Multitargeting nature of muscarinic orthosteric agonists and antagonists
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
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Mechanisms of Pilocarpine‐Induced Nitric Oxide and Prostaglandin Production in Porcine Ciliary Muscle [PDF]
Pilocarpine, a muscarinic receptor agonist, is clinically used to reduce intraocular pressure via ciliary muscle contraction. However, the intracellular signaling pathways mediating pilocarpine‐induced nitric oxide (NO) and prostaglandin E2 (PGE2 ...
Giovanna Benozzi +3 more
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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 treatment of Alzheimer’s disease are discussed.
David R. Kelly, Kenneth J. Broadley
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Additive interaction of intrathecal ginsenosides and neostigmine in the rat formalin test [PDF]
BackgroundThe authors evaluated the effect of intrathecal mixture of ginsenosides with neostigmine on formalin-induced nociception and made further clear the role of the spinal muscarinic (M) receptors on the activity of ginsenosides.MethodsA catheter ...
Cheon-Hee Park +3 more
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Irritable bowel syndrome (IBS) is a chronic functional bowel disorder characterized by intestinal dysmotility. Changes in intestinal microbiota (dysbiosis) can lead to alterations in neuro-muscular functions in the gut. Toll-like receptors (TLRs) 2 and 4
Elena Layunta +2 more
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Alterations in histamine responses between juvenile and adult urinary bladder urothelium, lamina propria and detrusor tissues [PDF]
Inflammatory mediators may have a role in various lower urinary tract disorders. Histamine is known to induce significant increases in both the tension and frequency of spontaneous phasic contractions in both urothelium with lamina propria (U&LP) and
Chess-Williams, Russ +2 more
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Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor
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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The present study was undertaken to clarify how spinal muscarinic receptors are involved in the antinociceptive effects in thermal stimulation. Intrathecal (i.t.) injection of the muscarinic agonist McN-A-343 inhibited the tail-flick response to noxious ...
Kenji Honda +6 more
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Effects of muscarinic and nicotinic receptors on contextual modulation in macaque area V1
Context affects the salience and visibility of image elements in visual scenes. Collinear flankers can enhance or decrease the perceptual and neuronal sensitivity to flanked stimuli. These effects are mediated through lateral interactions between neurons
Jose L. Herrero, Alexander Thiele
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Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
core +1 more source

