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GPCR/G ProteinImmunology/Inflammation-
Bilastine?????????H1??????????????????????????????????????????????????????????????????
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生物活性
Description
Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].
Clinical Trial
Charite University, Berlin, Germany-Faes Farma, S.A.
Cold Contact Urticaria
September 2010
Phase 2-Phase 3
Faes Farma, S.A.
Allergic Rhinoconjunctivitis-Chronic Urticaria
January 2010
Phase 1-Phase 2
Faes Farma, S.A.
Healthy
May 2010
Phase 1
Menarini International Operations Luxembourg SA
Allergic Rhinitis-Urticaria
October 2015
Phase 4
Faes Farma, S.A.-Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd-MDS Pharma Services Switzerland AG
Healthy
November 2007
Phase 1
Universidade do Sul de Santa Catarina
Allergic Rhinitis
August 2013
Phase 4
Charite University, Berlin, Germany
Chronic Urticaria
July 2014
Phase 3
Menarini International Operations Luxembourg SA
Seasonal Allergic Rhinoconjunctivitis-Asthma
April 2016
Phase 4
Faes Farma, S.A.-Merck Sharp & Dohme Corp.-Allied Research International
Seasonal Allergic Rhinitis-Hay Fever-Allergic Conjunctivitis-Hypersensitivity
December 2007
Phase 2
Faes Farma, S.A.-Allied Research International
Seasonal Allergic Rhinitis-Hay Fever-Rhinoconjunctivitis
October 2007
Phase 2
Yuhan Corporation
Seasonal Allergic Rhinitis
June 2011
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
April 2003
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
October 2006
Phase 2
Faes Farma, S.A.
Healthy
August 2006
Phase 1
Faes Farma, S.A.
Perennial Allergic Rhinitis
May 2004
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
May 2005
Phase 3
Faes Farma, S.A.
Urticaria
July 2006
Phase 3
Grupo de Alergología Clínica y Experimental
Urticaria
August 2013
Phase 4
Association Asthma, Bulgaria-Nasaleze
Seasonal Allergic Rhinitis
May 2015
Phase 4
Charite University, Berlin, Germany-Faes Farma, S.A.
Cold Contact Urticaria
September 2010
Phase 2-Phase 3
Faes Farma, S.A.
Allergic Rhinoconjunctivitis-Chronic Urticaria
January 2010
Phase 1-Phase 2
Faes Farma, S.A.
Healthy
May 2010
Phase 1
Menarini International Operations Luxembourg SA
Allergic Rhinitis-Urticaria
October 2015
Phase 4
Faes Farma, S.A.-Charles River Clinical Services Edinburgh Ltd and CR Laboratories Preclinical Services Ltd-MDS Pharma Services Switzerland AG
Healthy
November 2007
Phase 1
Universidade do Sul de Santa Catarina
Allergic Rhinitis
August 2013
Phase 4
Charite University, Berlin, Germany
Chronic Urticaria
July 2014
Phase 3
Menarini International Operations Luxembourg SA
Seasonal Allergic Rhinoconjunctivitis-Asthma
April 2016
Phase 4
Faes Farma, S.A.-Merck Sharp & Dohme Corp.-Allied Research International
Seasonal Allergic Rhinitis-Hay Fever-Allergic Conjunctivitis-Hypersensitivity
December 2007
Phase 2
Faes Farma, S.A.-Allied Research International
Seasonal Allergic Rhinitis-Hay Fever-Rhinoconjunctivitis
October 2007
Phase 2
Yuhan Corporation
Seasonal Allergic Rhinitis
June 2011
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
April 2003
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
October 2006
Phase 2
Faes Farma, S.A.
Healthy
August 2006
Phase 1
Faes Farma, S.A.
Perennial Allergic Rhinitis
May 2004
Phase 3
Faes Farma, S.A.
Seasonal Allergic Rhinitis
May 2005
Phase 3
Faes Farma, S.A.
Urticaria
July 2006
Phase 3
Grupo de Alergología Clínica y Experimental
Urticaria
August 2013
Phase 4
Association Asthma, Bulgaria-Nasaleze
Seasonal Allergic Rhinitis
May 2015
Phase 4
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References
