Muscarinic Receptor Agonists and Antagonists [PDF]
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 ...
David R. Kelly, Kenneth J. Broadley
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Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor. [PDF]
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 PJ +7 more
europepmc +4 more sources
Katayama et al. report a vibrational spectroscopic study using ATR–FTIR of the human M2 muscarinic acetylcholine receptor (M2R). Their work involves an extensive comparison of agonists, antagonists, and inverse agonists, in which they show that they C ...
Kota Katayama +8 more
doaj +1 more source
Lung cancer is the leading cause of cancer death worldwide and new treatment strategies are clearly needed. The recent discovery that lung and other cancers synthesize and secrete acetylcholine (ACh) which acts as an autocrine growth factor suggests that
Therapy Pingfang Song, Eliot R. Spindel
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Evidence for Respiratory Neuromodulator Interdependence after Cholinergic Disruption in the Ventral Respiratory Column [PDF]
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
core +2 more sources
A Cholinergic Synaptically Triggered Event Participates in the Generation of Persistent Activity Necessary for Eye Fixation [PDF]
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, JC +5 more
core +5 more sources
New and developing non-adrenoreceptor small molecule drugs for the treatment of asthma [PDF]
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.
core +1 more source
State-Dependent and -Independent Effects of Dialyzing Excitatory Neuromodulator Receptor Antagonists into the Ventral Respiratory Column [PDF]
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
core +2 more sources
Cholinergic Regulation of Orexin/Hypocretin Neurons Through M3Muscarinic Receptor in Mice
The cholinergic system plays an important role in regulation of arousal and REM sleep. In the present study, we showed that a muscarinic receptor agonist, carbachol (CCh), activates almost 20% of orexin-producing neurons (orexin neurons), which play a ...
Kousaku Ohno +2 more
doaj +1 more source
Clinical Factors Associated With Dose Escalation of Solifenacin for the Treatment of Overactive Bladder in Real Life Practice [PDF]
PurposeTo determine the baseline clinical characteristics associated with dose escalation of solifenacin in patients with overactive bladder (OAB).MethodsWe analyzed the data of patients with OAB (micturition frequency ≥8/day and urgency ≥1/day) who were
Ji-Youn Chun +5 more
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