TY  - CONF
AU  - Poe, Michael M.
AU  - Gallos, George
AU  - Puthenkalam, Roshan
AU  - Savić, Miroslav
AU  - Emala, Charles
AU  - Ernst, Margot
AU  - Cook, James M.
PY  - 2015
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2510
PB  - Amer Chemical Soc, Washington
C3  - Abstracts of Papers of the American Chemical Society
T1  - Imidazobenzodiazepines for improving alpha 5-GABAAR subtype selectivity and their pharmacological relevance
VL  - 250
UR  - https://hdl.handle.net/21.15107/rcub_farfar_2510
ER  - 

@conference{
author = "Poe, Michael M. and Gallos, George and Puthenkalam, Roshan and Savić, Miroslav and Emala, Charles and Ernst, Margot and Cook, James M.",
year = "2015",
publisher = "Amer Chemical Soc, Washington",
journal = "Abstracts of Papers of the American Chemical Society",
title = "Imidazobenzodiazepines for improving alpha 5-GABAAR subtype selectivity and their pharmacological relevance",
volume = "250",
url = "https://hdl.handle.net/21.15107/rcub_farfar_2510"
}

Poe, M. M., Gallos, G., Puthenkalam, R., Savić, M., Emala, C., Ernst, M.,& Cook, J. M.. (2015). Imidazobenzodiazepines for improving alpha 5-GABAAR subtype selectivity and their pharmacological relevance. in Abstracts of Papers of the American Chemical Society
Amer Chemical Soc, Washington., 250.
https://hdl.handle.net/21.15107/rcub_farfar_2510

Poe MM, Gallos G, Puthenkalam R, Savić M, Emala C, Ernst M, Cook JM. Imidazobenzodiazepines for improving alpha 5-GABAAR subtype selectivity and their pharmacological relevance. in Abstracts of Papers of the American Chemical Society. 2015;250.
https://hdl.handle.net/21.15107/rcub_farfar_2510 .

Poe, Michael M., Gallos, George, Puthenkalam, Roshan, Savić, Miroslav, Emala, Charles, Ernst, Margot, Cook, James M., "Imidazobenzodiazepines for improving alpha 5-GABAAR subtype selectivity and their pharmacological relevance" in Abstracts of Papers of the American Chemical Society, 250 (2015),
https://hdl.handle.net/21.15107/rcub_farfar_2510 .

TY  - JOUR
AU  - Clayton, Terry
AU  - Poe, Michael M.
AU  - Rallapalli, Sundari
AU  - Biawat, Poonam
AU  - Savić, Miroslav
AU  - Rowlett, James K.
AU  - Gallos, George
AU  - Emala, Charles
AU  - Kaczorowski, Catherine C.
AU  - Stafford, Douglas C.
AU  - Arnold, Leggy
AU  - Cook, James M.
PY  - 2015
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2317
AB  - An updated model of the GABA(A) benzodiazepine receptor pharmacophore of the alpha 5-BzR/GABA(A) subtype has been constructed prompted by the synthesis of subtype selective ligands in light of the recent developments in both ligand synthesis, behavioral studies, and molecular modeling studies of the binding site itself. A number of BzR/GABA(A) alpha 5 subtype selective compounds were synthesized, notably alpha 5-subtype selective inverse agonist PWZ-029 (1) which is active in enhancing cognition in both rodents and primates. In addition, a chiral positive allosteric modulator (PAM), SH-053-2'F-R-CH3 (2), has been shown to reverse the deleterious effects in the MAM-model of schizophrenia as well as alleviate constriction in airway smooth muscle. Presented here is an updated model of the pharmacophore for alpha 5 beta 2 gamma 2 Bz/GABA(A) receptors, including a rendering of PWZ-029 docked within the alpha 5-binding pocket showing specific interactions of the molecule with the receptor. Differences in the included volume as compared to alpha 1 beta 2 gamma 2, alpha 2 beta 2 gamma 2, and alpha 3 beta 2 gamma 2 will be illustrated for clarity. These new models enhance the ability to understand structural characteristics of ligands which act as agonists, antagonists, or inverse agonists at the Bz BS of GABA(A) receptors.
PB  - Hindawi Ltd, London
T2  - International Journal of Medicinal Chemistry
T1  - A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model
DO  - 10.1155/2015/430248
ER  - 

@article{
author = "Clayton, Terry and Poe, Michael M. and Rallapalli, Sundari and Biawat, Poonam and Savić, Miroslav and Rowlett, James K. and Gallos, George and Emala, Charles and Kaczorowski, Catherine C. and Stafford, Douglas C. and Arnold, Leggy and Cook, James M.",
year = "2015",
abstract = "An updated model of the GABA(A) benzodiazepine receptor pharmacophore of the alpha 5-BzR/GABA(A) subtype has been constructed prompted by the synthesis of subtype selective ligands in light of the recent developments in both ligand synthesis, behavioral studies, and molecular modeling studies of the binding site itself. A number of BzR/GABA(A) alpha 5 subtype selective compounds were synthesized, notably alpha 5-subtype selective inverse agonist PWZ-029 (1) which is active in enhancing cognition in both rodents and primates. In addition, a chiral positive allosteric modulator (PAM), SH-053-2'F-R-CH3 (2), has been shown to reverse the deleterious effects in the MAM-model of schizophrenia as well as alleviate constriction in airway smooth muscle. Presented here is an updated model of the pharmacophore for alpha 5 beta 2 gamma 2 Bz/GABA(A) receptors, including a rendering of PWZ-029 docked within the alpha 5-binding pocket showing specific interactions of the molecule with the receptor. Differences in the included volume as compared to alpha 1 beta 2 gamma 2, alpha 2 beta 2 gamma 2, and alpha 3 beta 2 gamma 2 will be illustrated for clarity. These new models enhance the ability to understand structural characteristics of ligands which act as agonists, antagonists, or inverse agonists at the Bz BS of GABA(A) receptors.",
publisher = "Hindawi Ltd, London",
journal = "International Journal of Medicinal Chemistry",
title = "A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model",
doi = "10.1155/2015/430248"
}

Clayton, T., Poe, M. M., Rallapalli, S., Biawat, P., Savić, M., Rowlett, J. K., Gallos, G., Emala, C., Kaczorowski, C. C., Stafford, D. C., Arnold, L.,& Cook, J. M.. (2015). A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. in International Journal of Medicinal Chemistry
Hindawi Ltd, London..
https://doi.org/10.1155/2015/430248

Clayton T, Poe MM, Rallapalli S, Biawat P, Savić M, Rowlett JK, Gallos G, Emala C, Kaczorowski CC, Stafford DC, Arnold L, Cook JM. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. in International Journal of Medicinal Chemistry. 2015;.
doi:10.1155/2015/430248 .

Clayton, Terry, Poe, Michael M., Rallapalli, Sundari, Biawat, Poonam, Savić, Miroslav, Rowlett, James K., Gallos, George, Emala, Charles, Kaczorowski, Catherine C., Stafford, Douglas C., Arnold, Leggy, Cook, James M., "A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model" in International Journal of Medicinal Chemistry (2015),
https://doi.org/10.1155/2015/430248 . .