Search Results - "Deskus, Jeffrey A."

A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist by Hartz, Richard A, Ahuja, Vijay T, Zhuo, Xiaoliang, Mattson, Ronald J, Denhart, Derek J, Deskus, Jeffrey A, Vrudhula, Vivekananda M, Pan, Senliang, Ditta, Jonathan L, Shu, Yue-Zhong, Grace, James E, Lentz, Kimberley A, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Krishnananthan, Subramaniam, Wong, Henry, Qian-Cutrone, Jingfang, Schartman, Richard, Denton, Rex, Lodge, Nicholas J, Zaczek, Robert, Macor, John E, Bronson, Joanne J

“…Detailed metabolic characterization of 8, an earlier lead pyrazinone-based corticotropin-releasing factor-1 (CRF1) receptor antagonist, revealed that this…”
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Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors by Lodge, Nicholas J, Li, Yu-Wen, Chin, Frederick T, Dischino, Douglas D, Zoghbi, Sami S, Deskus, Jeffrey A, Mattson, Ronald J, Imaizumi, Masao, Pieschl, Rick, Molski, Thaddeus F, Fujita, Masahiro, Dulac, Heidi, Zaczek, Robert, Bronson, Joanne J, Macor, John E, Innis, Robert B, Pike, Victor W

“…Abstract Introduction A radioligand for measuring the density of corticotropin-releasing factor subtype-1 receptors (CRF1 receptors) in living animal and human…”
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Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists by SUN, Li-Qiang, JIE CHEN, CEN XU, BRUCE, Marc, DESKUS, Jeffrey A, EPPERSON, James R, TAKAKI, Katherine, JOHNSON, Graham, IBEN, Lawrence, MAHLE, Cathy D, RYAN, Elaine

“…A series of benzoxazole derivatives was synthesized and evaluated as melatoninergic ligands. The binding affinity of these compounds for human MT(1) and MT(2)…”
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Conformationally Restricted Homotryptamines. Part 7: 3-cis-(3-Aminocyclopentyl)indoles As Potent Selective Serotonin Reuptake Inhibitors by King, H. Dalton, Meng, Zhaoxing, Deskus, Jeffrey A, Sloan, Charles P, Gao, Qi, Beno, Brett R, Kozlowski, Edward S, LaPaglia, Melissa A, Mattson, Gail K, Molski, Thaddeus F, Taber, Matthew T, Lodge, Nicholas J, Mattson, Ronald J, Macor, John E

“…A series of conformationally restricted homotryptamines has been synthesized and shown to be potent inhibitors of hSERT. Conformational restriction of the…”
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[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: Introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents by Deskus, Jeffrey A., Dischino, Douglas D., Mattson, Ronald J., Ditta, Jonathan L., Parker, Michael F., Denhart, Derek J., Zuev, Dmitry, Huang, Hong, Hartz, Richard A., Ahuja, Vijay T., Wong, Henry, Mattson, Gail K., Molski, Thaddeus F., Grace, James E., Zueva, Larisa, Nielsen, Julia M., Dulac, Heidi, Li, Yu-Wen, Guaraldi, Mary, Azure, Michael, Onthank, David, Hayes, Megan, Wexler, Eric, McDonald, Jennifer, Lodge, Nicholas J., Bronson, Joanne J., Macor, John E.

“…Based on a favorable balance between CRF-R1 affinity, lipophilicity and metabolic stability, compound 10 was evaluated for potential development as PET…”
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Conformationally Restricted Homotryptamines. 2. Indole Cyclopropylmethylamines as Selective Serotonin Reuptake Inhibitors by Mattson, Ronald J, Catt, John D, Denhart, Derek J, Deskus, Jeffrey A, Ditta, Jonathan L, Higgins, Mendi A, Marcin, Lawrence R, Sloan, Charles P, Beno, Brett R, Gao, Qi, Cunningham, Melissa A, Mattson, Gail K, Molski, Thaddeus F, Taber, Matthew T, Lodge, Nicholas J

“…A series of indole cyclopropylmethylamines were found to be potent serotonin reuptake inhibitors. Nitrile substituents at the 5 and 7 positions of the indole…”
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Chronobiotic activity of N-[2-(2,7-dimethoxyfluoren-9-yl)ethyl]-propanamide. Synthesis and melatonergic pharmacology of fluoren-9-ylethyl amides by Epperson, James R., Bruce, Marc A., Catt, John D., Deskus, Jeffrey A., Hodges, Donald B., Karageorge, George N., Keavy, Daniel J., Mahle, Cathy D., Mattson, Ronald J., Ortiz, Astrid A., Parker, Michael F., Takaki, Katherine S., Watson, Brett T., Joseph P.Yevich

“…Compound 2b demonstrated full agonism at both human MT 1 and MT 2 receptors and demonstrated chronobiotic activity in both acute and chronic rat models,…”
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In Vitro Intrinsic Clearance-Based Optimization of N 3-Phenylpyrazinones as Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by Hartz, Richard A, Ahuja, Vijay T, Rafalski, Maria, Schmitz, William D, Brenner, Allison B, Denhart, Derek J, Ditta, Jonathan L, Deskus, Jeffrey A, Yue, Eddy W, Arvanitis, Argyrios G, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Wong, Harvey, Grace, James E, Lentz, Kimberley A, Li, Jianqing, Lodge, Nicholas J, Zaczek, Robert, Combs, Andrew P, Olson, Richard E, Mattson, Ronald J, Bronson, Joanne J, Macor, John E

“…A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropin-releasing factor-1 (CRF1) receptor antagonists. Selected…”
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Conformationally restricted homotryptamines. Part 6: Indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors by Ditta, Jonathan L., Denhart, Derek J., Deskus, Jeffrey A., Epperson, James R., Meng, Zhaoxing, Gao, Qi, Mattson, Gail K., LaPaglia, Mellissa A., Taber, Matthew T., Molski, Thaddeus F., Lodge, Nicholas J., Mattson, Ronald J., Macor, John E.

“…Racemic 5-(trans-2-aminomethylcyclopropyl)indoles, 5-(trans-2-aminomethylcyclopentyl) indoles, and 5-(cis-2-aminomethylcyclopentyl)indoles were synthesized and…”
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Synthesis, Structure−Activity Relationships, and In Vivo Evaluation of N 3-Phenylpyrazinones as Novel Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by Hartz, Richard A, Ahuja, Vijay T, Arvanitis, Argyrios G, Rafalski, Maria, Yue, Eddy W, Denhart, Derek J, Schmitz, William D, Ditta, Jonathan L, Deskus, Jeffrey A, Brenner, Allison B, Hobbs, Frank W, Payne, Joseph, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Mattson, Gail K, Peng, Yong, Wong, Harvey, Grace, James E, Lentz, Kimberley A, Qian-Cutrone, Jingfang, Zhuo, Xiaoliang, Shu, Yue-Zhong, Lodge, Nicholas J, Zaczek, Robert, Combs, Andrew P, Olson, Richard E, Bronson, Joanne J, Mattson, Ronald J, Macor, John E

“…Evidence suggests that corticotropin-releasing factor-1 (CRF1) receptor antagonists may offer therapeutic potential for the treatment of diseases associated…”
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Conformationally restricted homotryptamines. Part 5: 3-(trans-2-aminomethylcyclopentyl)indoles as potent selective serotonin reuptake inhibitors by Denhart, Derek J., Deskus, Jeffrey A., Ditta, Jonathan L., Gao, Qi, Dalton King, H., Kozlowski, Edward S., Meng, Zhaoxing, LaPaglia, Melissa A., Mattson, Gail K., Molski, Thaddeus F., Taber, Matthew T., Lodge, Nicholas J., Mattson, Ronald J., Macor, John E.

“…A series of amines with structure 10 were synthesized and tested for inhibition of the human serotonin transporter (hSERT). A series of racemic…”
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Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors by Deskus, Jeffrey A., Epperson, James R., Sloan, Charles P., Cipollina, Joseph A., Dextraze, Pierre, Qian-Cutrone, Jingfang, Gao, Qi, Ma, Baoqing, Beno, Brett R., Mattson, Gail K., Molski, Thaddeus F., Krause, Rudolph G., Taber, Matthew T., Lodge, Nicholas J., Mattson, Ronald J.

“…A series of indole tetrahydropyridine and indole cyclohexenylamines was prepared, and their binding affinities at the human serotonin transporter (SERT) were…”
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Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor by Dalton King, H., Denhart, Derek J., Deskus, Jeffrey A., Ditta, Jonathan L., Epperson, James R., Higgins, Mendi A., Kung, Joyce E., Marcin, Lawrence R., Sloan, Charles P., Mattson, Gail K., Molski, Thaddeus F., Krause, Rudolph G., Bertekap, Robert L., Lodge, Nicholas J., Mattson, Ronald J., Macor, John E.

“…Hybrid molecules containing the cyclopropylmethylamino side chain found in the parent homotryptamine system and an isosteric heteroaryl or naphthyl core were…”
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Aminotriazine 5-HT7 antagonists by MATTSON, Ronald J, DENHART, Derek J, PURANDARE, Ashok, TORTOLANI, David, YUFEN ZHAO, HUA YANG, YEOLA, Suresh, PALMER, Jane, TORRENTE, John, STARK, Arlene, JOHNSON, Graham, CATT, John D, DEE, Michael F, DESKUS, Jeffrey A, DITTA, Jonathan L, EPPERSON, James, KING, H. Dalton, AIMING GAO, POSS, Michael A

“…The present studies have identified a series of aminotriazines as novel 5-HT(7) receptor antagonists. Compounds 10 and 17 have high affinity for the 5-HT(7)…”
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4-Substituted anilides as selective melatonin MT2 receptor agonists by EPPERSON, James R, DESKUS, Jeffrey A, GENTILE, Anthony J, IBEN, Lawrence G, RYAN, Elaine, SARBIN, Nathan S

“…A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2)…”
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Diaminopyrimidine and diaminopyridine 5-HT7 ligands by DENHART, Derek J, PURANDARE, Ashok V, MATTSON, Ronald J, CATT, John D, KING, H. Dalton, AIMING GAO, DESKUS, Jeffrey A, POSS, Michael A, STARK, Arlene D, TORRENTE, John R, JOHNSON, Graham

“…The present studies have identified a series of diaminopyrimidines and diaminopyridines as novel 5-HT(7) receptor ligands. Three regiosiomeric classes of…”
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Heterocyclic aminopyrrolidine derivatives as melatoninergic agents by SUN, Li-Qiang, JIE CHEN, ORTIZ, Astrid, MOLSTAD, David, RYAN, Elaine, YELESWARAM, Krishnaswamy, CEN XU, GUANGLIN LUO, MATTSON, Ronald J, EPPERSON, James R, DESKUS, Jeffrey A, LI, Wen-Sen, TAKAKI, Katherine, HODGES, Donald B, IBEN, Lawrence, MAHLE, Cathy D

“…A series of chiral heterocyclic aminopyrrolidine derivatives was synthesized as novel melatoninergic ligands. Binding affinity assays were performed on cloned…”
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Corrections to In Vitro Intrinsic Clearance-Based Optimization of N 3-Phenylpyrazinones as Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by Hartz, Richard A., Ahuja, Vijay T., Rafalski, Maria, Schmitz, William D., Brenner, Allison B., Denhart, Derek J., Ditta, Jonathan L., Deskus, Jeffrey A., Yue, Eddy W., Arvanitis, Argyrios G., Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F., Wong, Harvey, Grace, James E., Lentz, Kimberley A., Li, Jianqing, Lodge, Nicholas J., Zaczek, Robert, Combs, Andrew P., Olson, Richard E., Mattson, Ronald J., Bronson, Joanne J., Macor, John E.

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In Vitro Intrinsic Clearance-Based Optimization of N3-Phenylpyrazinones as Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by HARTZ, Richard A, AHUJA, Vijay T, LELAS, Snjezana, LI, Yu-Wen, MOLSKI, Thaddeus F, WONG, Harvey, GRACE, James E, LENTZ, Kimberley A, JIANQING LI, LODGE, Nicholas J, ZACZEK, Robert, COMBS, Andrew P, RAFALSKI, Maria, OLSON, Richard E, MATTSON, Ronald J, BRONSON, Joanne J, MACOR, John E, SCHMITZ, William D, BRENTER, Allison B, DENHART, Derek J, DITTA, Jonathan L, DESKUS, Jeffrey A, YUE, Eddy W, ARVANITIS, Argyrios G

“…A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropin-releasing factor-1 (CRF(1)) receptor antagonists. Selected…”
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Synthesis, Structure—Activity Relationships, and In Vivo Evaluation of N3-Phenylpyrazinones as Novel Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists by HARTZ, Richard A, AHUJA, Vijay T, HOBBS, Frank W, PAYNE, Joseph, LELAS, Snjezana, LI, Yu-Wen, MOLSKI, Thaddeus F, MATTSON, Gail K, YONG PENG, WONG, Harvey, GRACE, James E, LENTZ, Kimberley A, ARVANITIS, Argyrios G, QIAN-CUTRONE, Jingfang, XIAOLIANG ZHUO, SHU, Yue-Zhong, LODGER, Nicholas J, ZACZEK, Robert, COMBS, Andrew P, OLSON, Richard E, BRONSON, Joanne J, MATTSON, Ronald J, MACOR, John E, RAFALSKI, Maria, YUE, Eddy W, DENHART, Derek J, SCHMITZ, William D, DITTA, Jonathan L, DESKUS, Jeffrey A, BRENNER, Allison B

“…Evidence suggests that corticotropin-releasing factor-1 (CRF(1)) receptor antagonists may offer therapeutic potential for the treatment of diseases associated…”
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