"目录号: HY-15296
Neuronal SignalingGPCR/G ProteinAutophagy-
Cabergoline 是一种麦角衍生的多巴胺 D2亚类受体激动剂，高亲和力作用于D2，D3和5-HT2B受体，Ki分别为 0.7，1.5 和 1.2。
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生物活性
Description
Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity forD2,D3, and5-HT2Breceptors (Ki=0.7, 1.5, and 1.2, respectively).
IC50& Target
Ki: 0.7 (Dopamine D2receptor), 1.5 (Dopamine D3receptor), 1.2 (5-HT2Breceptor)[1]
In Vitro
Cabergoline acts as a potent agonist of D2, D3and 5-HT2Breceptors. Pretreatment with Cabergoline inhibits H2O2-induced neuronal cell death in a dose-dependent manner. In the following experiments, 10 μM of Cabergoline is used to investigate its neuroprotective effects. MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H2O2incubation. The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H2O2exposure[1].
In Vivo
Cabergoline has a longer elimination half-life (63 to 109 h) compared with other D2-like receptor agonists, both a long-lasting clinical effect following single-dose administration, and an improvement in the quality of life of patients with chronic diseases are expected[1]. The most significant reduction in rapid eye movement (REM) sleep bout number occurred during the light phase, in which Cabergoline-injected female handled mice has 67.3% less REM sleep bouts (F(1,11)=12.892, P=0.004) than Cabergoline-injected females that are restrained, although the greatest number in reduction of REM sleep bouts occurr during the dark phase (82.3% fewer REM sleep bouts; F(1,11)=3.667, P=0.082). In male mice, Cabergoline reduces baseline Prolactin (PRL) levels (98.5%; F(1,6)=13.192, P=0.011) from 5.8±1.3 to 0.08 ng/mL within 2 hours of injection. After a 7-day recovery period, PRL levels return to values that are not different from baseline (5.0±0.60 ng/mL; F(1,6)=0.715, P=0.43)[2].
Clinical Trial
Baylor College of Medicine-National Institute on Drug Abuse (NIDA)
Cocaine Dependence-Cocaine Abuse-Cocaine Addiction-Substance Abuse
July 2011
Phase 1
National Institute on Drug Abuse (NIDA)-University of California, Los Angeles
Cocaine-Related Disorders-Substance-Related Disorders
June 2001
Phase 2
Novartis Pharmaceuticals-Novartis
Cushing's Disease
March 6, 2014
Phase 2
Postgraduate Institute of Medical Education and Research
Macroprolactinoma
May 2010
Etlik Zubeyde Hanim Womens' Health and Teaching Hospital
Polycystic Ovarian Syndrome-Ovarian Hyperstimulation Syndrome
March 2008
Aljazeera Hospital
OHSS
May 2013
Phase 2
Mona M Shaban-Cairo University
Ovarian Hyperstimulation Syndrome
December 2015
Phase 3
Northwestern University-Lynn Sage Foundation
Recurrent Breast Cancer-Stage IV Breast Cancer
November 2012
Early Phase 1
Hospital de Cruces
Complications Associated With Artificial Fertilization-Disorder of Endocrine Ovary
August 2007
Early Phase 1
Federico II University
Prolactinomas
January 2007
Phase 4
Par Pharmaceutical, Inc.-Anapharm
To Determine Bioequivalence Under Fed Conditions.
July 2001
Phase 1
Par Pharmaceutical, Inc.-Anapharm
To Determine Bioequivalence Under Fasting Conditions
August 2001
Phase 1
Seth Gordhandas Sunderdas Medical College
Cushing's Disease-Corticotroph Adenoma
November 2007
Phase 3
Benha University
Infertility
April 2014
Phase 2-Phase 3
Kasr El Aini Hospital
Infertility
December 2014
Phase 2-Phase 3
Aljazeera Hospital
OHSS
October 2016
Phase 2
Benha University
Infertility
April 2014
Phase 2-Phase 3
Federal University of São Paulo
Acromegaly
May 2005
Phase 4
Royan Institute
Ovarian Hyperstimulation Syndrome
June 2009
Phase 1-Phase 2
KK Women's and Children's Hospital
Ovarian Hyperstimulation Syndrome
April 2012
Phase 3
Columbia University
Body Weight-Impaired Glucose Tolerance in Obese
April 2002
Phase 1-Phase 2
Shin Kong Wu Ho-Su Memorial Hospital
In Vitro Fertilization
January 2010
Phase 4
Mashhad University of Medical Sciences
Diabetes Type 2
January 2012
Universidade Federal do Rio de Janeiro
Non-functioning Pituitary Adenomas-Prolactinomas
March 2010
Phase 2-Phase 3
Woman's Health University Hospital, Egypt
Female Reproductive Problem
May 2015
Phase 2
Novartis Pharmaceuticals-Novartis
Acromegaly
March 2006
Phase 4
St. Olavs Hospital-Norwegian University of Science and Technology
Pituitary Neoplasms-Adenoma
November 2014
Phase 3
Instituto Valenciano de Infertilidad, IVI VALENCIA
Ovarian Hyperstimulation Syndrome
April 2004
Phase 3
Istanbul Bakirkoy Maternity and Children Diseases Hospital
Adverse Reaction to Other Drugs and Medicines
March 2010
Phase 4
Technische Universität Dresden-Pfizer
Parkinson's Disease
February 2005
Phase 4
Pfizer
Restless Legs Syndrome
November 2002
Phase 3
Pfizer
Restless Legs Syndrome
January 2003
Phase 3
Pfizer
Parkinson Disease
July 2004
Phase 4
Boston Children’s Hospital
Endometriosis
May 2016
Phase 2
Institute for Neurodegenerative Disorders-Pfizer-GE Healthcare
Parkinson Disease-Parkinsonian Syndrome
January 2005
Novartis Pharmaceuticals-Novartis
Acromegaly
September 2006
Phase 4
University of Aarhus-Aarhus University Hospital
Hyperprolactinemia-Insulin Resistance
May 2008
Ludwig-Maximilians - University of Munich
Acromegaly
January 2008
Phase 4
Chiasma, Inc.
Acromegaly
February 2016
Phase 3
Baylor College of Medicine-National Institute on Drug Abuse (NIDA)
Cocaine Dependence-Cocaine Abuse-Cocaine Addiction-Substance Abuse
July 2011
Phase 1
National Institute on Drug Abuse (NIDA)-University of California, Los Angeles
Cocaine-Related Disorders-Substance-Related Disorders
June 2001
Phase 2
Novartis Pharmaceuticals-Novartis
Cushing's Disease
March 6, 2014
Phase 2
Postgraduate Institute of Medical Education and Research
Macroprolactinoma
May 2010
Etlik Zubeyde Hanim Womens' Health and Teaching Hospital
Polycystic Ovarian Syndrome-Ovarian Hyperstimulation Syndrome
March 2008
Aljazeera Hospital
OHSS
May 2013
Phase 2
