Page last updated: 2024-11-12

lorcaserin

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Description

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]

Cross-References

ID SourceID
PubMed CID11658860
CHEMBL ID360328
CHEBI ID65353
SCHEMBL ID169382
MeSH IDM0520419

Synonyms (43)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"Lorcaserin is a modestly selective agonist for 2C serotonin receptors (5-HT2CR). "( 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
)
2.42
"Lorcaserin is a selective serotonin 2c receptor agonist approved as an anti-obesity agent. "( Effects of lorcaserin on cardiometabolic risk factors in overweight and obese patients: A systematic review and meta-analysis.
Kuo, HH; Lee, YH; Lin, CY; Lin, PL; Liu, LY; Liu, ME; Wang, KT, 2020
)
2.39
"Lorcaserin is a serotonin 5-HT"( Adjunctive effect of the serotonin 5-HT
Dewey, WL; González-Maeso, J; Lippold, KM; Poklis, JL; Sierra, S; Stevens, DL, 2020
)
1.28
"Lorcaserin is an anti-obesity drug whose weight loss effect results from 5-hydroxytryptamin (5-HT)"( Lorcaserin Administration has Pro-Ejaculatory Effects in Rats via 5-HT
Antunes, E; de Almeida Kiguti, LR; Kempinas, WG; Pacheco, TL, 2020
)
3.44
"Lorcaserin is a serotonin 2C receptor antagonist that was FDA approved in 2012. "( Pharmacokinetic drug evaluation of extended release lorcaserin for the treatment of obesity.
Dunham, MW; Hurren, KM, 2017
)
2.15
"Lorcaserin is a serotonin 2c receptor agonist that promotes weight loss while contributing to the prevention and improvement of type 2 diabetes and improvement of atherogenic lipid profiles, without higher rates of major cardiovascular events. "( Lorcaserin treatment decreases body weight and reduces cardiometabolic risk factors in obese adults: A six-month, randomized, placebo-controlled, double-blind clinical trial.
Farr, OM; Kelesidis, T; Koniaris, A; Mantzoros, CS; Mathew, H; Oussaada, SM; Paschou, SA; Perakakis, N; Tuccinardi, D; Upadhyay, J, 2019
)
3.4
"Lorcaserin is a modestly selective agonist for 2C serotonin receptors (5-HT"( The serotonin-2C agonist Lorcaserin delays intravenous choice and modifies the subjective and cardiovascular effects of cocaine: A randomized, controlled human laboratory study.
Boinpelly, VC; Grasing, KW; Hickman, MD; Pirtle, JL; Surineni, K; Thakur, HK, 2019
)
2.26
"Lorcaserin HCl is a novel, synthetic, centrally-acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients."( Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics Aspects of Lorcaserin, a Selective Serotonin 5-HT2C Receptor Agonist: An Update.
Aware, KS; Hatware, K; Patil, K; Sharma, S, 2020
)
1.51
"Lorcaserin is a selective 5-hydroxytryptamine 2C agonist which exerts robust benefits on long-term weight loss by suppressing appetite among adults with overweight or obesity."( Lorcaserin for prevention and remission of type 2 diabetes mellitus in people with overweight or obesity: protocol for a systematic review and meta-analysis.
Fu, W; He, G; Jin, Y; Li, Z; Luo, M; Wen, J; Zeng, H; Zhou, P, 2019
)
2.68
"Lorcaserin is a selective 5-HT2C agonist evaluated for weight management in clinical trials. "( Echocardiographic assessment of cardiac valvular regurgitation with lorcaserin from analysis of 3 phase 3 clinical trials.
Anderson, CM; Koch, GG; Sanchez, M; Shanahan, WR; Smith, SR; Weissman, NJ, 2013
)
2.07
"Lorcaserin is a selective serotonin 5-HT2C agonist that regulates food intake, while the combination of phentermine/topiramate causes appetite suppression and enhanced satiety."( New obesity agents: lorcaserin and phentermine/topiramate.
Fleming, JW; McClendon, KS; Riche, DM,
)
1.18
"Lorcaserin is a centrally acting, selective serotonin C (5-HT2C) receptor full agonist that is associated with increased satiety and decreased food consumption in patients."( The safety and efficacy of lorcaserin in the management of obesity.
Cross, LB; Hess, R, 2013
)
1.41
"Lorcaserin is a serotonin agonist, whereas phentermine/topiramate is a combination of a sympathomimetic agent and an antiepileptic drug; both these agents have been shown to reduce weight significantly and improve cardiovascular and metabolic parameters, such as blood pressure, lipids, and HbA1C."( New antiobesity agents: lorcaserin (Belviq) and phentermine/topiramate ER (Qsymia).
Cheng-Lai, A; Shyh, G,
)
1.16
"Lorcaserin is a novel serotonin 5-HT2C selective agonist which has been shown in three phase III studies to significantly reduce weight and cardiovascular risk factors such as diabetes."( New pharmacological treatments for the management of obesity.
Ebbert, JO; Edakkanambeth Varayil, J; Hurt, RT, 2014
)
1.12
"Lorcaserin is a serotonergic agonist specific to the 5HT- 2C receptor approved for chronic management of obesity in patients with a BMI ≥ 30 kg/m(2) or a BMI ≥ 27 kg/m(2) with comorbidities related to obesity."( Lorcaserin Hcl for the treatment of obesity.
Aronne, LJ; Kumar, RB; Shukla, AP, 2015
)
2.58
"Lorcaserin is a unique highly selective serotonergic agonist designed to mitigate the risks associated with previous agents in this class. "( Lorcaserin Hcl for the treatment of obesity.
Aronne, LJ; Kumar, RB; Shukla, AP, 2015
)
3.3
"Lorcaserin is a novel, potent and highly efficacious 5-HT2C receptor agonist, recently approved by US Food and Drug Administration for the treatment of obesity. "( A Validated UPLC-MS-MS Assay for the Rapid Determination of Lorcaserin in Plasma and Brain Tissue Samples.
Al-Rashood, KA; Bajrai, AA; Ezzeldin, E; Iqbal, M; Raish, M, 2016
)
2.12
"Lorcaserin is a selective 5-HT2C (5-hydroxytryptamine 2C) receptor agonist indicated for weight management. "( Evaluation of lorcaserin on progression of prediabetes to type 2 diabetes and reversion to euglycemia.
Fain, R; Li, Y; Nesto, R; Shanahan, W, 2016
)
2.24
"Lorcaserin is a selective serotonin 2C receptor (5-HT2C) agonist approved in the United States for use in chronic weight management as an adjunct to a reduced-calorie diet and increased physical activity. "( Lorcaserin in Obese and Overweight Patients Taking Prohibited Serotonergic Agents: A Retrospective Analysis.
Fain, R; Nguyen, CT; Shanahan, W; Zhou, S, 2016
)
3.32
"Lorcaserin is a serotonin 5-hydroxytryptamine 2c receptor agonist effective in treating obesity. "( Lorcaserin Administration Decreases Activation of Brain Centers in Response to Food Cues and These Emotion- and Salience-Related Changes Correlate With Weight Loss Effects: A 4-Week-Long Randomized, Placebo-Controlled, Double-Blind Clinical Trial.
Camp, M; Farr, OM; Gavrieli, A; Kaye, H; Kilim, H; Koniaris, A; Mantzoros, CS; Mathew, H; Migdal, A; Spyrou, N; Srnka, A; Upadhyay, J; Vamvini, M, 2016
)
3.32
"Lorcaserin is a novel selective serotonin 2C receptor agonist indicated by the US Food and Drug Administration for chronic weight management in adults with obesity or overweight with ≥1 comorbidity. "( Safety and tolerability review of lorcaserin in clinical trials.
Fain, R; Greenway, FL; Ma, T; Rubino, D; Shanahan, W, 2016
)
2.16
"Lorcaserin is a serotonin 2C receptor agonist approved for chronic weight management. "( Lorcaserin treatment allows for decreased number needed to treat for weight and glycemic parameters in week 12 responders with ≥5% weight loss.
Fain, R; Fujioka, K; Handelsman, Y; Li, X; Shanahan, W; Wang, Z, 2016
)
3.32
"Lorcaserin is a selective serotonin 2C receptor agonist approved by the Food and Drug Administration for chronic weight management. "( Lorcaserin for Smoking Cessation and Associated Weight Gain: A Randomized 12-Week Clinical Trial.
Glicklich, A; Rose, JE; Sanchez-Kam, M; Shanahan, WR; Stubbe, S, 2017
)
3.34
"Lorcaserin is an FDA-approved medication for weight management in overweight or obese patients which also provides a noticeable benefit in treating drug dependence."( Combination Varenicline and Lorcaserin for Tobacco Dependence Treatment and Weight Gain Prevention in Overweight and Obese Smokers: A Pilot Study.
Choi, DS; Croghan, IT; Ebbert, JO; Hays, JT; Hurt, RT; Schroeder, DR, 2017
)
1.47
"Lorcaserin (APD356) is a potent, selective 5-HT(2C) agonist with ~15-fold and 100-fold selectivity vs. "( Lorcaserin (APD356), a selective 5-HT(2C) agonist, reduces body weight in obese men and women.
Anderson, CM; Donahue, DJ; Morgan, ME; Prosser, WA; Shanahan, WR; Smith, SR, 2009
)
3.24
"Lorcaserin (APD-356) is a selective 5-HT2c receptor agonist that promotes weight loss."( Lorcaserin and adiposopathy: 5-HT2c agonism as a treatment for 'sick fat' and metabolic disease.
Bays, HE, 2009
)
2.52
"Lorcaserin is a selective serotonin 2C receptor agonist that could be useful in reducing body weight."( Multicenter, placebo-controlled trial of lorcaserin for weight management.
Anderson, CM; Bays, H; Chuang, E; Sanchez, M; Shanahan, WR; Smith, SR; Stubbe, S; Weissman, NJ, 2010
)
2.07
"Lorcaserin is a selective and potent serotonin 2C receptor subtype (5-HT(2C)) agonist under development for the treatment of obesity. "( Evaluation of the abuse potential of lorcaserin, a serotonin 2C (5-HT2C) receptor agonist, in recreational polydrug users.
Anderson, CM; Bartlett, C; Schoedel, KA; Sellers, EM; Shazer, RL; Shram, MJ, 2011
)
2.08
"Lorcaserin is a selective 5-hydroxytryptamine receptor 2c agonist developed as a weight-loss drug. "( Lorcaserin: drug profile and illustrative model of the regulatory challenges of weight-loss drug development.
Bays, HE, 2011
)
3.25
"Lorcaserin is a novel selective agonist of the 5-HT(2C) receptor for weight loss therapy."( Lorcaserin for the treatment of obesity.
Ravussin, E; Redman, LM, 2010
)
2.52
"Lorcaserin is a novel selective agonist of the serotonin 2C receptor."( A one-year randomized trial of lorcaserin for weight loss in obese and overweight adults: the BLOSSOM trial.
Anderson, CM; Fidler, MC; Raether, B; Sanchez, M; Shanahan, WR; Smith, SR; Weissman, NJ, 2011
)
2.1
"Lorcaserin is a new anti-obesity drug recently approved by US Food and Drug Administration. "( Efficacy and safety of lorcaserin in obese adults: a meta-analysis of 1-year randomized controlled trials (RCTs) and narrative review on short-term RCTs.
Chan, EW; Chui, CS; He, Y; Lau, WC; Wong, AY; Wong, IC, 2013
)
2.14

Effects

ExcerptReferenceRelevance
"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

Treatment

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.

ExcerptReferenceRelevance
"Lorcaserin treatment significantly improves HRQOL compared with placebo."( Health-related quality of life in randomized controlled trials of lorcaserin for obesity management: what mediates improvement?
Crosby, RD; Kolotkin, RL; Wang, Z, 2017
)
1.41
"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
)
2.64
"Lorcaserin treatment reduced fat mass (P < 0.001), the fatty liver index (P < 0.0001) and energy intake (P < 0.03) without affecting energy expenditure or lean mass."( Lorcaserin treatment decreases body weight and reduces cardiometabolic risk factors in obese adults: A six-month, randomized, placebo-controlled, double-blind clinical trial.
Farr, OM; Kelesidis, T; Koniaris, A; Mantzoros, CS; Mathew, H; Oussaada, SM; Paschou, SA; Perakakis, N; Tuccinardi, D; Upadhyay, J, 2019
)
2.68
"Lorcaserin-treated patients had a rate of FDA-defined valvulopathy similar to placebo."( Safety and efficacy of lorcaserin: a combined analysis of the BLOOM and BLOSSOM trials.
Aronne, L; Fain, R; Glicklich, A; Li, Y; Shanahan, W; Smith, S; Soliman, W, 2014
)
1.43
"Pretreatment of lorcaserin, or the positive control clonidine (an alpha 2-adrenoceptor agonist), ameliorated the naloxone-precipitated withdrawal symptoms."( Activation of serotonin 5-HT(2C) receptor suppresses behavioral sensitization and naloxone-precipitated withdrawal symptoms in morphine-dependent mice.
Dong, L; Jiang, Q; Liu, H; Pang, G; Stackman, RW; Tao, X; Wu, X; Zhang, G; Zhang, YM, 2016
)
0.77

Toxicity

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.

ExcerptReferenceRelevance
" The secondary aims were to evaluate the side effect profiles of lorcaserin and CP-809101 and to determine the plasma levels of lorcaserin at a dose (1 mg/kg) that reduces both food and nicotine reinforcement for comparison to plasma concentrations reported in human trials."( Evaluation of chemically diverse 5-HT₂c receptor agonists on behaviours motivated by food and nicotine and on side effect profiles.
Coen, K; de Lannoy, IA; Fletcher, PJ; Higgins, GA; Izhakova, J; Lau, W; Le, AD; Lee, DK; Silenieks, LB, 2013
)
0.63
" Finally, there may be differences in the side effect profiles between lorcaserin and CP-809101, raising the possibility for tolerability differences amongst 5-HT2C agonists."( Evaluation of chemically diverse 5-HT₂c receptor agonists on behaviours motivated by food and nicotine and on side effect profiles.
Coen, K; de Lannoy, IA; Fletcher, PJ; Higgins, GA; Izhakova, J; Lau, W; Le, AD; Lee, DK; Silenieks, LB, 2013
)
0.62
" We conducted a systematic review and meta-analysis of randomized controlled trials (RCTs) to evaluate the association of lorcaserin therapy with weight loss and adverse events in obese adults (18-65 years old)."( Efficacy and safety of lorcaserin in obese adults: a meta-analysis of 1-year randomized controlled trials (RCTs) and narrative review on short-term RCTs.
Chan, EW; Chui, CS; He, Y; Lau, WC; Wong, AY; Wong, IC, 2013
)
0.91
" 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."( The safety and efficacy of lorcaserin in the management of obesity.
Cross, LB; Hess, R, 2013
)
1.01
" However, in the existing studies PHEN/TPM ER had a superior weight loss profile to lorcaserin but the incidence of adverse effects was lower with lorcaserin."( Tolerability and safety of the new anti-obesity medications.
Aldhoon-Hainerová, I; Hainer, V, 2014
)
0.63
" The most common adverse events associated with lorcaserin treatment were headache, upper respiratory tract infection, and nasopharyngitis."( Safety and efficacy of lorcaserin: a combined analysis of the BLOOM and BLOSSOM trials.
Aronne, L; Fain, R; Glicklich, A; Li, Y; Shanahan, W; Smith, S; Soliman, W, 2014
)
0.97
"This pooled analysis of the phase III BLOOM and BLOSSOM trials shows that lorcaserin 10 mg twice daily, in combination with diet and exercise, is safe and tolerable, and is associated with statistically significant weight loss and clinically relevant improvements in cardiometabolic parameters."( Safety and efficacy of lorcaserin: a combined analysis of the BLOOM and BLOSSOM trials.
Aronne, L; Fain, R; Glicklich, A; Li, Y; Shanahan, W; Smith, S; Soliman, W, 2014
)
0.94
" Thus, if following the appropriate guidelines according to package labels, the practitioner can feel safe in prescribing these medications."( Safety and tolerability of medications approved for chronic weight management.
Fujioka, K, 2015
)
0.42
"To compare weight loss and adverse events among drug treatments for obesity using a systematic review and network meta-analysis."( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis.
Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016
)
0.43
"Proportions of patients with at least 5% weight loss and at least 10% weight loss, magnitude of decrease in weight, and discontinuation of therapy because of adverse events at 1 year."( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis.
Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016
)
0.43
"35) were associated with the highest odds of adverse event-related treatment discontinuation."( Association of Pharmacological Treatments for Obesity With Weight Loss and Adverse Events: A Systematic Review and Meta-analysis.
Camilleri, M; Chandar, AK; Dulai, PS; Khera, R; Loomba, R; Murad, MH; Prokop, LJ; Singh, S; Wang, Z, 2016
)
0.43
" Headache was the most common adverse event experienced by patients during all Phase III trials."( Safety and tolerability review of lorcaserin in clinical trials.
Fain, R; Greenway, FL; Ma, T; Rubino, D; Shanahan, W, 2016
)
0.71
" Patients reporting ≥ 1 of 9 potentially serotonergic adverse events (AEs), mean weight loss (WL), and ≥5% WL are reported."( Coadministration of lorcaserin and phentermine for weight management: A 12-week, randomized, pilot safety study.
Aronne, LJ; Fain, R; Fujioka, K; Garvey, WT; Greenway, FL; Pilson, R; Smith, SR; Zhou, S, 2017
)
0.78
" Adverse events of special interest were uncommon, and the rates were generally similar in the two groups, except for a higher number of patients with serious hypoglycemia in the lorcaserin group (13 vs."( Cardiovascular Safety of Lorcaserin in Overweight or Obese Patients.
Bohula, EA; Bonaca, MP; Brown, C; Budaj, A; Dhadda, S; Fanola, CL; Francis, B; Garcia-Castillo, A; Gupta, M; Im, K; Inzucchi, SE; Keech, AC; Kuder, J; Leiter, LA; McGuire, DK; Miao, W; Patel, T; Perdomo, C; Qamar, A; Ruff, CT; Sabatine, MS; Scirica, BM; Smith, SR; Weissman, NJ; White, HD; Wiviott, SD, 2018
)
0.98
"Over the past several decades, many antiobesity drugs have been withdrawn from the market due to unanticipated adverse events, often involving cardiotoxicity."( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database.
Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020
)
0.56
"We used the US Food and Drug Administration Adverse Event Reporting System (FAERS) database and retrieved data from January 2013 through December 2018."( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database.
Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020
)
0.56
"During the evaluated period, a total of 6,787,840 adverse event reports were submitted to FAERS."( The cardiovascular safety of antiobesity drugs-analysis of signals in the FDA Adverse Event Report System Database.
Gorelik, B; Gorelik, E; Hirsh-Raccah, B; Masarwa, R; Matok, I; Perlman, A, 2020
)
0.56
" However, they are costly and may have adverse effects in some individuals."( Long-Term Efficacy and Safety of Anti-Obesity Treatment: Where Do We Stand?
Lee, SY; Tak, YJ, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" 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

Compound-Compound Interactions

ExcerptReferenceRelevance
"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

Bioavailability

ExcerptReferenceRelevance
"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

Dosage Studied

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.

ExcerptRelevanceReference
" 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
appetite depressantAgent that is used to decrease appetite.
anti-obesity agentAny 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]

Drug Classes (2)

ClassDescription
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
benzazepineA 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 Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.09010.01237.983543.2770AID1645841
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.80610.000229.305416,493.5996AID743069; AID743075
cytochrome P450 2D6Homo sapiens (human)Potency1.94970.00108.379861.1304AID1645840
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency23.70830.000627.21521,122.0200AID743202
Cellular tumor antigen p53Homo sapiens (human)Potency11.88320.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki10.00000.00031.465610.0000AID418839
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.62120.00000.385510.0000AID1512840; AID1574711; AID1656832; AID418835; AID731446
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.07130.00010.954910.0000AID1512839; AID1574713; AID1656833; AID418837; AID594581; AID594585; AID780300
Sodium-dependent serotonin transporterHomo sapiens (human)Ki2.60600.00000.70488.1930AID418838
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.15170.00030.769310.0000AID1512841; AID1574712; AID1656829; AID418836; AID731445
Sodium-dependent dopamine transporter Homo sapiens (human)Ki10.00000.00021.11158.0280AID418840
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)EC50 (µMol)0.03990.00030.20692.0000AID1446073
Cytochrome P450 3A4Homo sapiens (human)EC50 (µMol)0.03990.00010.23283.2000AID1446073
5-hydroxytryptamine receptor 2AHomo sapiens (human)EC50 (µMol)0.35870.00000.22763.4750AID1199735; AID1280456; AID1446071; AID1565294; AID1656830; AID1686087; AID246590; AID312492; AID418828
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC50 (µMol)0.02220.00010.10082.4500AID1199729; AID1280452; AID1446067; AID1446073; AID1565288; AID1656835; AID1686079; AID1686091; AID1686094; AID246589; AID312493; AID418831; AID594578; AID594586; AID731447
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC50 (µMol)0.50830.00040.20611.0000AID1199721; AID1199732; AID1280454; AID1446069; AID1565291; AID1686083; AID246591; AID312494; AID418829; AID594588
5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)EC50 (µMol)0.01620.01080.01350.0162AID594742
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (273)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
monoamine transportSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent dopamine transporter Homo sapiens (human)
lactationSodium-dependent dopamine transporter Homo sapiens (human)
sensory perception of smellSodium-dependent dopamine transporter Homo sapiens (human)
locomotory behaviorSodium-dependent dopamine transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent dopamine transporter Homo sapiens (human)
response to iron ionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine transportSodium-dependent dopamine transporter Homo sapiens (human)
adenohypophysis developmentSodium-dependent dopamine transporter Homo sapiens (human)
response to nicotineSodium-dependent dopamine transporter Homo sapiens (human)
positive regulation of multicellular organism growthSodium-dependent dopamine transporter Homo sapiens (human)
regulation of dopamine metabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to cocaineSodium-dependent dopamine transporter Homo sapiens (human)
dopamine biosynthetic processSodium-dependent dopamine transporter Homo sapiens (human)
dopamine catabolic processSodium-dependent dopamine transporter Homo sapiens (human)
response to ethanolSodium-dependent dopamine transporter Homo sapiens (human)
cognitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent dopamine transporter Homo sapiens (human)
response to cAMPSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
prepulse inhibitionSodium-dependent dopamine transporter Homo sapiens (human)
dopamine uptakeSodium-dependent dopamine transporter Homo sapiens (human)
hyaloid vascular plexus regressionSodium-dependent dopamine transporter Homo sapiens (human)
amino acid transportSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine transportSodium-dependent dopamine transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent dopamine transporter Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
locomotory behavior5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
feeding behavior5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
regulation of nervous system process5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
regulation of appetite5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (91)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protease bindingSodium-dependent dopamine transporter Homo sapiens (human)
signaling receptor bindingSodium-dependent dopamine transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
protein bindingSodium-dependent dopamine transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent dopamine transporter Homo sapiens (human)
dopamine bindingSodium-dependent dopamine transporter Homo sapiens (human)
amine bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein-containing complex bindingSodium-dependent dopamine transporter Homo sapiens (human)
metal ion bindingSodium-dependent dopamine transporter Homo sapiens (human)
protein phosphatase 2A bindingSodium-dependent dopamine transporter Homo sapiens (human)
heterocyclic compound bindingSodium-dependent dopamine transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent dopamine transporter Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (47)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasmSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
cell surfaceSodium-dependent dopamine transporter Homo sapiens (human)
membraneSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
neuron projectionSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell bodySodium-dependent dopamine transporter Homo sapiens (human)
axon terminusSodium-dependent dopamine transporter Homo sapiens (human)
membrane raftSodium-dependent dopamine transporter Homo sapiens (human)
postsynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
dopaminergic synapseSodium-dependent dopamine transporter Homo sapiens (human)
flotillin complexSodium-dependent dopamine transporter Homo sapiens (human)
axonSodium-dependent dopamine transporter Homo sapiens (human)
presynaptic membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membraneSodium-dependent dopamine transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent dopamine transporter Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
synapse5-hydroxytryptamine receptor 2CCanis lupus familiaris (dog)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (182)

Assay IDTitleYearJournalArticle
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID624219Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B2008The 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.
AID624235Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A2008The 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.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2008The 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.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2008The 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.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)2008The 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.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2008The 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.
AID1199732Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2015Journal 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.
AID1512842Selectivity ratio of Ki for 5-HT2AR (unknown origin) to Ki for 5-HT2CR (unknown origin)2019Journal 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
AID731445Agonist activity at 5-HT2B receptor (unknown origin)2013Bioorganic & 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.
AID1656881Selectivity 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]-12020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1686097Bias 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1446071Agonist 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 assay2017Journal 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.
AID418834Selectivity ratio of EC50 for human 5HT2B receptor to EC50 for human 5HT2C receptor2009Journal 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.
AID594588Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay2011Bioorganic & 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.
AID1446069Agonist 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 assay2017Journal 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.
AID731446Agonist activity at 5-HT2A receptor (unknown origin)2013Bioorganic & 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.
AID1446073Agonist 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 assay2017Journal 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.
AID1686087Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1686083Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID594578Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay2011Bioorganic & 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.
AID1199739Selectivity ratio of EC50 for human 5-HT2A receptor to EC50 for human 5HT2C receptor2015Journal 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.
AID312493Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal 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.
AID312497Reduction of food intake in Sprague-Dawley rat at 50 umol/kg, po after 2 hrs relative to control2008Journal 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.
AID1686079Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID312512Reduction of body weight in Sprague-Dawley rat at 18 mg/kg, po, qd after 28 days relative to control2008Journal 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.
AID312496Reduction of food intake in Sprague-Dawley rat at 25 umol/kg, po after 2 hrs relative to control2008Journal 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.
AID1686089Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID780316Selectivity ratio of Ki for 5-HT2A receptor (unknown origin) to Ki for 5-HT2C receptor (unknown origin)2013Bioorganic & 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.
AID1446094Agonist 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 serotonin2017Journal 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.
AID1574713Displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT
AID1686088Agonist 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-HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1359193Anorexic 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 hrs2018European journal of medicinal chemistry, May-25, Volume: 152Identification of novel β-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents.
AID1446075Ratio of Emax to EC50 for human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells2017Journal 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.
AID418832Agonist activity at human 5HT2C receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin2009Journal 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.
AID252842Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2C receptor in HEK293 cells2005Bioorganic & 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.
AID594583Agonist 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 control2011Bioorganic & 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.
AID418836Displacement of [3H]LSD from human 5HT2B receptor2009Journal 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.
AID418831Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2009Journal 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.
AID312500Half life in Sprague-Dawley rat at 5 mg/kg, iv2008Journal 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.
AID312511Selectivity ratio of pEC50 for human 5HT2B to pEC50 for human 5HT2C2008Journal 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.
AID1280452Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay2016Journal 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.
AID418839Displacement of [3H]nisoxetine from NET2009Journal 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.
AID312509Reduction of body weight in Sprague-Dawley rat at 36 mg/kg, po, bid after 28 days relative to control2008Journal 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.
AID1512843Selectivity ratio of Ki for 5-HT2BR (unknown origin) to Ki for 5-HT2CR (unknown origin)2019Journal 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
AID252843Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2A receptor in HEK293 cells2005Bioorganic & 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.
AID1199721Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis2015Journal 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.
AID312513Reduction of body weight in Sprague-Dawley rat at 9 mg/kg, po, bid after 28 days relative to control2008Journal 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.
AID1280456Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay2016Journal 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.
AID780300Binding affinity to 5-HT2C receptor (unknown origin)2013Bioorganic & 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.
AID594581Displacement of [3H]meselurgine from human 5HT2C receptor expressed in Swiss mouse 3T3 cells by scintillation proximity assay2011Bioorganic & 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.
AID312508Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2008Journal 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.
AID1656828Agonist activity at 5HT2B receptor (unknown origin) relative to control2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1565288Agonist 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID1595986Anti-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 analysis2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
AID1280455Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2016Journal 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.
AID1656830Partial agonist activity at 5HT2A receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1686092Agonist 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-HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1686098Bias 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID594587Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as 5-HT-induced maximum response by inositol phosphate accumulation assay2011Bioorganic & 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.
AID1686084Agonist 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-HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1686094Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1686081Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1656832Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2A receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1446067Agonist 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 assay2017Journal 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.
AID780317Selectivity ratio of Ki for 5-HT2B receptor (unknown origin) to Ki for 5-HT2C receptor (unknown origin)2013Bioorganic & 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.
AID312502Clearance in Sprague-Dawley rat at 5 mg/kg, iv2008Journal 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.
AID418828Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2009Journal 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.
AID1656836Agonist 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 control2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID418837Displacement of [3H]mesulergine from 5HT2C receptor2009Journal 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.
AID1595982Anti-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)2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
AID246591Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release2005Bioorganic & 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.
AID312514Reduction of body weight in Sprague-Dawley rat at 18 mg/kg, po, bid after 28 days relative to control2008Journal 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.
AID1565292Agonist 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 control2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID312501Half life in Sprague-Dawley rat at 10 mg/kg, po2008Journal 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.
AID1686096Agonist 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 5HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1565294Agonist 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID1574712Displacement of [3H]DOI from recombinant human 5HT2B receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT
AID1574714Selectivity 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 membranes2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT
AID594585Displacement of [125I]DOI from human recombinant 5HT2C receptor expressed in HEK293 cells by scintillation counting2011Bioorganic & 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.
AID1446098Agonist 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 2017Journal 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.
AID418827Agonist activity at human 5HT2A receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin2009Journal 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.
AID1656833Displacement 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 method2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1595969Anorexic 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 control2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
AID1199736Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2015Journal 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.
AID1656835Agonist 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 method2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1199720Selectivity for human recombinant 5HT2C receptor over human recombinant 5HT2B receptor2015Journal 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.
AID1280457Agonist activity at human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2016Journal 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.
AID418840Displacement of [3H]WIN-35428 from DAT2009Journal 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.
AID1686091Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1446081Toxicity in C57BL/6J mouse assessed as reduction in baseline locomotive activity at 3 mg/kg, ip after 15 mins2017Journal 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.
AID418835Displacement of [3H]ketanserin from human 5HT2A receptor2009Journal 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.
AID594580Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay relative to control2011Bioorganic & 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.
AID1512840Agonist activity at 5-HT2AR (unknown origin)2019Journal 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
AID1199730Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2015Journal 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.
AID1565295Agonist 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 control2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID252844Percentage maximum response relative to serotonin towards 5-hydroxytryptamine 2B receptor in HEK293 cells2005Bioorganic & 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.
AID1574715Selectivity 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 membranes2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT
AID1280454Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay2016Journal 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.
AID1686085Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID312499Reduction of food intake in Sprague-Dawley rat after 6 hrs relative to control2008Journal 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.
AID312504Tmax in Sprague-Dawley rat at 10 mg/kg, po2008Journal 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.
AID418842Selectivity ratio of Ki for human 5HT2B receptor to Ki for 5HT2C receptor2009Journal 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.
AID594742Agonist activity at dog 5HT2C receptor2011Bioorganic & 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.
AID731447Agonist activity at 5-HT2C receptor (unknown origin)2013Bioorganic & 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.
AID594586Agonist activity at human 5HT2C receptor expressed in HEK293 cells by inositol phosphate accumulation assay2011Bioorganic & 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.
AID1686093Agonist 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 assay2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1595979Anti-obesity activity in high fat diet-induced obese C57BL/6J mouse model assessed as reduction in body weight at 10 mg/kg, po2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
AID418841Selectivity ratio of Ki for human 5HT2A receptor to Ki for 5HT2C receptor2009Journal 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.
AID312507AUC (0-infinity) in Sprague-Dawley rat at 10 mg/kg, po2008Journal 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.
AID1446096Agonist 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 serotonin2017Journal 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.
AID1446095Agonist 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 serotonin2017Journal 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.
AID1446076Ratio 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 activity2017Journal 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.
AID312498Reduction of food intake in Sprague-Dawley rat at 100 umol/kg, po after 2 hrs relative to control2008Journal 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.
AID246589Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release2005Bioorganic & 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.
AID1686080Agonist 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-HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID1512839Agonist activity at 5-HT2CR (unknown origin)2019Journal 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
AID1446086Antipsychotic 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 mins2017Journal 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.
AID1199733Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2015Journal 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.
AID1199722Agonist 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-HT2015Journal 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.
AID1446083Antipsychotic 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 mins2017Journal 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.
AID1199735Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2015Journal 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.
AID1656876Selectivity 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]-12020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID246590Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release2005Bioorganic & 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.
AID418829Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2009Journal 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.
AID312492Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal 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.
AID1512841Agonist activity at 5-HT2BR (unknown origin)2019Journal 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
AID1565291Agonist 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID418838Displacement of [3H]citalopram from SERT2009Journal 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.
AID1565289Agonist 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 control2019European journal of medicinal chemistry, Nov-15, Volume: 182Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT
AID1656831Partial agonist activity at 5HT2A receptor (unknown origin) relative to control2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID594743Agonist activity at dog 5HT2C receptor ralative to control2011Bioorganic & 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.
AID1199729Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay2015Journal 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.
AID1359256Anti-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 analysis2018European journal of medicinal chemistry, May-25, Volume: 152Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy.
AID312506AUC (0-infinity) in Sprague-Dawley rat at 5 mg/kg, iv2008Journal 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.
AID1574711Displacement of [3H]DOI from recombinant human 5HT2A receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT
AID1280453Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay relative to 5-HT2016Journal 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.
AID312505Cmax in Sprague-Dawley rat at 10 mg/kg, po2008Journal 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.
AID594589Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as 5-HT-induced maximum response by inositol phosphate accumulation assay2011Bioorganic & 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.
AID1686095Agonist 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 5HT2016Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
Design and Discovery of Functionally Selective Serotonin 2C (5-HT
AID312503Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv2008Journal 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.
AID1199738Selectivity ratio of EC50 for human 5-HT2B receptor to EC50 for human 5HT2C receptor2015Journal 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.
AID312495Reduction of food intake in Sprague-Dawley rat at 12.5 umol/kg, po after 2 hrs relative to control2008Journal 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.
AID1656829Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin)2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Discovery of a lead series of potent benzodiazepine 5-HT
AID1623958Induction of anorexia in Sprague-Dawley rat assessed as suppression of food intake at 2 pmol, icv measured after 3 to 6 hrs2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT
AID418830Agonist activity at human 5HT2B receptor expressed in HEK293 cells at 10 uM assessed as calcium flux by FLIPR assay relative to serotonin2009Journal 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.
AID1359253Anti-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 weeks2018European journal of medicinal chemistry, May-25, Volume: 152Discovery of coumarin-dihydroquinazolinone analogs as niacin receptor 1 agonist with in-vivo anti-obesity efficacy.
AID312510Selectivity ratio of pEC50 for human 5HT2A to pEC50 for human 5HT2C2008Journal 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.
AID418833Selectivity ratio of EC50 for human 5HT2A receptor to EC50 for human 5HT2C receptor2009Journal 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.
AID312494Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal 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]

Research

Studies (266)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (3.76)29.6817
2010's211 (79.32)24.3611
2020's45 (16.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 63.28

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.

MetricThis Compound (vs All)
Research Demand Index63.28 (24.57)
Research Supply Index5.75 (2.92)
Research Growth Index5.65 (4.65)
Search Engine Demand Index106.87 (26.88)
Search Engine Supply Index2.03 (0.95)

This Compound (63.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials39 (14.18%)5.53%
Reviews70 (25.45%)6.00%
Case Studies2 (0.73%)4.05%
Observational0 (0.00%)0.25%
Other164 (59.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]