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

  title={Preclinical Pharmacology of Bilastine, a New Selective Histamine H1 Receptor Antagonist},
  author={R. Corcostegui and Luis Labeaga and Ana Inner{\'a}rity and Arben Beri{\vs}a and Aurelio Orjales},
  journal={Drugs in R \& D},
AbstractObjective: 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… 

In Vivo Pharmacological Characterisation of Bilastine, a Potent and Selective Histamine H1 Receptor Antagonist

In vivo preclinical studies corroborate those obtained from previously conducted in vitro experiments of bilastine, and provide evidence that bilastines possesses antihistaminic as well as antiallergic properties, with similar potency to cetirizine and superior potency to fexofenadine.

Elucidation of Inverse Agonist Activity of Bilastine

Preseasonal prophylactic administration with bilastine could down-regulate basal H1R gene expression in the nasal mucosa and ameliorate the nasal symptoms during the peak pollen period.

Safety profile of bilastine: 2nd generation H1-antihistamines.

  • F. Scaglione
  • Medicine, Biology
    European review for medical and pharmacological sciences
  • 2012
Bilastine is a new H1 antagonist with no sedative side effects, no cardiotoxic effects, and no hepatic metabolism, and it meets the current criteria for medication used in the treatment of allergic rhinitis and urticaria.

Pharmacology of Antihistamines

All H1-antihistamines have anti-inflammatory effects but it requires regular daily dosing rather than dosing 'on-demand' for this effect to be clinically demonstrable.

Bilastine and the central nervous system.

Bilastine is a new H1 antihistamine that proves to be effective in treating allergic rhinoconjunctivitis (seasonal and perennial) and urticaria and is defined as a clinically promising drug with a good safety profile as regards adverse effects upon the central nervous system.

Safety and efficacy of bilastine: a new H1-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria

  • M. Church
  • Medicine
    Expert opinion on drug safety
  • 2011
Bilastine has high selectivity for H1-receptors, is rapidly and effectively absorbed, undergoes negligible metabolism and is a substrate for P-glycoprotein, which limits its passage across the blood–brain barrier.

Bilastine as a Potential Treatment in Allergic Rhinitis

Bilastine is a novel H1 antihistamine with anti-allergic properties which is highly effective in the treatment of symptoms of allergic rhinitis and has a favorable pharmacokinetic and pharmacodynamic profile and is generally well tolerated.

Pharmacokinetic-Pharmacodynamic Modelling of the Antihistaminic (H1) Effect of Bilastine

The pharmacokinetic and pharmacodynamic relationships of bilastine were reliably described with the use of an indirect response pharmacodynamic model, which led to an accurate prediction of the pharmacodynamic activity of bilastsine.



In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent.

This compound displayed very low affinity for serotonergic, noradrenergic and muscarinic cholinergic receptors as evidenced in both binding assays and functional tests.

Regulation of the human histamine H1 receptor stably expressed in Chinese hamster ovary cells

In CHOhumH1 cells the human histamine H1 receptor is susceptible to short‐term and long‐term receptor regulation in which PKC does not seem to play a role, which provides an excellent model system for studying the mechanism(s) of PKC‐independent H1 receptors regulation.

Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist

Interestingly, 4-methylhistamine is identified as a high-affinity H4R ligand that has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes, of major importance for future studies to unravel the physiological roles of the H 4R.

The current cardiac safety situation with antihistamines

  • Y. G. YapA. Camm
  • Biology, Medicine
    Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology
  • 1999
Concomitant administration with drugs that inhibit the hepatic cytochrome P‐450 (imidazole antifungals, macrolide antibiotics) or those that prolong the QT interval by the same or other mechanism increases their effect on the cardiac repolarization.

Antiallergic effect of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidaz ole difumarate (KB-2413).

Antiallergic effects of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazol e difumarate (KB-2413) were investigated in immediate type hypersensitivities. KB-2413 (0.005-0.04 mg/kg p.o.)


Various applications of pAx measurements are discussed based on the hypothesis that drugs and drug antagonists compete for receptors according to the mass law, and a new measure, pAh, is introduced to express the activity of unsurmountable antagonists.

The spirally cut tracheal strip preparation

This document is intended to provide a history of the field and some of the techniques used, as well as specific cases, that were developed over a period of several years to develop a theory of pharmacology and its application in the context of modern medicine.