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PMID: 6287309 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

An initial characterization of human heart beta-adrenoceptors and their mediation of the positive inotropic effects of catecholamines.

Naunyn-Schmiedeberg's archives of pharmacology ·Vol. 319 ·No. 3 ·1982-06-00 ·Pages 216-21

Kaumann AJ, Lemoine H, Morris TH, Schwederski U

Abstract

The positive inotropic effects of catecholamines were studied on samples of ventricular myocardium taken from patients undergoing open heart surgery. The adenylyl cyclase and binding of 3H-(-)-bupranolol were examined in membrane particles prepared from similarly obtained samples. The equilibrium dissociation constant (KD) for (-)-bupranolol was estimated in 4 ways: blockade of the positive inotropic effects of catecholamines, blockade of the stimulation of the adenylyl cyclase by catecholamines, saturation binding of 3H-(-)-bupranolol, inhibition of the binding of 3H-(-)-bupranolol by its unlabeled stereoisomers. The estimates of KD fall in the range 0.5-1.4 nmol/l. The stereo-selectivity ratio (KD (+)-isomer/KD (-)-isomer) is 73. Both values for bupranolol are very similar in cat and man. The inotropic potency of (-)-noradrenaline is nearly 2 orders of magnitude higher in cat heart tissues than in tissues from human hearts. The difference in inotropic potencies between species is only partially accounted for by the five-fold lower potency of (-)-noradrenaline for the human heart adenylyl cyclase as compared to the cat enzyme.

MeSH Terms
Adenylyl Cyclases/analysis Animals Bupranolol/metabolism,pharmacology Catecholamines/pharmacology Cats Dose-Response Relationship, Drug Humans In Vitro Techniques Myocardial Contraction/drug effects Myocardium/metabolism Receptors, Adrenergic/physiology Receptors, Adrenergic, beta/metabolism,physiology Species Specificity Stimulation, Chemical
Chemicals
Catecholamines Receptors, Adrenergic Receptors, Adrenergic, beta Bupranolol Adenylyl Cyclases
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Kaumann A J
Lemoine H
Morris T H
Schwederski U
References (22)
22 references, click to expand
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Article Info
Journal
Naunyn-Schmiedeberg's archives of pharmacology
Abbr.
Naunyn Schmiedebergs Arch Pharmacol
ISSN
0028-1298
DOI
10.1007/BF00495868
Published
1982-06-00
Pages
216-21
Language
English
Region
Germany
NLM ID
0326264
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00495868 View journal details
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