4. LABAs: Pharmacology, Mechanisms and Interaction with Anti-Inflammatory Treatments

  1. Jan Lötvall
  1. Gary P. Anderson

Published Online: 29 FEB 2012

DOI: 10.1002/9781119998624.ch4

Advances in Combination Therapy for Asthma and COPD

Advances in Combination Therapy for Asthma and COPD

How to Cite

Anderson, G. P. (2012) LABAs: Pharmacology, Mechanisms and Interaction with Anti-Inflammatory Treatments, in Advances in Combination Therapy for Asthma and COPD (ed J. Lötvall), John Wiley & Sons, Ltd, Chichester, UK. doi: 10.1002/9781119998624.ch4

Editor Information

  1. Krefting Research Centre, University of Gothenburg, Göteborg, Sweden

Author Information

  1. Lung Disease Research Group, Departments of Pharmacology and Medicine, University of Melbourne, Parkville, 3010 VIC, Australia

Publication History

  1. Published Online: 29 FEB 2012
  2. Published Print: 3 FEB 2012

ISBN Information

Print ISBN: 9780470727027

Online ISBN: 9781119998624

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Keywords:

  • LABAs, pharmacology, mechanisms;
  • galenical forms of LABAs;
  • receptor clusters, cellular organization;
  • ‘reassertion’ paradox, ‘exosites’;
  • beta-blockers not LABAs;
  • LABAs and steroids, molecular cooperativity

Summary

This chapter contains sections titled:

  • Galenical forms of LABAs: formulations, isomers, enantiomers, diasteriomers and salts

  • Absolute and functional β2-adrenoceptor selectivity

  • Cellular organization of receptor clusters: functional structure of the β2-adrenoceptor and mode of signalling

  • Dimers and oligomers: homo- and heterodimerism/oligoism

  • Pharmacogenomics of the β2-adrenoceptor and adenylate cyclase polymorphism in relation to LABAs

  • Understanding the ‘reassertion’ paradox, ‘exosites’ and relative speed of onset: the membrane diffusion microkinetic model of LABA action

  • Regulation and desensitization

  • Full versus partial agonism (pharmacological efficacy)

  • Beta-blockers not LABAs?

  • Non-receptor-mediated effects?

  • Biochemical basis of functional antagonism and its critical role in LABA action in disease and exacerbations

  • Molecular cooperativity between LABAs and steroids

  • Perspective

  • References