Results 1 to 10 of about 27,985 (262)
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.
Kenneth J. Broadley, David R. Kelly
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Isomerization of the muscarinic receptor . antagonist complex.
Journal of Biological Chemistry, 1979 The mechanism of binding of two antagonists, 3-quinuclidinyl benzilate and N-methyl-4-piperidinyl benzilate, to the muscarinic receptor was studied. The pseudo-first order rate constant of association showed a hyperbolic dependence on the concentration of the antagonist(s) indicating that the interaction involves two equilibria.
Jaak Järv +2 more
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Multitargeting nature of muscarinic orthosteric agonists and antagonists
Frontiers in Physiology, 2022 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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Molecular probes for muscarinic receptors: Functionalized congeners of selective muscarinic antagonists [PDF]
Life Sciences, 1995 The muscarinic agonist oxotremorine and the tricyclic muscarinic antagonists pirenzepine and telenzepine have been derivatized using a functionalized congener approach for the purpose of synthesizing high affinity ligand probes that are suitable for conjugation with prosthetic groups, for receptor cross-linking, fluorescent and radioactive detection ...
Kenneth A. Jacobson +2 more
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Migrastatin Acts as a Muscarinic Acetylcholine Receptor Antagonist [PDF]
The Journal of Antibiotics, 2006 Migrastatin and its analogs have various biological activities such as inhibition of cell migration and anchorage-independent growth of cancer cells. Although its biosynthesis and chemical synthesis have been under investigation, little is known about the biological target of migrastatin.
Koichi Nakae +3 more
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Practical considerations when prescribing a long-acting muscarinic antagonist for patients with COPD. [PDF]
Int J Chron Obstruct Pulmon Dis, 2018 D'Urzo AD, Kardos P, Wiseman R.
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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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Additive interaction of intrathecal ginsenosides and neostigmine in the rat formalin test [PDF]
Korean Journal of Anesthesiology, 2013 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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Cells, 2022 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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Journal of Pharmacological Sciences, 2008 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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