"目录号: HY-14773
Mirabegron 是一种选择性的肾上腺素受体 (β3-adrenoceptor) 激动剂，EC50为 22.4 nM。
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生物活性
Description
Mirabegron is a selectiveβ3-adrenoceptoragonist withEC50of 22.4 nM.
IC50& Target
EC50: 22.4 nM (β3-adrenoceptor)[1]
In Vitro
Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50value is 22.4 nM. EC50values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50of Mirabegron in rat bladder strips precontracted with 10-6M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%[1].
In Vivo
Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. In contrast, Mirabegron does not decrease the amplitude of rhythmic bladder contraction at up to 3 mg/kg i.v.. On the contrary, Oxybutynin significantly increases the frequency of rhythmic bladder contraction and decreased its amplitude at doses of 0.272 mg/kg i.v. or more[1].
Clinical Trial
CHU de Quebec-Universite Laval
Overactive Bladder-Urinary Incontinence
April 2013
Phase 3
CHU de Quebec-Universite Laval
Overactive Bladder-Urinary Incontinence
April 2013
Phase 3
Astellas Pharma Inc
Healthy-Pharmacokinetics of Mirabegron
April 2009
Phase 1
Astellas Pharma Inc
Healthy-Pharmacokinetics of Mirabegron
May 2009
Phase 1
Astellas Pharma Inc
Pharmacokinetics of YM178
October 2008
Phase 1
Astellas Pharma Inc
Pharmacokinetics of Mirabegron-Healthy Subjects
October 2008
Phase 1
Astellas Pharma Inc
Healthy Subjects-Plasma Concentration of Mirabegron
August 2012
Phase 1
Astellas Pharma Inc-Astellas Pharma Europe B.V.
Pharmacokinetics of Mirabegron-Neurogenic Detrusor Overactivity-Overactive Bladder
July 2014
Phase 1
Astellas Pharma Inc
Pharmacokinetics of Mirabegron-Bioavailability-Healthy Subjects
February 2006
Phase 1
Loyola University-Astellas Pharma US, Inc.
Overactive Bladder
January 2015
Phase 4
Johns Hopkins University-Astellas Pharma US, Inc.
Erectile Dysfunction-Overactive Bladder-Urinary Incontinence
September 2016
Phase 1-Phase 2
Astellas Pharma Inc
Healthy Volunteers-Pharmacokinetics of Mirabegron
March 2009
Phase 1
State University of New York at Buffalo-Astellas Pharma Inc
Urinary Frequency/Urgency-Bladder Irritable-Bladder Pain Syndrome
January 2017
Phase 4
Astellas Pharma Inc
Pharmacokinetics of Mirabegron-Healthy Subjects
September 2002
Phase 1
Astellas Pharma Inc
Healthy Volunteers-Pharmacokinetics of Mirabegron
March 2009
Phase 1
Lawson Health Research Institute
Urinary Bladder, Neurogenic
July 2014
Phase 2-Phase 3
Astellas Pharma Inc
Healthy Volunteers-Pharmacodynamics of Mirabegron
July 2009
Phase 1
Astellas Pharma Inc
Overactive Bladder-Cardiovascular Disease
December 2012
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Neurogenic Detrusor Overactivity
June 17, 2016
Phase 3
Ingrid Jazet-Leiden University Medical Center
Obesity
June 2016
Phase 4
Buddhist Tzu Chi General Hospital
Overactive Bladder Syndrome
November 16, 2015
Phase 3
Buddhist Tzu Chi General Hospital
Urinary Incontinence-Overactive Bladder Syndrome
April 28, 2015
Phase 3
Astellas Pharma Inc
Pharmacokinetics of Mirabegron and Tolterodine-Healthy
June 2013
Phase 4
Astellas Pharma Inc
Urinary Bladder, Overactive
April 2009
Phase 3
HealthPartners Institute
Parkinson Disease-Overactive Bladder-Impaired Cognition
December 2015
Phase 4
Astellas Pharma Global Development, Inc.-Astellas Pharma Inc
Overactive Bladder (OAB)
October 14, 2014
Phase 4
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Healthy Subjects-Pharmacokinetics-Drug-Drug Interaction (DDI)
March 2014
Phase 1
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Overactive Bladder-Neurogenic Detrusor Overactivity
November 2015
Phase 1
Theodore R. Brown, MD MPH-Astellas Pharma Inc-EvergreenHealth
Multiple Sclerosis
May 2014
Phase 4
Astellas Pharma Inc
Pharmacokinetics-Healthy Subjects
May 2005
Phase 1
Kessler Foundation-National Institute on Disability, Independent Living, and Rehabilitation Research
Spinal Cord Injuries-Urinary Bladder, Neurogenic
July 5, 2017
Phase 2
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Pharmacokinetics-Healthy Subjects-Mild and Moderate Hepatic Impairment
November 2008
Phase 1
Astellas Pharma Inc
Intraocular Pressure
November 2010
Phase 1
Philadelphia Urosurgical Associates-Astellas Pharma Global Development, Inc.
Cystitis, Interstitial
August 2016
Phase 3
Karolinska Institutet
Overactive Bladder
August 2013
Phase 4
Astellas Pharma Inc
Overactive Bladder
October 2012
Phase 4
Southern Illinois University-Astellas Scientific & Medical Affairs, Inc.-Sisters of the Third Order of St. Francis
Lower Urinary Tract Symptoms-Nocturia
April 2015
Astellas Pharma Inc
Lower Urinary Tract Symptoms-Bladder Outlet Obstruction
December 2006
Phase 2
Astellas Pharma Inc
Urinary Bladder, Overactive
April 2008
Phase 3
Astellas Pharma Europe B.V.-Astellas Pharma Inc
Healthy Subjects-Pharmacokinetics-Drug-Drug Interaction (DDI)
May 2014
Phase 1
Astellas Pharma Inc
Cardiovascular-Healthy Subjects-Pharmacokinetics
August 2010
Phase 1
Astellas Pharma Inc
Healthy Volunteers-Pharmacokinetics of Mirabegron
October 2008
Phase 1
Astellas Pharma Inc-Astellas Pharma Singapore Pte. Ltd.
Overactive Bladder
January 25, 2016
Phase 4
Astellas Pharma Inc
Urinary Bladder, Overactive
April 2008
Phase 3
Samsung Medical Center
Overactive Bladder
June 2015
Phase 4
Astellas Pharma
