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PMID: 6145597 Published · ppublish English Journal Article

The rat lipolytic beta-adrenoceptor: studies using novel beta-adrenoceptor agonists.

European journal of pharmacology ·Vol. 100 ·No. 3-4 ·1984-05-04 ·Pages 309-19

Wilson C, Wilson S, Piercy V, Sennitt MV, Arch JR

Abstract

EC50 and relative intrinsic activity values were obtained for isoprenaline, fenoterol, salbutamol, prenalterol and three new beta-adrenoceptor agonists, BRL 28410, BRL 35113 and BRL 35135 on rat white adipocyte lipolysis, rat atrial rate and tension, rat uterus tension and guinea-pig tracheal tension. Fenoterol and salbutamol were selective for tracheal and uterine responses, prenalterol was selective for atrial responses, but BRL 28410, BRL 35113 and BRL 35135 were selective for the adipocyte lipolytic response. pA2 values for propranolol, practolol, ICI 118,551 and sotalol were obtained on adipocytes, atria and trachea. pA2 values for propranolol and sotalol were much lower on adipocytes than on atria or trachea. The pA2 value for practolol was lower on adipocytes than on atria and the pA2 value for ICI 118,551 was lower on adipocytes than on trachea. Both agonist and antagonist studies therefore suggest that the rat adipocyte lipolytic receptor does not fit into the current beta 1/beta 2-adrenoceptor classification.

MeSH Terms
Adipose Tissue/drug effects Adrenergic beta-Agonists Adrenergic beta-Antagonists/pharmacology Animals Female Guinea Pigs Heart/drug effects Heart Rate/drug effects In Vitro Techniques Lipolysis/drug effects Male Muscle Relaxation/drug effects Muscle, Smooth, Vascular/drug effects Myocardial Contraction/drug effects Rats Rats, Inbred Strains Receptors, Adrenergic, beta/drug effects Trachea/drug effects Uterus/drug effects
Chemicals
Adrenergic beta-Agonists Adrenergic beta-Antagonists Receptors, Adrenergic, beta
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Wilson C
Wilson S
Piercy V
Sennitt M V
Arch J R
Article Info
Journal
European journal of pharmacology
Abbr.
Eur J Pharmacol
ISSN
0014-2999
Published
1984-05-04
Pages
309-19
Language
English
Region
Netherlands
NLM ID
1254354
Subset
IM
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