ArticleBritish journal of pharmacology2000
Disparate ligand-mediated Ca(2+) responses by wild-type, mutant Ser(200)Ala and Ser(204)Ala alpha(2A)-adrenoceptor: G(alpha15) fusion proteins: evidence for multiple ligand-activation binding sites.
Article in British journal of pharmacology, 2000. 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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8 citing papers in PubMed, 20 citations in OpenAlex.
- Neuropharmacological Effects of the Dichloromethane Extract from the Stems ofPharmaceuticals (Basel, Switzerland) · 2023Article
- Ligands of Adrenergic Receptors: A Structural Point of View.Biomolecules · 2021Review
- Activation of the αNature chemical biology · 2020Article
- Remote control of neuronal signaling.Pharmacological reviews · 2011Review
- Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine.ACS chemical neuroscience · 2010Article
- Engineered G-protein Coupled Receptors are Powerful Tools to Investigate Biological Processes and Behaviors.Frontiers in molecular neuroscience · 2009Article
- Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand.Proceedings of the National Academy of Sciences of the United States of America · 2007Article
- Partial to complete antagonism by putative antagonists at the wild-type alpha(2C)-adrenoceptor based on kinetic analyses of agonist:antagonist interactions.British journal of pharmacology · 2000Article
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2 authors at 2 institutions in 2 countries.
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Abstract
Ligand : receptor interactions were analysed at wt, mutant Ser(200)Ala and Ser(204)Ala alpha(2A) ARs by measuring Ca(2+) responses in CHO-K1 cells either by co-expression with a G(alpha15) protein or at a receptor : G(alpha15) protein stoichiometry of 1.0 using fusion proteins. The magnitude of the UK 14304-mediated Ca(2+) response as elicited by a G(alpha15) protein was largest with both mutant Ser(200)Ala and Ser(204)Ala alpha(2A)ARs compared to the wt alpha(2A) AR in the co-expression and fusion protein experiments. The activation profiles of the wt and both mutant alpha(2A) ARs as analysed by a series of alpha(2) AR agonists differed. d-Medetomidine and clonidine appeared most efficacious at the Ser(204)Ala alpha(2A) AR, whereas oxymetazoline was also partially active at the Ser(200)Ala alpha(2A) AR. Talipexole was silent at both mutant alpha(2A) ARs. The intrinsic activity of (-)-adrenaline was either absent or partial at the Ser(204)Ala and Ser(200)Ala alpha(2A) AR, respectively. This latter observation is related to its lower binding affinity for both mutant alpha(2A) ARs. Ligands characterized as antagonists at wt and Ser(200)Ala alpha(2A) ARs demonstrated either no intrinsic activity (i.e., RX 811059) or positive efficacy with a different rank order of maximal response at the Ser(204)Ala alpha(2A) AR (atipamezole=SKF 86466=idazoxan>dexefaroxan) than Asp(79)Asn alpha(2A) AR (atipamezole>idazoxan approximately SKF 86466>dexefaroxan) and Thr(373)Lys alpha(2A) AR (SKF 86466>atipamezole approximately idazoxan>dexefaroxan). These effects were only observed in the co-expression experiments at concentrations in line with their binding affinities. In conclusion, these Ca(2+) data suggest that multiple activation binding sites exist for these ligands at the alpha(2A) AR, and that their activation may be affected in different ways by the mutations being investigated.
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