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Eur J Pharmacol. 2000 Jan 3;387(1):R5-7.

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

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Department of Pharmacochemistry, Division of Medicinal Chemistry, Leiden/Amsterdam Center for Drug Research, Vrije Universiteit Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, Netherlands.


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.

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