HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Reproterol--A monomolecular combination of orciprenaline and theophylline: novel aspects of its mode of action in asthma.

AbstractBACKGROUND AND OBJECTIVE:
Reproterol is a monomolecular combination of orciprenaline and theophylline used as beta-adrenergic agonist to induce bronchodilation in bronchial asthma. Since the mechanism of action of reproterol has not been investigated so far, its potential anti-inflammatory activity in asthma remains still unknown. Therefore, we have studied in vitro whether the theophylline component of the reproterol molecule might enhance the stimulatory effect of the beta-adrenoceptor on cAMP production resulting in suppression of inflammatory mediator production.
METHODS:
The effects of reproterol, orciprenaline and theophylline (10(-9)-10(-5) M) on spontaneous cAMP (5 x 10(4) cells/30 min)- and on LPS (10 microg/ml)-stimulated LTB4 production (10(5) cells/4 h) were determined in normal monocytes in vitro.
RESULTS:
Production of cAMP (n = 9) was significantly augmented in a dose-dependent manner by orciprenaline (30 +/- 8%) and theophylline (28 +/- 10%), but mostly by reproterol (127 +/- 8%) at 10(-5) M. Despite incubation with propranolol, significant stimulation of cAMP production was notable following reproterol therapy. Production of LTB4 was significantly inhibited by reproterol (-48 +/- 14%) and less by theophylline (-28 +/- 10%), but was stimulated by orciprenaline (+20 +/- 8%) at 10(-5) M.
CONCLUSION:
We conclude that reproterol exerts a strong stimulatory effect on monocyte cAMP production and a suppressive effect on LTB4 production possibly due to a synergistic mode of action on adenylate cyclase activity and inhibition of phosphodiesterases. More clinical studies in bronchial asthma will be needed to determine whether these results may translate into clinically relevant effects.
AuthorsU R Juergens, M Stöber, H Vetter
JournalRespiration; international review of thoracic diseases (Respiration) Vol. 66 Issue 3 Pg. 220-4 ( 1999) ISSN: 0025-7931 [Print] Switzerland
PMID10364737 (Publication Type: Comment, Journal Article)
Chemical References
  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Bronchodilator Agents
  • Drug Combinations
  • reproterol
  • Leukotriene B4
  • Metaproterenol
  • Theophylline
  • Cyclic AMP
Topics
  • Adrenergic beta-Agonists (pharmacology)
  • Adrenergic beta-Antagonists (pharmacology)
  • Adult
  • Bronchodilator Agents (pharmacology)
  • Cyclic AMP (biosynthesis)
  • Drug Combinations
  • Humans
  • Leukotriene B4 (biosynthesis)
  • Metaproterenol (analogs & derivatives, pharmacology)
  • Reference Values
  • Theophylline (analogs & derivatives, pharmacology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: