazobenzodiazepines as Novel Asthma Treatments

Por Jahan, Rajwana, Stephen, Michael Rajesh, Forkuo, Gloria S., Kodali, Revathi, Guthrie, Margaret L., Nieman, Amanda N., Yuan, Nina Y., Zahn, Nicolas M., Poe, Michael M., Li, Guanguan, Yu, Olivia B., Yocum, Gene T., Emala, Charles W., Stafford, Douglas C., Cook, James M., Arnold, Leggy A.
Publicado no Eur J Med Chem (2016)

Synthesis and characterization of a novel gamma-aminobutyric acid type A (GABA(A)) receptor ligand that combines outstanding metabolic stability, pharmacokinetics, and anxiolytic e...

Por Poe, Michael M., Methuku, Kashi Reddy, Li, Guanguan, Verma, Ashwini R., Teske, Kelly A., Stafford, Douglas C., Arnold, Leggy A., Cramer, Jeffrey W., Jones, Timothy M., Cerne, Rok, Krambis, Michael J., Witkin, Jeffrey M., Jambrina, Enrique, Rehman, Sabah, Ernst, Margot, Cook, James M., Schkeryantz, Jeffrey M.
Publicado no J Med Chem (2016)

A novel orally available asthma drug candidate that reduces smooth muscle constriction and inflammation by targeting GABA(A) receptors in the lung

Por Forkuo, Gloria S., Nieman, Amanda N., Kodali, Revathi, Zahn, Nicolas M., Li, Guanguan, Rashid Roni, M. S., Stephen, Michael Rajesh, Harris, Ted W., Jahan, Rajwana, Guthrie, Margaret L., Yu, Olivia B., Fisher, Janet L., Yocum, Gene T., Emala, Charles W., Steeber, Douglas A., Stafford, Douglas C., Cook, James M., Arnold, Leggy A.
Publicado no Mol Pharm (2018)

Development of GABA(A) Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments

Por Forkuo, Gloria S., Guthrie, Margaret L., Yuan, Nina Y., Nieman, Amanda N., Kodali, Revathi, Jahan, Rajwana, Stephen, Michael R., Yocum, Gene T., Treven, Marco, Poe, Michael M., Li, Guanguan, Yu, Olivia B., Hartzler, Benjamin D., Zahn, Nicolas M., Ernst, Margot, Emala, Charles W., Stafford, Douglas C., Cook, James M., Arnold, Leggy A.
Publicado no Mol Pharm (2016)

Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABA(A) Receptor Modulators

Por Forkuo, Gloria S., Nieman, Amanda N., Yuan, Nina Y., Kodali, Revathi, Yu, Olivia B., Zahn, Nicolas M., Jahan, Rajwana, Li, Guanguan, Stephen, Michael Rajesh, Guthrie, Margaret L., Poe, Michael M., Hartzler, Benjamin D., Harris, Ted W., Yocum, Gene T., Emala, Charles W., Steeber, Douglas A., Stafford, Douglas C., Cook, James M., Arnold, Leggy A.
Publicado no Mol Pharm (2017)