lorcaserin: orally active, small-molecule 5-hydroxytryptamine 2C agonist for the potential treatment of obesity and diabetes [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
lorcaserin : A benzazepine that is 2,3,4,5-tetrahydro-3-benzazepine substituted at position 1 by a methyl group and a t position 6 by a chloro group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
ID Source | ID |
---|---|
PubMed CID | 11658860 |
CHEMBL ID | 360328 |
CHEBI ID | 65353 |
SCHEMBL ID | 169382 |
MeSH ID | M0520419 |
Synonym |
---|
616202-92-7 |
AC-553 |
gtpl2941 |
(r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-benzo[d]azepine |
belviq |
lorcaserin |
bdbm50161646 |
(1r)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1h-3-benzazepine |
CHEMBL360328 , |
chebi:65353 , |
NCGC00182550-01 |
(1r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine |
ar-10a |
8-chloro-2,3,4,5-tetrahydro-1-methyl-1h-3-benzazepine |
cas-616202-92-7 |
tox21_113018 |
dtxcid0028585 |
dtxsid3048659 , |
hsdb 8128 |
unii-637e494o0z |
belvig |
637e494o0z , |
(r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine |
lorcaserin [inn] |
AKOS006326204 |
HY-11093 |
CS-1232 |
lorcaserin [who-dd] |
1h-3-benzazepine, 8-chloro-2,3,4,5-tetrahydro-1-methyl-, (1r)- |
lorcaserin [vandf] |
lorcaserin [mi] |
XTTZERNUQAFMOF-QMMMGPOBSA-N |
AM81248 |
SCHEMBL169382 |
tox21_113018_1 |
NCGC00182550-02 |
(5r)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine |
DB04871 |
Q340139 |
T4U , |
lorcaserinum |
lorcaserine |
a08aa11 |
Lorcaserin is an anti-obesity drug whose weight loss effect results from 5-hydroxytryptamin (5-HT) Lorcasersin HCl is a novel, synthetic, centrally-acting selective serotonin C receptor, l agonist, which results in increased satiety.
Excerpt | Reference | Relevance |
---|---|---|
"Lorcaserin has been approved for chronic weight management in the United States as an adjunct to a reduced-calorie diet and exercise, and the previous phase 3 Behavioral Modification and Lorcaserin for Obesity and Overweight Management in Diabetes Mellitus (BLOOM-DM) study has shown that, in addition to weight loss, lorcaserin is associated with improvements in glycemic parameters." | ( Impact of lorcaserin on glycemic control in overweight and obese patients with type 2 diabetes: analysis of week 52 responders and nonresponders. Fain, R; Garvey, WT; Ma, T; Pi-Sunyer, X; Shanahan, W, 2016) | 1.56 |
Lorcaserin treatment reduced fat mass (P < 0.001), the fatty liver index and energy intake without affecting energy expenditure or lean mass. Pretreatment of lorcasersin or the positive control clonidine ameliorated the naloxone-precipitated withdrawal symptoms.
The selectivity of lorcaserin for 5-HT2C receptors should reduce patient risk for the serious adverse complications that are associated with nonselective 5- HT agonist therapies, such as cardiac valvulopathy and pulmonary hypertension. There may be differences in the side effect profiles between lorcasersin and CP-809101.
Excerpt | Reference | Relevance |
---|---|---|
" Three studies were conducted to evaluate the pharmacokinetic properties and tolerability of lorcaserin in these populations." | ( Pharmacokinetics and Tolerability of Lorcaserin in Special Populations: Elderly Patients and Patients with Renal or Hepatic Impairment. Anderson, C; Christopher, RJ; Morgan, ME; Sanchez, M; Shanahan, W; Tang, Y, 2017) | 0.95 |
" Methods for understanding PK will help in conducting pharmacokinetic - pharmacodynamic (PK-PD) correlations and improving the quality and applicability of data obtained using zebrafish." | ( Correlation of pharmacokinetics and brain penetration data of adult zebrafish with higher mammals including humans. Kulkarni, P; Medishetti, R; Nune, N; Oruganti, S; Rao, P; Saxena, U; Sripuram, V; Sriram, D; Yellanki, S; Yogeeswari, P, ) | 0.13 |
Excerpt | Reference | Relevance |
---|---|---|
"Lorcaserin in combination with phentermine improves control of food cravings during short-term energy restriction." | ( Effect of Lorcaserin Alone and in Combination with Phentermine on Food Cravings After 12-Week Treatment: A Randomized Substudy. Aronne, LJ; Coulter, AA; Fujioka, K; Garvey, WT; Greenway, FL; Nikonova, EV; Rebello, CJ; Smith, SR; Zhou, S, 2018) | 2.33 |
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Lorcaserin pretreatment produced a dose-dependent flattening of the dose-response function for heroin self-administration in each subject. Additional factors associated with decreased drug taking include intermittent dosing for dopamine antagonists and use of progressive-ratio schedules.
Excerpt | Relevance | Reference |
---|---|---|
" The model could also be used to assess dose-response relationships." | ( Assessment of maximum weight change and duration of therapeutic effect for non-surgical treatment of obesity using an exponential model. Chan, LS; Kaptein, EM; Kaptein, JS, 2012) | 0.38 |
" In monkeys discriminating cocaine from saline, lorcaserin alone did not occasion cocaine-appropriate responding but shifted the cocaine dose-response curve to the right and down in two of three monkeys." | ( Lorcaserin Reduces the Discriminative Stimulus and Reinforcing Effects of Cocaine in Rhesus Monkeys. Collins, GT; France, CP; Gerak, LR; Javors, MA, 2016) | 2.13 |
"To determine whether dosage adjustment is likely to be necessary for effective and well-tolerated use of a pharmaceutical agent, guidance documents from the US Food and Drug Administration recommend pharmacokinetics studies in patients with impaired renal or impaired hepatic function and in the elderly population." | ( Pharmacokinetics and Tolerability of Lorcaserin in Special Populations: Elderly Patients and Patients with Renal or Hepatic Impairment. Anderson, C; Christopher, RJ; Morgan, ME; Sanchez, M; Shanahan, W; Tang, Y, 2017) | 0.73 |
" Lorcaserin pretreatment produced a dose-dependent flattening of the dose-response function for heroin self-administration in each subject." | ( Lorcaserin decreases the reinforcing effects of heroin, but not food, in rhesus monkeys. Bergman, J; Kohut, SJ, 2018) | 2.83 |
" Additional factors associated with decreased drug taking include intermittent dosing for dopamine antagonists and use of progressive-ratio schedules for lorcaserin." | ( Biphasic reward effects are characteristic of both lorcaserin and drugs of abuse: implications for treatment of substance use disorders. Burnell, K; De, A; Grasing, KW, 2022) | 1.17 |
Role | Description |
---|---|
appetite depressant | Agent that is used to decrease appetite. |
anti-obesity agent | Any substance which is used to reduce or control weight. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
benzazepine | A group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.0901 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 13.8061 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 1.9497 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 23.7083 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 11.8832 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 10.0000 | 0.0003 | 1.4656 | 10.0000 | AID418839 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.6212 | 0.0000 | 0.3855 | 10.0000 | AID1512840; AID1574711; AID1656832; AID418835; AID731446 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 0.0713 | 0.0001 | 0.9549 | 10.0000 | AID1512839; AID1574713; AID1656833; AID418837; AID594581; AID594585; AID780300 |
Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 2.6060 | 0.0000 | 0.7048 | 8.1930 | AID418838 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.1517 | 0.0003 | 0.7693 | 10.0000 | AID1512841; AID1574712; AID1656829; AID418836; AID731445 |
Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 10.0000 | 0.0002 | 1.1115 | 8.0280 | AID418840 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Cytochrome P450 1A2 | Homo sapiens (human) | EC50 (µMol) | 0.0399 | 0.0003 | 0.2069 | 2.0000 | AID1446073 |
Cytochrome P450 3A4 | Homo sapiens (human) | EC50 (µMol) | 0.0399 | 0.0001 | 0.2328 | 3.2000 | AID1446073 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | EC50 (µMol) | 0.3587 | 0.0000 | 0.2276 | 3.4750 | AID1199735; AID1280456; AID1446071; AID1565294; AID1656830; AID1686087; AID246590; AID312492; AID418828 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | EC50 (µMol) | 0.0222 | 0.0001 | 0.1008 | 2.4500 | AID1199729; AID1280452; AID1446067; AID1446073; AID1565288; AID1656835; AID1686079; AID1686091; AID1686094; AID246589; AID312493; AID418831; AID594578; AID594586; AID731447 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | EC50 (µMol) | 0.5083 | 0.0004 | 0.2061 | 1.0000 | AID1199721; AID1199732; AID1280454; AID1446069; AID1565291; AID1686083; AID246591; AID312494; AID418829; AID594588 |
5-hydroxytryptamine receptor 2C | Canis lupus familiaris (dog) | EC50 (µMol) | 0.0162 | 0.0108 | 0.0135 | 0.0162 | AID594742 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID624219 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID624235 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID624216 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C | 2008 | The Journal of pharmacology and experimental therapeutics, May, Volume: 325, Issue:2 | Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. |
AID1199732 | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1512842 | Selectivity ratio of Ki for 5-HT2AR (unknown origin) to Ki for 5-HT2CR (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
AID731445 | Agonist activity at 5-HT2B receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists. |
AID1656881 | Selectivity index, ratio of Ki for displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2B receptor expressed in HEK293 cells measured after 2 hrs by scintillation counter method to Ki for displacement of [125I]-1 | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1686097 | Bias factor, ratio of log(Emax/EC50) of lorcaserin to test compound for agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1446071 | Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID418834 | Selectivity ratio of EC50 for human 5HT2B receptor to EC50 for human 5HT2C receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID594588 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1446069 | Agonist activity at human 5-HT2B receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID731446 | Agonist activity at 5-HT2A receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists. |
AID1446073 | Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1686087 | Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1686083 | Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID594578 | Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1199739 | Selectivity ratio of EC50 for human 5-HT2A receptor to EC50 for human 5HT2C receptor | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID312493 | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID312497 | Reduction of food intake in Sprague-Dawley rat at 50 umol/kg, po after 2 hrs relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1686079 | Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID312512 | Reduction of body weight in Sprague-Dawley rat at 18 mg/kg, po, qd after 28 days relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID312496 | Reduction of food intake in Sprague-Dawley rat at 25 umol/kg, po after 2 hrs relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1686089 | Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux by measuring log(Emax/EC50) incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID780316 | Selectivity ratio of Ki for 5-HT2A receptor (unknown origin) to Ki for 5-HT2C receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model. |
AID1446094 | Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay relative to serotonin | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1574713 | Displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
AID1686088 | Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1359193 | Anorexic effect in diet-induced obese C57BL/6J mouse assessed as reduction in cumulative food intake at 10 mg/kg, po pretreated for 30 mins followed by food addition measured after 4 hrs | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Identification of novel β-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents. |
AID1446075 | Ratio of Emax to EC50 for human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID418832 | Agonist activity at human 5HT2C receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID252842 | Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2C receptor in HEK293 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID594583 | Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization at 10 uM by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID418836 | Displacement of [3H]LSD from human 5HT2B receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID418831 | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID312500 | Half life in Sprague-Dawley rat at 5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID312511 | Selectivity ratio of pEC50 for human 5HT2B to pEC50 for human 5HT2C | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1280452 | Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID418839 | Displacement of [3H]nisoxetine from NET | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID312509 | Reduction of body weight in Sprague-Dawley rat at 36 mg/kg, po, bid after 28 days relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1512843 | Selectivity ratio of Ki for 5-HT2BR (unknown origin) to Ki for 5-HT2CR (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
AID252843 | Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2A receptor in HEK293 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID1199721 | Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID312513 | Reduction of body weight in Sprague-Dawley rat at 9 mg/kg, po, bid after 28 days relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1280456 | Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID780300 | Binding affinity to 5-HT2C receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model. |
AID594581 | Displacement of [3H]meselurgine from human 5HT2C receptor expressed in Swiss mouse 3T3 cells by scintillation proximity assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID312508 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1656828 | Agonist activity at 5HT2B receptor (unknown origin) relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1565288 | Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID1595986 | Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as reduction in body fat mass at 10 mg/kg, po measured after 6 weeks relative to control by NMR-based magnetic resonance imaging analysis | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity. |
AID1280455 | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID1656830 | Partial agonist activity at 5HT2A receptor (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1686092 | Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1686098 | Bias factor, ratio of log(Emax/EC50) of lorcaserin to test compound for agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID594587 | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as 5-HT-induced maximum response by inositol phosphate accumulation assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1686084 | Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1686094 | Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1686081 | Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux by measuring log (Emax/EC50) incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1656832 | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2A receptor (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1446067 | Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID780317 | Selectivity ratio of Ki for 5-HT2B receptor (unknown origin) to Ki for 5-HT2C receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22 | In vitro structure-activity relationships of aplysinopsin analogs and their in vivo evaluation in the chick anxiety-depression model. |
AID312502 | Clearance in Sprague-Dawley rat at 5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID418828 | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1656836 | Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate at 10 ul measured after 2 hrs in presence of [3H]inositol by scintillation counter method relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID418837 | Displacement of [3H]mesulergine from 5HT2C receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1595982 | Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as change in body weight at 10 mg/kg, po measured after 6 weeks (Rvb = 3.86 +/- 0.99 g) | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity. |
AID246591 | Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID312514 | Reduction of body weight in Sprague-Dawley rat at 18 mg/kg, po, bid after 28 days relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1565292 | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID312501 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1686096 | Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment by measuring log (Emax/EC50) incubated for 20 hrs by Tango assay relative to 5HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1565294 | Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID1574712 | Displacement of [3H]DOI from recombinant human 5HT2B receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
AID1574714 | Selectivity ratio of Ki for displacement of [3H]DOI from recombinant human 5HT2A receptor expressed in HEK293T cell membranes to Ki for displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
AID594585 | Displacement of [125I]DOI from human recombinant 5HT2C receptor expressed in HEK293 cells by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1446098 | Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay relative to | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID418827 | Agonist activity at human 5HT2A receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1656833 | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2C receptor expressed in HEK293 cells measured after 2 hrs by scintillation counter method | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1595969 | Anorexic effect in high fat diet-induced obese C57BL/6J mouse model assessed as reduction in cumulative food intake at 10 mg/kg, po pretreated for 30 mins followed by food addition measured after 4 hrs relative to control | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity. |
AID1199736 | Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1656835 | Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1199720 | Selectivity for human recombinant 5HT2C receptor over human recombinant 5HT2B receptor | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1280457 | Agonist activity at human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID418840 | Displacement of [3H]WIN-35428 from DAT | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1686091 | Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1446081 | Toxicity in C57BL/6J mouse assessed as reduction in baseline locomotive activity at 3 mg/kg, ip after 15 mins | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID418835 | Displacement of [3H]ketanserin from human 5HT2A receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID594580 | Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1512840 | Agonist activity at 5-HT2AR (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
AID1199730 | Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1565295 | Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID252844 | Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2B receptor in HEK293 cells | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID1574715 | Selectivity ratio of Ki for displacement of [3H]DOI from recombinant human 5HT2B receptor expressed in HEK293T cell membranes to Ki for displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
AID1280454 | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID1686085 | Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux by measuring log(Emax/EC50) incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID312499 | Reduction of food intake in Sprague-Dawley rat after 6 hrs relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID312504 | Tmax in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID418842 | Selectivity ratio of Ki for human 5HT2B receptor to Ki for 5HT2C receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID594742 | Agonist activity at dog 5HT2C receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID731447 | Agonist activity at 5-HT2C receptor (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists. |
AID594586 | Agonist activity at human 5HT2C receptor expressed in HEK293 cells by inositol phosphate accumulation assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1686093 | Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux by measuring log (Emax/EC50) incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1595979 | Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as reduction in body weight at 10 mg/kg, po | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9 | Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity. |
AID418841 | Selectivity ratio of Ki for human 5HT2A receptor to Ki for 5HT2C receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID312507 | AUC (0-infinity) in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1446096 | Agonist activity at human 5-HT2A receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay relative to serotonin | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1446095 | Agonist activity at human 5-HT2B receptor expressed in Flp-IN HEK293 cells assessed as induction of calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay relative to serotonin | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1446076 | Ratio of Emax to EC50 for tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment activity | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID312498 | Reduction of food intake in Sprague-Dawley rat at 100 umol/kg, po after 2 hrs relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID246589 | Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID1686080 | Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID1512839 | Agonist activity at 5-HT2CR (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
AID1446086 | Antipsychotic activity in PCP-induced hyperactivity C57BL/6J mouse model assessed as reduction in PCP-induced hyper-locomotion at 3 mg/kg, ip preincubated for 15 mins followed by PCP addition measured after 60 mins | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1199733 | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1199722 | Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis relative to 5-HT | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1446083 | Antipsychotic activity in AMPH-induced hyperactivity C57BL/6J mouse model assessed as reduction in amphetamine-induced hyper-locomotion at 3 mg/kg, ip preincubated for 15 mins followed by AMPH addition measured after 90 mins | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications. |
AID1199735 | Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1656876 | Selectivity index, ratio of Ki for displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2A receptor expressed in HEK293 cells measured after 2 hrs by scintillation counter method to Ki for displacement of [125I]-1 | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID246590 | Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity. |
AID418829 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID312492 | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1512841 | Agonist activity at 5-HT2BR (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1 | Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT |
AID1565291 | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID418838 | Displacement of [3H]citalopram from SERT | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1565289 | Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT |
AID1656831 | Partial agonist activity at 5HT2A receptor (unknown origin) relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID594743 | Agonist activity at dog 5HT2C receptor ralative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1199729 | Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID1359256 | Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as decrease in fat mass at 10 mg/kg, po for 6 weeks by NMR-MRI analysis | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy. |
AID312506 | AUC (0-infinity) in Sprague-Dawley rat at 5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1574711 | Displacement of [3H]DOI from recombinant human 5HT2A receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2 | Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT |
AID1280453 | Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2 | Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. |
AID312505 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID594589 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as 5-HT-induced maximum response by inositol phosphate accumulation assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
AID1686095 | Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay relative to 5HT | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Design and Discovery of Functionally Selective Serotonin 2C (5-HT |
AID312503 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1199738 | Selectivity ratio of EC50 for human 5-HT2B receptor to EC50 for human 5HT2C receptor | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. |
AID312495 | Reduction of food intake in Sprague-Dawley rat at 12.5 umol/kg, po after 2 hrs relative to control | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID1656829 | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Discovery of a lead series of potent benzodiazepine 5-HT |
AID1623958 | Induction of anorexia in Sprague-Dawley rat assessed as suppression of food intake at 2 pmol, icv measured after 3 to 6 hrs | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT |
AID418830 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID1359253 | Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as reduction in body weight gain at 10 mg/kg, po for 6 weeks | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy. |
AID312510 | Selectivity ratio of pEC50 for human 5HT2A to pEC50 for human 5HT2C | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
AID418833 | Selectivity ratio of EC50 for human 5HT2A receptor to EC50 for human 5HT2C receptor | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. |
AID312494 | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | 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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 10 (3.76) | 29.6817 |
2010's | 211 (79.32) | 24.3611 |
2020's | 45 (16.92) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (63.28) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 39 (14.18%) | 5.53% |
Reviews | 70 (25.45%) | 6.00% |
Case Studies | 2 (0.73%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 164 (59.64%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |