Drugs in R & D

, Volume 6, Issue 6, pp 371–384 | Cite as

Preclinical Pharmacology of Bilastine, a New Selective Histamine H1 Receptor Antagonist

Receptor Selectivity and in Vitro Antihistaminic Activity
  • Reyes Corcóstegui
  • Luis Labeaga
  • Ana Innerárity
  • Agustin Berisa
  • Aurelio Orjales
Original Research Article


Objective: This study aimed to establish the receptor selectivity and antihistaminic activity of bilastine, a new selective antihistamine receptor antagonist.

Design and methods: In vitro experiments were conducted using a receptor binding screening panel and guinea-pig and rat tissues. Antihistaminic activity was determined using H1 receptor binding studies and in vitro H1 antagonism studies conducted in guinea-pig tissues and human cell lines. Receptor selectivity was established using a receptor binding screening panel and a receptor antagonism screening conducted in guinea-pig, rat and rabbit tissues. Inhibition of inflammatory mediators was determined through the Schultz-Dale reaction in sensitised guinea-pig ileum.

Results: Bilastine 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 guineapig 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. The specificity of its H1-receptor antagonistic activity was also demonstrated in a series of in vitro experiments conducted on guinea-pig and rat tissues. The results of these studies confirmed the lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3-receptors. The results of the in vitro Schultz-Dale reaction demonstrated that bilastine also has anti-inflammatory activity.

Conclusions: These preclinical studies provide evidence that bilastine has H1-antihistamine activity, with high specificity for H1-receptors, and poor or no affinity for other receptors. Bilastine has also been shown to have anti-inflammatory properties.


Histamine Cetirizine Fexofenadine Chronic Idiopathic Urticaria Carbogen 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



This work has been funded in part by the Ministry of Industry, Tourism and Commerce (formerly Ministry of Science and Technology) of Spain (PROFIT) and by the Department of Industry, Commerce and Tourism of the Basque Government (INTEK).

All the authors are employees of FAES FARMA, SA.


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© Adis Data Information BV 2005

Authors and Affiliations

  • Reyes Corcóstegui
    • 1
  • Luis Labeaga
    • 1
  • Ana Innerárity
    • 1
  • Agustin Berisa
    • 1
  • Aurelio Orjales
    • 1
  1. 1.Department of ResearchFAES FARMA, SALeioaSpain

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