| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Steven R Smith, Warren A Prosser, David J Donahue, Michael E Morgan, Christen M Anderson, William R Shanaha. Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women. Obesity (Silver Spring, Md.). vol 17. issue 3. 2009-06-04. PMID:19057523. |
lorcaserin (apd356), a selective 5-ht(2c) agonist, reduces body weight in obese men and women. |
2009-06-04 |
2023-08-12 |
Not clear |
| Steven R Smith, Warren A Prosser, David J Donahue, Michael E Morgan, Christen M Anderson, William R Shanaha. Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women. Obesity (Silver Spring, Md.). vol 17. issue 3. 2009-06-04. PMID:19057523. |
lorcaserin (apd356) is a potent, selective 5-ht(2c) agonist with ~15-fold and 100-fold selectivity vs. 5-ht(2a) and 5-ht(2b) receptors, respectively. |
2009-06-04 |
2023-08-12 |
Not clear |
| Jason C G Halford, Joanne A Harrol. Neuropharmacology of human appetite expression. Developmental disabilities research reviews. vol 14. issue 2. 2008-12-11. PMID:18646016. |
a 5-ht(2c) agonist lorcaserin is also currently undergoing large-scale clinical trials, but the effect of the drug on human appetite is unknown as yet. |
2008-12-11 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
in this study, we describe the in vitro and in vivo characteristics of lorcaserin [(1r)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1h-3 benzazepine], a selective, high affinity 5-ht(2c) full agonist. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
lorcaserin bound to human and rat 5-ht(2c) receptors with high affinity (k(i) = 15 +/- 1 nm, 29 +/- 7 nm, respectively), and it was a full agonist for the human 5-ht(2c) receptor in a functional inositol phosphate accumulation assay, with 18- and 104-fold selectivity over 5-ht(2a) and 5-ht(2b) receptors, respectively. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
lorcaserin was also highly selective for human 5-ht(2c) over other human 5-ht receptors (5-ht(1a), 5-ht(3), 5-ht(4c), 5-ht5(5a), 5-ht(6), and 5-ht(7)), in addition to a panel of 67 other g protein-coupled receptors and ion channels. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
lorcaserin did not compete for binding of ligands to serotonin, dopamine, and norepinephrine transporters, and it did not alter their function in vitro. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
behavioral observations indicated that unlike the 5-ht(2a) agonist (+/-)-1-(2,5-dimethoxy-4-phenyl)-2-aminopropane, lorcaserin did not induce behavioral changes indicative of functional 5-ht(2a) agonist activity. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
acutely, lorcaserin reduced food intake in rats, an effect that was reversed by pretreatment with the 5-ht(2c)-selective antagonist 6-chloro-5-methyl-1-[6-(2-methylpyridin-3-yloxy)pyridin-3-yl-carbamoyl]indoline (sb242,084) but not the 5-ht(2a) antagonist (r)-(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenylethyl)]-4-piperidine-methanol (mdl 100,907), demonstrating mediation by the 5-ht(2c) receptor. |
2008-05-19 |
2023-08-12 |
human |
| William J Thomsen, Andrew J Grottick, Frederique Menzaghi, Hazel Reyes-Saldana, Stephen Espitia, Diane Yuskin, Kevin Whelan, Michael Martin, Michael Morgan, Weichao Chen, Hussien Al-Shamma, Brian Smith, Derek Chalmers, Dominic Beha. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. The Journal of pharmacology and experimental therapeutics. vol 325. issue 2. 2008-05-19. PMID:18252809. |
these data demonstrate lorcaserin to be a potent, selective, and efficacious agonist of the 5-ht(2c) receptor, with potential for the treatment of obesity. |
2008-05-19 |
2023-08-12 |
human |
| Brian M Smith, Jeffrey M Smith, James H Tsai, Jeffrey A Schultz, Charles A Gilson, Scott A Estrada, Rita R Chen, Douglas M Park, Emily B Prieto, Charlemagne S Gallardo, Dipanjan Sengupta, Peter I Dosa, Jon A Covel, Albert Ren, Robert R Webb, Nigel R A Beeley, Michael Martin, Michael Morgan, Stephen Espitia, Hazel R Saldana, Christina Bjenning, Kevin T Whelan, Andrew J Grottick, Frederique Menzaghi, William J Thomse. 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. Journal of medicinal chemistry. vol 51. issue 2. 2008-04-17. PMID:18095642. |
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. |
2008-04-17 |
2023-08-12 |
rat |
| Jason C G Halford, Joanne A Harrold, Emma J Boyland, Clare L Lawton, John E Blundel. Serotonergic drugs : effects on appetite expression and use for the treatment of obesity. Drugs. vol 67. issue 1. 2007-03-21. PMID:17209663. |
weight loss in the obese has also been produced by treatment with both the serotonin precursor 5-hydroxytryptophan and the preferential 5-ht2c receptor agonist mcpp.a new generation of 5-ht2c receptor selective agonists have been developed and at least one, lorcaserin (apd356), is currently undergoing clinical trials. |
2007-03-21 |
2023-08-12 |
Not clear |