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Olodaterol (BI1744)??????????????2-adrenoceptor????????????EC50??????1.4??0.08 nM???
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生物活性
Description
Olodaterol (BI1744) is a long acting??2-adrenoceptoragonist with anEC50of 1.4??0.08 nM.
IC50& Target
EC50: 1.4??0.08 nM (??2-adrenoceptor)[1]
In Vitro
Olodaterol shows a potent, nearly full agonistic response at the h??2-adrenoceptor (EC50=0.1 nM; intrinsic activity=88% compared with isoprenaline) and a significant selectivity profile (241- and 2299-fold against the h??1- and h??3-ARs, respectively). Likewise, olodaterol is able to potently reverse contraction induced by different stimuli in isolated human bronchi[2].
In Vivo
Olodaterol is a long acting ??2-agonist that induces bronchodilation up to 24 h after dosing in patients with chronic obstructive pulmonary disease (COPD) . Olodaterol dose-dependently attenuates cell influx and pro-inflammatory mediator release in murine and guinea pig models of pulmonary inflammation. Olodaterol attenuates pro-inflammatory mediator release from human parenchymal explants and whole blood and reduced expression of CD11b adhesion molecules on granulocytes, but without direct effects on IL-8-induced neutrophil transwell migration[3]. Once-daily olodaterol 5 ??g is an effective therapy in improving lung function and symptomatic outcomes in patients with moderate to very severe (COPD) receiving other maintenance therapy, with a satisfactory safety profile[4].
Clinical Trial
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
June 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
November 2008
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Asthma
January 2006
Phase 2
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
June 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
November 2008
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Asthma
January 2006
Phase 2
Boehringer Ingelheim-RTI health solutions, US
Pulmonary Disease, Chronic Obstructive
February 1, 2017
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
October 2012
Phase 1
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
March 8, 2016
Phase 4
Boehringer Ingelheim
Asthma
March 2011
Phase 2
University of Dundee-Boehringer Ingelheim-NHS Tayside
Chronic Obstructive Pulmonary Disease
June 2017
Phase 4
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 24, 2017
Phase 1
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
September 22, 2016
Phase 4
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
September 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
September 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2014
Phase 2
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 12, 2016
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
March 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
November 2013
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 13, 2015
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 2012
Phase 3
Boehringer Ingelheim
Asthma
October 2011
Phase 2
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
March 2012
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
November 2013
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
September 2011
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
September 2011
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
February 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
March 2014
Phase 3
University of Dundee
Asthma
August 2016
Phase 4
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
October 2013
Phase 3
Boehringer Ingelheim
Asthma
February 2010
Phase 2
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
January 2010
Phase 2
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
June 2009
Phase 3
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
March 29, 2017
Phase 4
Boehringer Ingelheim
Pulmonary Disease, Chronic Obstructive
December 19, 2016
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