Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor
Journal of Chemical Theory and Computation, 2023 Patient symptom relief is often heavily influenced by the residence time of the inhibitor-target complex. For the human muscarinic receptor 3 (hMR3), tiotropium is a long-acting bronchodilator used in conditions such as asthma or chronic obstructive pulmonary disease (COPD). The mechanistic insights into this inhibitor remain unclear; specifically, the
Buigues, Pedro J. +7 more
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Muscarinic Receptor Agonists and Antagonists [PDF]
Molecules, 2001 A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed.
David R. Kelly, Kenneth J. Broadley
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Evidence for Respiratory Neuromodulator Interdependence after Cholinergic Disruption in the Ventral Respiratory Column [PDF]
, 2015 Reverse dialysis of the muscarinic receptor antagonist, atropine (ATR, 50 mM), into the pre-Bötzinger Complex region of the ventral respiratory column (VRC) of awake and sleeping goats increases breathing frequency and serotonin (5-HT), substance P (SP),
Forster, Hubert +6 more
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State-Dependent and -Independent Effects of Dialyzing Excitatory Neuromodulator Receptor Antagonists into the Ventral Respiratory Column [PDF]
, 2017 Unilateral dialysis of the broad-spectrum muscarinic receptor antagonist atropine (50 mM) into the ventral respiratory column [(VRC) including the pre-Bötzinger complex region] of awake goats increased pulmonary ventilation (V̇i) and breathing frequency (
Burgraff, Nicholas J. +7 more
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Constitutive activity of the M1–M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists [PDF]
, 1995 We investigated whether muscarinic receptors of the M1–M4 receptor subtypes are constitutively active. We have found that the synthesis of cyclic AMP was enhanced by the muscarinic antagonists atropine and N-methylscopolamine (NMS) in Chinese hamster ...
Bačáková, Lucie +3 more
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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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Presynaptic M1 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in the hippocampus in vitro [PDF]
, 1990 The effects of the cholinoceptor agonist, carbachol (CCh), were examined in the rat hippocampal slice preparation. Intracellular recordings from CA1 pyramidal neurones revealed that CCh (1–3 μM) inhibited excitatory postsynaptic responses evoked by ...
Sheridan, Robert D., Sutor, Bernd
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A Cholinergic Synaptically Triggered Event Participates in the Generation of Persistent Activity Necessary for Eye Fixation [PDF]
, 2004 An exciting topic regarding integrative properties of the nervous system is how transient motor commands or brief sensory stimuli are able to evoke persistent neuronal changes, mainly as a sustained, tonic action potential firing.
Alvarado, Juan Carlos +5 more
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Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]
, 2016 Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed +5 more
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Cholinergic suppression: A postsynaptic mechanism of long-term associative learning [PDF]
, 1986 Food avoidance learning in the mollusc Pleurobranchaea entails reduction in the responsiveness of key brain interneurons in the feeding neural circuitry, the paracerebral feeding command interneurons (PCNs), to the neurotransmitter acetylcholine (AcCho).
Davis, W. Jackson +5 more
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