A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]
, 2017 The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi +6 more
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Striatal cholinergic interneurons generate beta and gamma oscillations in the corticostriatal circuit and produce motor deficits [PDF]
, 2016 Cortico-basal ganglia-thalamic (CBT) neural circuits are critical modulators of cognitive and motor function. When compromised, these circuits contribute to neurological and psychiatric disorders, such as Parkinson's disease (PD).
Bucklin, Mark +5 more
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Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma? [PDF]
, 2014 The authors acknowledge the medical writing assistance received from Sam Yarwood, PhD, of Complete HealthVizion, in the form of literature searches and preparation and revision of the draft manuscript.Peer reviewedPublisher ...
Fromer, Leonard +4 more
core +10 more sources
Cholinergic modulation of dopamine overflow in the rat neostriatum: A fast cyclic voltammetric study in vitro [PDF]
, 1994 Stimulus-evoked dopamine overflow in rat neostriatal slices was determined using fast cyclic voltammetry. The dopamine efflux induced by intrastriatal stimulation increased with stimulus intensity and was found to be enhanced by more than 100% upon ...
Kudernatsch, Martina, Sutor, Bernd
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Proceedings of the National Academy of Sciences of the United States of America, 2018 Significance The orthosteric binding sites of the five muscarinic acetylcholine receptor (mAChR) subtypes are highly conserved, making the development of selective antagonists challenging.
M. Korczynska +17 more
semanticscholar +1 more source
Alpha9 nicotinic acetylcholine receptors and the treatment of pain [PDF]
, 2009 Chronic pain is a vexing worldwide problem that causes substantial disability and consumes significant medical resources. Although there are numerous analgesic medications, these work through a small set of molecular mechanisms.
Absalom, Nathan +4 more
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Investigative Ophthalmology and Visual Science, 2018 Purpose Myopia is a refractive disorder that degrades vision. It can be treated with atropine, a muscarinic acetylcholine receptor (mAChR) antagonist, but the mechanism is unknown. Atropine may block α-adrenoceptors at concentrations ≥0.1 mM, and another
Brittany J. Carr +6 more
semanticscholar +1 more source
New and developing non-adrenoreceptor small molecule drugs for the treatment of asthma [PDF]
, 2017 Introduction: Inhaled corticosteroids (ICS) alone or in combination with an inhaled long-acting beta2-agonist (LABA) are the preferred long-term treatment for adults and adolescents with symptomatic asthma.
Thomson, Neil C.
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Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists
Proceedings of the National Academy of Sciences of the United States of America, 2018 Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes.
Hongtao Liu +19 more
semanticscholar +1 more source
A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart [PDF]
, 1982 These experiments employ the photoisomerizable compound, 3,3'-bis- [alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), to study the response to muscarinic agents in frog myocardium. In homogenates from the heart, trans-Bis-Q blocks the binding of [3H]-N-
Birdsall, Nigel J. M. +5 more
core +1 more source