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Dopamine D(2)-D(3) receptor heteromers: pharmacological properties and therapeutic significance
No full textHeteromerization of dopamine receptors has been shown for
both the D1/D5 and D2/D3/D4 receptor families, which couple
positively and negatively, respectively, to adenylyl cyclase.
The present article reviews data on dopamine heteromers
formed by D3, focusing in particular on associations with
their D2 counterparts. Certain antiparkinsonian agents,
like the preferential and high efficacy D3 > D2 agonists,
pramipexole, and ropinirole, show amplified potency
at D2–D3 heteromers versus constituent monomers.
Accordingly, in cells cotransfected with D2 and D3 receptors,
pramipexole, and ropinirole suppress forskolin (FK)-
stimulated cAMP production with higher potencies as
compared to cells transfected with D2 or D3 receptors only.
Furthermore, in cells cotransfected with D2 and an excess
of D3 receptors, the partial agonists aripiprazole, S33592,
bifeprunox, N-desmethylclozapine, and preclamol lose
agonist properties and abolish the actions of quinpirole.
Then, partial agonists are transformed into antagonists
upon cotransfection of D2 with an excess of D3 receptors.
A hypothetical relationship of the above observations to the
pathophysiology and possibly treatment of neuropsychiatric
diseases is discussed
Seizure evoked from area tempestas are subject to control by GABA and glutamate receptor in substantia nigra.
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Role of excitatory amino-acids in diethyldithiocarbamate-induced cell death in mesencephalic cultures
No full textReconstituition of functional muscarinic receptors by coexpression of amino and carboxyl terminal receptor fragments
No full textFunctional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studies by mutational analysis of the m3 muscarinic receptor
No full textL-Deprenyl fails to protect mesencephalic dopamine neurons and PC12 cells from the neurotoxic effect of 1-methyl-4-phenylpyridinium ion
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