Document Detail


Beta-adrenoceptor subtypes mediating the airways response to BRL 35135 in man.
MedLine Citation:
PMID:  12959274     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1 The purpose of the study was to assess the bronchorelaxant effects of the beta3-adrenoceptor agonist BRL 35135 in normal human airways. 2 Eight healthy male subjects were studied, having previously demonstrated airways responsiveness to inhaled salbutamol 200 microg, with a group mean (+/- s.e. mean) fall in airways resistance (Raw), from baseline, of 37 +/- 5%. 3 Subjects attended the laboratory on 3 separate days, having fasted and taken placebo (PL) or nadolol 20 mg (N20), 2 h previously. 4 After 30 min rest, baseline measurements of Raw, serum potassium, glucose and free fatty acid were performed before subjects were given single oral doses of BRL 35135 8 mg (BRL) or placebo BRL. Measurements were repeated 60 min after the BRL or placebo BRL were given. 5 There was a significant (P < 0.05) fall in Raw (% change from baseline, as means and 95% CI) with PL/BRL: -32(-18, -46), compared with either PL/PL: -8(5, -21), or N20/BRL: -11(2, -24). There was no significant difference between PL/PL and N20/BRL. 6 A similar pattern to Raw was observed for both of the beta2-mediated metabolic responses which were also antagonised by nadolol. For the potassium response (mmol l(-1)), there was a significant (P < 0.05) difference between PL/BRL: -0.50(-0.31, -0.69), in comparison with either PL/PL: 0.08(-0.11, 0.27) or N20/BRL: 0.09(-0.10, 0.28), but values for PL/PL and N20/BRL were not significantly different. In contrast, with the free fatty acid response (nmol 1(-1)), the increase seen with N20/BRL: 85(1.0, 171.0) was significantly (P < 0.05) different from PL/PL: 3.7(-82.3, 89.8), but was not different from PL/BRL: 132.5(46.5, 218.5). 7 In conclusion, BRL 35135 produced airways, potassium and glucose responses which were antagonised by nadolol, whereas the lipolysis response was not. This suggests that there are not functional beta3-adrenoceptors in human airways.
Authors:
D M Newnham; C G Ingram; A Mackie; B J Lipworth
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Publication Detail:
Type:  Clinical Trial; Controlled Clinical Trial; Journal Article    
Journal Detail:
Title:  British journal of clinical pharmacology     Volume:  36     ISSN:  0306-5251     ISO Abbreviation:  Br J Clin Pharmacol     Publication Date:  1993 Dec 
Date Detail:
Created Date:  2003-09-08     Completed Date:  2003-10-07     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  7503323     Medline TA:  Br J Clin Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  567-71     Citation Subset:  IM    
Affiliation:
Department of Clinical Pharmacology, Ninewells Hospital and Medical School, University of Dundee, Dundee.
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MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Agonists / pharmacology*
Adult
Airway Resistance / drug effects
Bronchi / drug effects*,  metabolism
Fatty Acids / metabolism
Glucose / metabolism
Humans
Male
Phenethylamines / pharmacology*
Potassium / metabolism
Receptors, Adrenergic, beta / metabolism
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Agonists; 0/Fatty Acids; 0/Phenethylamines; 0/Receptors, Adrenergic, beta; 50-99-7/Glucose; 7440-09-7/Potassium; 91097-81-3/BRL 35135
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