"目录号: HY-15368
GPCR/G ProteinNeuronal Signaling-
Lorcaserin Hydrochloride 是一种具有选择性的人5-HT2C的完全激动剂，Ki值为 15 nM。
相关产品
Clozapine N-oxide-Chlorpromazine hydrochloride-Pimavanserin-Brexpiprazole-Scopolamine hydrobromide-Cariprazine hydrochloride-Harmine-Lu AE58054 Hydrochloride-TG6-10-1-Perphenazine-Aripiprazole-Ferulic acid sodium-Olanzapine-Sertindole-B-HT 920-
生物活性
Description
Lorcaserin (Hydrochloride) is a selective full agonist of human5-HT2Creceptor withKiof 15 nM.
IC50& Target
Ki: 15 nM (5-HT2C)
In Vitro
Lorcaserin is 18-fold more potent at human 5-HT2C(EC50= 9 nM) than at human 5-HT2A?(EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C?than human 5-HT2B(EC50= 943 nM)[1].
In Vivo
Lorcaserin decreases cumulative food intake at 2, 4, 6, and 22 h with a significant decrease continuing throughout the 22-h duration of the study at the highest dose (24 mg/kg) only. The reduction in food intake induced by lorcaserin (18 mg/kg, p.o.) is mediated by 5-HT2Cand not 5-HT2Areceptors. Lorcaserin significantly reduces active, and increased inactive counts, and increases the incidence of penile grooming, an effect mediated by the 5-HT2Creceptor[1]. Lorcaserin (20 mg/kg) doses causes a significant linear dose-related reduction in responses on the active lever but has no significant effect on the response to the inactive lever. Lorcaserin (0.3125, 0.625, 1.25, and 2.5 mg/kg) also produces a significant reduction in nicotine self-administration[2].
Clinical Trial
Arena Pharmaceuticals
Obesity
December 2004
Phase 2
Arena Pharmaceuticals
Obesity
June 2005
Phase 2
Eisai Co., Ltd.-Eisai Inc.
Healthy Subjects
July 2014
Phase 1
Arena Pharmaceuticals
Smoking Cessation
March 2014
Phase 2
Eisai Inc.-Thrombolysis In Myocardial Infarction (TIMI) Academic Research Organization
Cardiovascular Disease-High Cardiovascular Risk-Obesity-Overweight-Type 2 Diabetes
January 2014
Phase 4
Arena Pharmaceuticals
Obesity
December 2004
Phase 2
Arena Pharmaceuticals
Obesity
June 2005
Phase 2
Eisai Co., Ltd.-Eisai Inc.
Healthy Subjects
July 2014
Phase 1
Arena Pharmaceuticals
Smoking Cessation
March 2014
Phase 2
Eisai Inc.-Thrombolysis In Myocardial Infarction (TIMI) Academic Research Organization
Cardiovascular Disease-High Cardiovascular Risk-Obesity-Overweight-Type 2 Diabetes
January 2014
Phase 4
Eisai Inc.
Obesity
March 2015
Phase 1
Arena Pharmaceuticals
Obesity
October 2008
Phase 1
Arena Pharmaceuticals
Hepatic Impairment
August 2008
Phase 1
Arena Pharmaceuticals
Renal Impairment
October 2008
Phase 1
Southern California Institute for Research and Education
Weight Gain
January 2014
Phase 4
Arena Pharmaceuticals
Pharmacokinetics in Obese Adolescents
December 2013
Phase 1
Arena Pharmaceuticals
Obesity
November 2006
Phase 3
Mayo Clinic
Tobacco Use Disorder-Weight Gain
September 2013
Phase 1-Phase 2
Arena Pharmaceuticals
Obesity
January 2008
Phase 3
Arena Pharmaceuticals
Obesity
December 2007
Phase 3
National Institute on Drug Abuse (NIDA)
Cocaine-Related Disorders
June 19, 2017
Phase 2
Beth Israel Deaconess Medical Center
Obesity-Weight Loss
October 2014
Phase 4
University of North Carolina, Chapel Hill-Columbia University-National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Schizophrenia-Schizoaffective Disorder-Overweight
September 2016
Phase 4
University of California, San Francisco-National Institute on Drug Abuse (NIDA)
Cocaine Use Disorder
August 2017
Phase 2
Arena Pharmaceuticals
Obesity
November 2008
Phase 1
Duke University-National Institute on Drug Abuse (NIDA)
Nicotine Dependence
November 8, 2016
Phase 2
New York State Psychiatric Institute
Cannabis Use Disorder
October 2016
Phase 1
Mayo Clinic
Overweight-Obese
June 2014
Phase 3
Arena Pharmaceuticals
Obesity
November 2008
Phase 1
Midwest Biomedical Research Foundation
Cocaine Use Disorders
November 2015
Phase 1-Phase 2
Eisai Inc.
Chronic Weight Management
October 2013
Phase 4
New York State Psychiatric Institute
Opioid-use Disorder
May 25, 2017
Phase 2-Phase 3
Arena Pharmaceuticals
Drug Abuse-Healthy
December 2008
Phase 1
National Institute on Drug Abuse (NIDA)
Cocaine Abuse
May 2015
Phase 1
University of Pennsylvania-Eisai Inc.
Obesity
January 2015
Mayo Clinic-National Institute on Drug Abuse (NIDA)
Obesity-Smoking Cessation
June 2016
Phase 2-Phase 3
Virginia Commonwealth University
Cocaine-Related Disorders-Opioid-Related Disorders
July 2015
Phase 1
Johns Hopkins University
Muscle Weakness-Sepsis
September 2015
Phase 1-Phase 2
Virginia Commonwealth University-National Institute on Drug Abuse (NIDA)
Cocaine Use Disorder
July 2015
Phase 1
Virginia Commonwealth University-National Institute on Drug Abuse (NIDA)
Opioid Abuse-Opioid Dependence-Opioid-Related Disorders-Opioid Use
January 30, 2017
Phase 1
Duke University-National Heart, Lung, and Blood Institute (NHLBI)
Cardiovascular Diseases
January 2018
Phase 1
View MoreCollapse
References
