Skip to main content
SpringerLink
Log in

Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines

  • Short Communication
  • Published:
Inflammation Research Aims and scope Submit manuscript

Summary.

The predictive efficacy of drugs in humans is frequently estimated from both a high affinity for their receptor as measured in vitro and a long plasmatic half-life. This is grossly misleading since one key parameter is missing: drug concentration at the receptor site in vivo. As a case study we compared the efficacies of three H1 antihistamines in inhibiting histamine-induced wheal and flare in humans at two different time points with the above mentioned parameters. It is concluded that estimating in vivo receptor occupancy, which takes into account both the affinity of the drug for the receptor and its free plasma concentration, is a far better predictor for human pharmacodynamics and hence antihistamine potency, than considering in vitro affinity and plasmatic half-life only.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

Author information

Authors and Affiliations

  1. In Vitro Pharmacology Department, Chemin du Foriest, UCB S.A., 1420, Braine l’Alleud, Belgium

    M. Gillard & P. Chatelain

  2. Non Clinical Department, UCB S.A., 21 rue de Neuilly, 92003, Nanterre Cedex, France

    M. Strolin Benedetti

  3. Non Clinical Department, Chemin du Foriest, UCB S.A., 1420, Braine l’Alleud, Belgium

    E. Baltes

Authors
  1. M. Gillard
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. M. Strolin Benedetti
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. P. Chatelain
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. E. Baltes
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to M. Strolin Benedetti.

Additional information

Received 2 May 2005; returned for revision 7 June 2005; accepted by M. J. Parnham 13 June 2005

Rights and permissions

Reprints and permissions

About this article

Cite this article

Gillard, M., Benedetti, M.S., Chatelain, P. et al. Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines. Inflamm. res. 54, 367–369 (2005). https://doi.org/10.1007/s00011-005-1368-3

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/s00011-005-1368-3

Keywords

Search

Navigation