Search Results - "GROTTICK, Andrew J"

Convergent observations of MK-801-induced impairment in rat 5C-CPT performance across laboratories: reversal with a D1 but not nicotinic agonist by Grottick, Andrew J., MacQueen, David L., Barnes, Samuel A., Carroll, Chris, Sanabria, Erin K., Bobba, Vishal, Young, Jared W.

“…Introduction Cognitive function is closely linked to functional outcomes in psychiatric disorders such as schizophrenia, however developing effective…”
Get full text

Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization by Thomsen, William J, Grottick, Andrew J, Menzaghi, Frederique, Reyes-Saldana, Hazel, Espitia, Stephen, Yuskin, Diane, Whelan, Kevin, Martin, Michael, Morgan, Michael, Chen, Weichao, Al-Shamma, Hussien, Smith, Brian, Chalmers, Derek, Behan, Dominic

“…5-Hydroxytryptamine (5-HT)(2C) receptor agonists hold promise for the treatment of obesity. In this study, we describe the in vitro and in vivo characteristics…”
Get more information

Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119 by Semple, Graeme, Fioravanti, Beatriz, Pereira, Guillherme, Calderon, Imelda, Uy, Jane, Choi, Karoline, Xiong, Yifeng, Ren, Albert, Morgan, Michael, Dave, Vibha, Thomsen, William, Unett, David J, Xing, Charles, Bossie, Stuart, Carroll, Chris, Chu, Zhi-Liang, Grottick, Andrew J, Hauser, Erin K, Leonard, James, Jones, Robert M

“…GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels…”
Get full text

Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity by Smith, Brian M, Smith, Jeffrey M, Tsai, James H, Schultz, Jeffrey A, Gilson, Charles A, Estrada, Scott A, Chen, Rita R, Park, Douglas M, Prieto, Emily B, Gallardo, Charlemagne S, Sengupta, Dipanjan, Dosa, Peter I, Covel, Jon A, Ren, Albert, Webb, Robert R, Beeley, Nigel R. A, Martin, Michael, Morgan, Michael, Espitia, Stephen, Saldana, Hazel R, Bjenning, Christina, Whelan, Kevin T, Grottick, Andrew J, Menzaghi, Frederique, Thomsen, William J

“…The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more…”
Get full text

Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain by Han, Sangdon, Thoresen, Lars, Jung, Jae-Kyu, Zhu, Xiuwen, Thatte, Jayant, Solomon, Michelle, Gaidarov, Ibragim, Unett, David J, Yoon, Woo Hyun, Barden, Jeremy, Sadeque, Abu, Usmani, Amin, Chen, Chuan, Semple, Graeme, Grottick, Andrew J, Al-Shamma, Hussein, Christopher, Ronald, Jones, Robert M

“…The discovery of a novel, selective and fully efficacious CB2 agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound 6…”
Get full text

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT 2C receptor by Schrader, Thomas O, Kasem, Michelle, Ren, Albert, Feichtinger, Konrad, Al Doori, Bilal, Wei, Jing, Wu, Chunrui, Dang, Huong, Le, Minh, Gatlin, Joel, Chase, Kelli, Dong, Jenny, Whelan, Kevin T, Sage, Carleton, Grottick, Andrew J, Semple, Graeme

“…The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT receptor agonists are…”
Get full text

Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists by Chaki, Shigeyuki, Funakoshi, Takeo, Hirota-Okuno, Shiho, Nishiguchi, Mariko, Shimazaki, Toshiharu, Iijima, Michihiko, Grottick, Andrew J, Kanuma, Kosuke, Omodera, Katsunori, Sekiguchi, Yoshinori, Okuyama, Shigeru, Tran, Thuy-Anh, Semple, Graeme, Thomsen, William

“…Melanin-concentrating hormone (MCH) is a cyclic peptide produced in the lateral hypothalamus. It has been implicated in a number of physiological processes…”
Get more information

Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia by Al-Shamma, Hussien A, Anderson, Christen, Chuang, Emil, Luthringer, Remy, Grottick, Andrew J, Hauser, Erin, Morgan, Michael, Shanahan, William, Teegarden, Bradley R, Thomsen, William J, Behan, Dominic

“…5-Hydroxytryptamine (5-HT)(2A) receptor inverse agonists are promising therapeutic agents for the treatment of sleep maintenance insomnias. Among these agents…”
Get more information

Convergent observations of MK-801-induced impairment in rat 5C-CPT performance across laboratories: reversal with a D 1 but not nicotinic agonist by Grottick, Andrew J, MacQueen, David L, Barnes, Samuel A, Carroll, Chris, Sanabria, Erin K, Bobba, Vishal, Young, Jared W

“…Cognitive function is closely linked to functional outcomes in psychiatric disorders such as schizophrenia, however developing effective treatments for…”
Get full text

A new family of H3 receptor antagonists based on the natural product Conessine by SANTORA, Vincent J, COVEL, Jonathan A, WEBB, Robert R, SAGE, Carleton, REN, Albert, PEREIRA, Guilherme, KNUDSEN, Jens, EDWARDS, Jeffrey E, SUAREZ, Marissa, FRAZER, John, THOMSEN, William, HAUSER, Erin, HAYASHI, Rena, WHELAN, Kevin, GROTTICK, Andrew J, HOFILENA, Brian J, IBARRA, Jason B, PULLEY, Michelle D, WEINHOUSE, Michael I, SENGUPTA, Dipanjan, DUFFIELD, Jonathan J, SEMPLE, Graeme

“…A new family of Histamine H(3) receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H(3) antagonist…”
Get full text

GPR52 Agonists Attenuate Ropinirole-Induced Preference for Uncertain Outcomes by Russell, Brittney, Barrus, Michael M., Tremblay, Melanie, Ma, Lawrence, Hrelja, Kelly, Wong, Christina, Hynes, Tristan J., Hobson, Scott, Grottick, Andrew J., Winstanley, Catharine A.

“…Dopamine D2/3 receptor agonists are less likely to trigger dyskinesias than l-dopa while still offering relief from the motor symptoms of Parkinson's disease…”
Get full text

Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916) by Semple, Graeme, Santora, Vincent J., Smith, Jeffrey M., Covel, Jonathan A., Hayashi, Rena, Gallardo, Charlemagne, Ibarra, Jason B., Schultz, Jeffrey A., Park, Douglas M., Estrada, Scott A., Hofilena, Brian J., Smith, Brian M., Ren, Albert, Suarez, Marissa, Frazer, John, Edwards, Jeffrey E., Hart, Ryan, Hauser, Erin K., Lorea, Jodie, Grottick, Andrew J.

“…The design of a new clinical candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described…”
Get full text

Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT2C receptor by Schrader, Thomas O., Zhu, Xiuwen, Kasem, Michelle, Ren, Albert, Liu, Chunyan, Wu, Chunrui, Dang, Huong, Le, Minh, Gatlin, Joel, Chase, Kelli, Frazer, John, Whelan, Kevin T., Grottick, Andrew J., Hutton, Clayton, Barden, Jeremy, Chen, Chuan, Ortiz, Alvaro, Feichtinger, Konrad, Semple, Graeme

“…[Display omitted] A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the…”
Get full text

Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays by Ren, Albert, Zhu, Xiuwen, Feichtinger, Konrad, Lehman, Juerg, Kasem, Michelle, Schrader, Thomas O., Wong, Amy, Dang, Huong, Le, Minh, Frazer, John, Unett, David J., Grottick, Andrew J., Whelan, Kevin T., Morgan, Michael E., Sage, Carleton R., Semple, Graeme

“…[Display omitted] A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were…”
Get full text

Investigating interactions between phentermine, dexfenfluramine, and 5-HT2C agonists, on food intake in the rat by Grottick, Andrew J., Whelan, Kevin, Sanabria, Erin K., Behan, Dominic P., Morgan, Michael, Sage, Carleton

“…Rationale Synergistic or supra-additive interactions between the anorectics (dex)fenfluramine and phentermine have been reported previously in the rat and in…”
Get full text

Differential Effects of the 5-HT2A Receptor Antagonist M100,907 and the 5-HT2C Receptor Antagonist SB242,084 on Cocaine-induced Locomotor Activity, Cocaine Self-administration and Cocaine-induced Reinstatement of Responding by Fletcher, Paul J, Grottick, Andrew J, Higgins, Guy A

“…These studies investigated the effects of antagonists selective for the 5-HT2A, 5-HT2B, or 5-HT2C receptor subtypes on behaviors elicited or maintained by…”
Get full text

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor by Schrader, Thomas O., Kasem, Michelle, Ren, Albert, Feichtinger, Konrad, Al Doori, Bilal, Wei, Jing, Wu, Chunrui, Dang, Huong, Le, Minh, Gatlin, Joel, Chase, Kelli, Dong, Jenny, Whelan, Kevin T., Sage, Carleton, Grottick, Andrew J., Semple, Graeme

“…[Display omitted] The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C…”
Get full text

Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control by Semple, Graeme, Ren, Albert, Fioravanti, Beatriz, Pereira, Guillherme, Calderon, Imelda, Choi, Karoline, Xiong, Yifeng, Shin, Young-Jun, Gharbaoui, Tawfik, Sage, Carleton R., Morgan, Michael, Xing, Charles, Chu, Zhi-Liang, Leonard, James N., Grottick, Andrew J., Al-Shamma, Hussein, Liang, Yin, Demarest, Keith T., Jones, Robert M.

“…The design of a new series of agonists of the orphan G-protein coupled receptor GPR119, starting from AR231453 is outlined. This resulted in the discovery of…”
Get full text

Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile by Semple, Graeme, Lehmann, Juerg, Wong, Amy, Ren, Albert, Bruce, Marc, Shin, Young-Jun, Sage, Carleton R., Morgan, Michael, Chen, Wei-Chao, Sebring, Kristen, Chu, Zhi-Liang, Leonard, James N., Al-Shamma, Hussein, Grottick, Andrew J., Du, Fuyong, Liang, Yin, Demarest, Keith, Jones, Robert M.

“…The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. Compound 16 (APD597,…”
Get full text

Discovery of APD371: Identification of a Highly Potent and Selective CB 2 Agonist for the Treatment of Chronic Pain by Han, Sangdon, Thoresen, Lars, Jung, Jae-Kyu, Zhu, Xiuwen, Thatte, Jayant, Solomon, Michelle, Gaidarov, Ibragim, Unett, David J, Yoon, Woo Hyun, Barden, Jeremy, Sadeque, Abu, Usmani, Amin, Chen, Chuan, Semple, Graeme, Grottick, Andrew J, Al-Shamma, Hussein, Christopher, Ronald, Jones, Robert M

“…The discovery of a novel, selective and fully efficacious CB agonist with satisfactory pharmacokinetic and pharmaceutical properties is described. Compound was…”
Get full text