The importance of choice of agonist in studies designed to predict β2:β1 adrenoceptor selectivity of antagonists from pA2 values on guinea-pig trachea and atria

O'Donnell S.R. and Wanstall J.C. (1979) The importance of choice of agonist in studies designed to predict β2:β1 adrenoceptor selectivity of antagonists from pA2 values on guinea-pig trachea and atria. Naunyn-Schmiedeberg's Archives of Pharmacology, 308 3: 183-190. doi:10.1007/BF00501381


Author O'Donnell S.R.
Wanstall J.C.
Title The importance of choice of agonist in studies designed to predict β2:β1 adrenoceptor selectivity of antagonists from pA2 values on guinea-pig trachea and atria
Journal name Naunyn-Schmiedeberg's Archives of Pharmacology   Check publisher's open access policy
ISSN 0028-1298
Publication date 1979-01-01
Sub-type Article (original research)
DOI 10.1007/BF00501381
Open Access Status Not yet assessed
Volume 308
Issue 3
Start page 183
End page 190
Total pages 8
Publisher Springer-Verlag
Subject 3004 Pharmacology
Abstract 1. pA2 values have been obtained for propranolol, butoxamine, H35/25 and atenolol on guinea-pig isolated trachea and atria (rate) using noradrenaline (β1-selective), isoprenaline (non-selective) and fenoterol (β2-selective) as agonists. 2. pA2 values varied with the agonist used on trachea but not on atria and, therefore, trachea: atria selectivity values varied with the agonist used. 3. It is suggested that the best estimate of the selectivity of an antagonist between β2- and β1-adrenoceptors is obtained by comparing its pA2 value obtained on trachea using a β2-selective agonist with that obtained on atria using a β1-selective agonist. The reasons for this are discussed. 4. The quantitative values for β2:β1 selectivity obtained using the above pA2 values were butoxamine 17.0, H35/25 13.5, propranolol 2.75 and atenolol 0.036, i.e. butoxamine and H35/25 were β2-selective, propranolol was non-selective and atenolol was β1-selective. 5. The results support the hypotheses that guinea-pig trachea contains a mixture of β1- and β2-adrenoceptors and that guinea-pig atria contain only β1-adrenoceptors.
Keyword Guinea-pig atria
Guinea-pig trachea
pA2 values
Receptor selectivity
Selective β-adrenoceptor antagonists
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import - Archived
 
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Created: Tue, 30 Aug 2016, 14:26:29 EST by System User