ArticleNaunyn-Schmiedeberg's archives of pharmacology2004
Aspartate138 is required for the high-affinity ligand binding site but not for the low-affinity binding site of the beta1-adrenoceptor.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 10 citations in OpenAlex.
- Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptor.Molecular pharmacology · 2014Article
- Ligand-directed signalling at beta-adrenoceptors.British journal of pharmacology · 2010Review
- The discovery of drugs for obesity, the metabolic effects of leptin and variable receptor pharmacology: perspectives from beta3-adrenoceptor agonists.Naunyn-Schmiedeberg's archives of pharmacology · 2008Review
- Tools to study beta3-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2007Review
- Comparison of three radioligands for the labelling of human beta-adrenoceptor subtypes.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- Effects of gender, age and hypertension on beta-adrenergic receptor function in rat urinary bladder.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- beta-adrenoceptors and potassium channels.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- Alpha1-, alpha2- and beta-adrenoceptors in the urinary bladder, urethra and prostate.British journal of pharmacology · 2006Review
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The beta(1)-adrenoceptor "two-site ligand binding hypothesis" was investigated by comparing the pharmacological activities of the receptor with an Asp to Glu mutation of amino acid 138 after transient transfection into CHO cells. The high-affinity binding of (-)-[(3)H]-CGP12177 (p K(D)=9.4) and binding inhibition by (-)-isoprenaline (p K(i)=6.2), observed with Asp138-beta(1)-adrenoceptors, were absent at Glu138-beta(1)-adrenoceptors. (-)-[(3)H]-CGP12177 bound with a p K(D)=7.6 to Glu138-beta(1)-adrenoceptors and (-)-isoprenaline enhanced binding, probably allosterically. Glu138-beta(1)-adrenoceptors compared with Asp138-beta(1)-adrenoceptors showed a 500,000-fold decrease in cyclic AMP-enhancing potency by (-)-isoprenaline and antagonism by (-)-bupranolol (1 microM) was abolished. At Glu138-beta(1)-adrenoceptors, the agonist potency of (-)-CGP12177, compared with (-)-isoprenaline was reduced five-fold, but the antagonism by (-)-bupranolol (p K(B)=7.1) was not significantly changed, compared with Asp138-beta(1)-adrenoceptor. Thus, Asp138 of the beta(1)-adrenoceptor is essential for the binding of (-)-isoprenaline, (-)-bupranolol and (-)-CGP12177 to a high-affinity site, but not for the binding of (-)-CGP12177 and (-)-bupranolol to a low-affinity site.
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