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Interactions between histamine H3 and dopamine D2 receptors and the implications for striatal function
Carla Ferrada1, Sergi Ferré, Vicent Casadó
1Institut d'Investigacions Biomèdiques August Pi i Sunyer, Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas, University of Barcelona, 08028 Barcelona, Spain.
Neuropharmacology
|June 13, 2008
Summary
Histamine H(3) receptors in the striatum modulate dopamine D(1) and D(2) receptor activity. These receptors interact postsynaptically and form heteromers with D(2) receptors, influencing motor control.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- The role of histamine H(3) receptors in the striatum is not well understood.
- Previous research shows conflicting results on H(3) and dopamine D(2) receptor interactions.
Purpose of the Study:
- To investigate the functional interactions between striatal histamine H(3) and dopamine D(1)/D(2) receptors.
- To explore the molecular basis of H(3)-D(2) receptor interactions.
Main Methods:
- Behavioral studies in reserpinized mice using receptor agonists and antagonists.
- Radioligand binding assays in striatal membrane preparations.
- Bioluminescence Resonance Energy Transfer (BRET) in co-transfected HEK-293 cells.
Main Results:
- Histamine H(3) receptors exhibit antagonistic postsynaptic interactions with both dopamine D(1) and D(2) receptors.
- H(3) receptor stimulation negatively modulates D(2) receptor affinity.
- Histamine H(3) and dopamine D(2) receptors form functional heteromers.
Conclusions:
- Postsynaptic histamine H(3) receptors play a significant role in modulating striatal dopaminergic transmission.
- H(3)-D(2) receptor heteromerization is a key mechanism for this modulation.
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