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Interaction Studies of Multiple Binding Sites on M4 Muscarinic Acetylcholine Receptors
Molecular Pharmacology, 2006This study investigated the reciprocal cross-interactions between two distinct allosteric sites on the M(4) muscarinic acetylcholine receptor (mAChR) in the absence or presence of different orthosteric ligands. Initial studies revealed that two novel benzimidazole allosteric modulators, 17-beta-hydroxy-17-alpha-ethy nyl-delta(4)-androstano[3,2-b ...
Alfred A, Lanzafame +2 more
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Muscarinic M4 receptor inhibition of dopamine D1-like receptor signalling in rat nucleus accumbens
European Journal of Pharmacology, 2002Several studies have indicated the occurrence of an antagonistic interaction between muscarinic and dopamine D1-like receptors in the ventral striatum, but the subtype(s) of muscarinic receptor involved has not been characterized. We show that in membranes of rat nucleus accumbens, carbachol inhibited the stimulation of adenylyl cyclase activity by ...
ONALI, PIER LUIGI +1 more
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Brain Research, 2001
The striatum has nearly equal numbers of striatonigral and striatopallidal projection neurons. All are GABAergic and inhibitory, but they lie in separate neuronal circuits ('direct' and 'indirect', respectively) that appear to exert opposite effects on movement. Methods are needed to evaluate the function of each circuit.
M P, Santiago, L T, Potter
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The striatum has nearly equal numbers of striatonigral and striatopallidal projection neurons. All are GABAergic and inhibitory, but they lie in separate neuronal circuits ('direct' and 'indirect', respectively) that appear to exert opposite effects on movement. Methods are needed to evaluate the function of each circuit.
M P, Santiago, L T, Potter
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Molecular Pharmacology, 1996
We analyzed the role of receptor internalization and recycling in muscarinic acetylcholine receptor (mAChR) desensitization and resensitization. Incubation of Chinese hamster ovary cells stably expressing the m4 mAChR with 1 mM carbachol for 1 hr reduced cell surface receptor number by 50-60% with no change in total receptor number. Pretreatment of the
G S, Bogatkewitsch +3 more
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We analyzed the role of receptor internalization and recycling in muscarinic acetylcholine receptor (mAChR) desensitization and resensitization. Incubation of Chinese hamster ovary cells stably expressing the m4 mAChR with 1 mM carbachol for 1 hr reduced cell surface receptor number by 50-60% with no change in total receptor number. Pretreatment of the
G S, Bogatkewitsch +3 more
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M4 Muscarinic Acetylcholine Receptor Modulation of Dopamine Receptor Functions
2017M4 muscarinic acetylcholine receptors (mAChRs) belong to the Rhodopsin family of G protein-couple receptors. These receptors are found most abundantly in the striatum and are implicated in a number of central nervous system disorders, including schizophrenia.
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Contraction of guinea-pig gallbladder: muscarinic M3 or M4 receptors?
European Journal of Pharmacology, 1997The muscarinic receptor mediating contraction of the guinea-pig isolated gallbladder, currently being disputed to belong either to the M3 or M4 subtype, was characterized by subtype-preferring agonists and discriminating antagonists. Highly significant correlations of agonist potencies to contract the gallbladder, e.g., arecaidine propargyl ester ...
M, Eltze +3 more
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Life Sciences, 1999
In membranes of Chinese hamster ovary cells expressing the cloned human M1-M4 muscarinic receptor subtypes, PD 102807, a novel M4 selective antagonist, was found to counteract the M4 receptor-induced stimulation of [35S]-GTPgammaS binding to membrane G proteins with a pK(B) of 7.40, a value which was 63-, 33- and 10-fold higher than those displayed at ...
OLIANAS, MARIA CONCETTA +1 more
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In membranes of Chinese hamster ovary cells expressing the cloned human M1-M4 muscarinic receptor subtypes, PD 102807, a novel M4 selective antagonist, was found to counteract the M4 receptor-induced stimulation of [35S]-GTPgammaS binding to membrane G proteins with a pK(B) of 7.40, a value which was 63-, 33- and 10-fold higher than those displayed at ...
OLIANAS, MARIA CONCETTA +1 more
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Enhanced self-administration of alcohol in muscarinic acetylcholine M4 receptor knockout mice
European Journal of Pharmacology, 2015Modulation of cholinergic neurotransmission via nicotinic acetylcholine receptors is known to alter alcohol-drinking behavior. It is not known if muscarinic acetylcholine receptor subtypes have similar effects. The muscarinic M4 receptor is highly expressed in the brain reinforcement system and involved in regulation of cholinergic and dopaminergic ...
de la Cour, Cecilie +6 more
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Use of Antimuscarinic Toxins To Facilitate Studies of Striatal m4 Muscarinic Receptors
The Journal of Pharmacology and Experimental Therapeutics, 1998Striatal m4 muscarinic receptors are important because their blockade controls movement, and they are preferentially located on striatal neurons that project to the internal globus pallidus. The following studies were performed in vitro to provide a basis for using antimuscarinic toxins to study the effects of selective m4 blockade on movement in vivo.
S L, Purkerson, L T, Potter
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Muscarinic M4 Receptor Recycling Requires a Motif in the Third Intracellular Loop
The Journal of Pharmacology and Experimental Therapeutics, 2008The present study was performed to identify sequence(s) in the third intracellular loop (i3) of the muscarinic acetylcholine receptor M4 subtype (M4 receptor) involved in its internalization and recycling. In transiently transfected human embryonic kidney 293-tsA201 cells, 40 to 50% of cell-surface M4 receptors are internalized in an agonist-dependent ...
Yuichi, Hashimoto +5 more
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