Medizinische Universität Graz - Research portal
Selected Publication:
SHR Neuro Cancer Cardio Lipid Metab Microb
Czermak, C; Lehofer, M; Liebmann, PM; Traynor, J.
35SGTPgammaS binding at the human dopamine D4 receptor variants hD4.2, hD4.4 and hD4.7 following stimulation by dopamine, epinephrine and norepinephrine.
Eur J Pharmacol. 2006; 531(1-3):20-24
Doi: 10.1016/j.ejphar.2005.11.063
Web of Science
PubMed
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- Co-authors Med Uni Graz
- Liebmann-Holzmann Peter
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- Abstract:
- Aim of the present study was to investigate possible differences between the human dopamine D4 receptor 48 bp polymorphism variants hD4.2, hD.4. and hD4.7 in agonist stimulated [35S]GTPgammaS binding, to investigate dopamine D4 receptor sodium sensitivity and to further characterize norepinephrine and epinephrine agonism at this receptor. G-protein activation at the receptor variants hD4.2, hD4.4 and hD4.7 expressed in CHO-K1 cells, following stimulation by dopamine, norepinephrine and epinephrine, was investigated using the [35S]GTPgammaS assay at experimental conditions of 10 and 100 mM sodium, respectively. Dopamine displayed a 2 fold higher potency of stimulating [35S]GTPgammaS binding at the hD4.2, compared to the hD4.4 and hD4.7 at 10 mM sodium. A significant difference in sodium sensitivity of basal [35S]GTPgammaS binding was found, with the hD4.7 being 1.7 fold more sensitive than the hD4.4 and 2.5 fold more sensitive than the hD4.2. Norepinephrine and epinephrine both produced concentration-dependent increases in [35S]GTPgammaS binding at all three receptor variants, and epinephrine showed only 2 fold less potency than dopamine. The present results are in certain line with previous reports of functional 2-3 fold differences between the dopamine D4 receptor variants. Agonism of norepinephrine and epinephrine at the dopamine D4 receptor may indicate an important way of cross-reactivity among the different monoamine neurotransmitter systems.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Binding, Competitive - drug effects
- CHO Cells - drug effects
- Catecholamines - pharmacology
- Cell Membrane - drug effects
- Cricetinae - drug effects
- Cricetulus - drug effects
- Dopamine - pharmacology
- Dopamine Agonists - pharmacology
- Dose-Response Relationship, Drug - pharmacology
- Epinephrine - pharmacology
- Guanosine 5'-O-(3-Thiotriphosphate) - metabolism
- Humans - metabolism
- Norepinephrine - pharmacology
- Polymorphism, Genetic - pharmacology
- Receptors, Dopamine D4 - genetics
- Sodium Chloride - pharmacology
- Sulfur Radioisotopes - pharmacology
- Find related publications in this database (Keywords)
- dopamine D4 receptor
- polymorphism
- norepinephrine
- epinephrine
- [S-35]GTP gamma S
- sodium