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

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 therapeut...

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Bibliographic Details
Published inEuropean journal of pharmacology Vol. 387; no. 1; pp. R5 - R7
Main Authors Bakker, Remko A, Wieland, Kerstin, Timmerman, Henk, Leurs, Rob
Format Journal Article
LanguageEnglish
Published Elsevier B.V 03.01.2000
Subjects
Constitutive activity
Histamine H 1 receptor
Inverse agonism
Histamine H 1 receptor
Inverse agonism
Constitutive activity
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Summary: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.
ISSN:0014-2999
1879-0712
DOI:10.1016/S0014-2999(99)00803-1