Literature DB >> 10633171

Constitutive activity of the histamine H(1) receptor reveals inverse agonism of histamine H(1) receptor antagonists.

R A Bakker1, K Wieland, H Timmerman, R Leurs.   

Abstract

Transient expression of the wild-type human histamine H(1) receptor in SV40-immortalised African green monkey kidney cells resulted in an agonist-independent elevation of the basal levels of the second messenger inositoltrisphospate. Several histamine H(1) receptor antagonists, including the therapeutically used anti-allergics cetirizine, loratadine and epinastine reduced this constitutive histamine H(1) receptor activity. Inverse agonism, i.e., stabilisation of an inactive conformation of the human histamine H(1) receptor, may therefore be a key component of the anti-allergic mechanism of action of clinically used antihistamines.

Entities:  

Mesh：

Substances：

Year:  2000        PMID： 10633171     DOI： 10.1016/s0014-2999(99)00803-1

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  23 in total

1.  Histamine H3-receptor-mediated [35S]GTP gamma[S] binding: evidence for constitutive activity of the recombinant and native rat and human H3 receptors.

Authors:  A Rouleau; X Ligneau; J Tardivel-Lacombe; S Morisset; F Gbahou; J-C Schwartz; J-M Arrang
Journal:  Br J Pharmacol       Date:  2002-01       Impact factor: 8.739

2.  Involvement of histamine receptors in the atypical antipsychotic profile of clozapine: a reassessment in vitro and in vivo.

Authors:  Marie Humbert-Claude; Elisabeth Davenas; Florence Gbahou; Ludwig Vincent; Jean-Michel Arrang
Journal:  Psychopharmacology (Berl)       Date:  2011-09-13       Impact factor: 4.530

Review 3.  Controlled Allergen Challenge Facilities and Their Unique Contributions to Allergic Rhinitis Research.

Authors:  Michelle L North; Mena Soliman; Terry Walker; Lisa M Steacy; Anne K Ellis
Journal:  Curr Allergy Asthma Rep       Date:  2015-04       Impact factor: 4.806

Review 4.  Pharmacological targeting of allergen-specific T lymphocytes.

Authors:  Peter A Tauber; Winfried F Pickl
Journal:  Immunol Lett       Date:  2017-03-18       Impact factor: 3.685

5.  Structure of the human histamine H1 receptor complex with doxepin.

Authors:  Tatsuro Shimamura; Mitsunori Shiroishi; Simone Weyand; Hirokazu Tsujimoto; Graeme Winter; Vsevolod Katritch; Ruben Abagyan; Vadim Cherezov; Wei Liu; Gye Won Han; Takuya Kobayashi; Raymond C Stevens; So Iwata
Journal:  Nature       Date:  2011-06-22       Impact factor: 49.962

Review 6.  Urticaria and Angioedema: an Update on Classification and Pathogenesis.

Authors:  Susanne Radonjic-Hoesli; Kathrin Scherer Hofmeier; Sara Micaletto; Peter Schmid-Grendelmeier; Andreas Bircher; Dagmar Simon
Journal:  Clin Rev Allergy Immunol       Date:  2018-02       Impact factor: 8.667

Review 7.  International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.

Authors:  Pertti Panula; Paul L Chazot; Marlon Cowart; Ralf Gutzmer; Rob Leurs; Wai L S Liu; Holger Stark; Robin L Thurmond; Helmut L Haas
Journal:  Pharmacol Rev       Date:  2015-07       Impact factor: 25.468

8.  11H-Dibenzo[b,e]azepine-6-carbonitrile.

Authors:  Guo-Dong Fan; Yu-Liang Xiao; Gui-Rong You; Gui-Yun Duan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-10-18

Review 9.  Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review.

Authors:  Philippe Devillier; Nicolas Roche; Christophe Faisy
Journal:  Clin Pharmacokinet       Date:  2008       Impact factor: 6.447

10.  Antihistaminic, anti-inflammatory, and antiallergic properties of the nonsedating second-generation antihistamine desloratadine: a review of the evidence.

Authors:  G Walter Canonica; Michael Blaiss
Journal:  World Allergy Organ J       Date:  2011-02-23       Impact factor: 4.084
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.