A More Sustainable Process for Preparation of the Muscarinic Acetylcholine Antagonist Umeclidinium Bromide
Sign Up to like & getrecommendations! Published in 2018 at "ChemMedChem"
DOI: 10.1002/cmdc.201800387
Abstract: A more sustainable process for the synthesis of the long‐acting muscarinic acetylcholine antagonist umeclidinium bromide is described. Specifically, we report the synthesis of ethyl 1‐(2‐chloroethyl)‐4‐piperidinecarboxylate, a key intermediate in the preparation of umeclidinium bromide, in… read more here.
Keywords: sustainable process; muscarinic acetylcholine; process; umeclidinium bromide ... See more keywords
IC/BPS‐associated alterations of M2 and M3 muscarinic acetylcholine receptor trafficking in human detrusor
Sign Up to like & getrecommendations! Published in 2019 at "Neurourology and Urodynamics"
DOI: 10.1002/nau.24087
Abstract: To explore caveolae‐ and clathrin‐mediated internalization of muscarinic M2 and M3 receptors, recycling and degradation in formalin‐fixed paraffin‐embedded detrusor sections; to study alterations possibly involved in the pathophysiology of the bladder functional disorder, interstitial cystitis/bladder… read more here.
Keywords: detrusor; alterations muscarinic; muscarinic acetylcholine; bps associated ... See more keywords
Benefits of long-term pilocarpine due to increased muscarinic acetylcholine receptor 3 in salivary glands.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2018.06.125
Abstract: Hypofunction of the salivary gland causes several life-disrupting side effects such as dental caries, oral candidiasis, loss of taste, and swallowing disorders. No satisfactory therapy has been established to treat salivary hypofunction. Pilocarpine represents a… read more here.
Keywords: administration; pilocarpine; long term; continuous administration ... See more keywords
Rooibos (Aspalathus linearis) extract, containing eriodictyol-6-C-β-d-glucoside as the active component, stimulates exocrine glands via the M3 muscarinic acetylcholine receptor
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Functional Foods"
DOI: 10.1016/j.jff.2019.02.018
Abstract: Abstract We previously discovered that rooibos extract activates the M3 muscarinic acetylcholine receptor (M3R), a key component of exocrine secretion. In this study, we examined the rooibos extract for active components in vitro and monitored… read more here.
Keywords: eriodictyol glucoside; acetylcholine receptor; muscarinic acetylcholine; glucoside active ... See more keywords
Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00192
Abstract: The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) represents a novel potential target for the treatment of multiple addictive disorders, including opioid use disorder. Through chemical optimization of several functional high-throughput screening hits, VU6019650 (27b)… read more here.
Keywords: orthosteric antagonist; acetylcholine receptor; opioid use; use disorder ... See more keywords
Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01812
Abstract: Targeting allosteric sites at M1 muscarinic acetylcholine receptors is a promising strategy for the treatment of Alzheimer's disease. Positive allosteric modulators not only may potentiate binding and/or signaling of the endogenous agonist acetylcholine (ACh) but… read more here.
Keywords: agonist activity; muscarinic acetylcholine; allosteric modulators; synthesis pharmacological ... See more keywords
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M2R Selectivity.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01967
Abstract: Muscarinic acetylcholine receptors (MRs), comprising five subtypes (M1R-M5R) in humans, exhibit a high degree of structural similarity. Therefore, subtype-selective MR agonists and antagonists are lacking. We present an approach to highly M2R-selective MR antagonists based… read more here.
Keywords: conjugation; m2r selectivity; muscarinic acetylcholine; dibenzodiazepinone type ... See more keywords
Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors
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DOI: 10.1038/srep40381
Abstract: Interaction of orthosteric ligands with extracellular domain was described at several aminergic G protein-coupled receptors, including muscarinic acetylcholine receptors. The orthosteric antagonists quinuclidinyl benzilate (QNB) and N-methylscopolamine (NMS) bind to the binding pocket of the… read more here.
Keywords: acetylcholine receptors; acetylcholine; allosteric binding; muscarinic acetylcholine ... See more keywords
Pharmacological and molecular characterization of the A‐type muscarinic acetylcholine receptor from Anopheles gambiae
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DOI: 10.1111/imb.12775
Abstract: Muscarinic acetylcholine receptors (mAChRs) which are G protein‐coupled receptors play key roles in insect physiology. Whereas vertebrate mAChRs are important targets for pharmaceutical drugs, insect mAChRs are under‐exploited by the agro‐chemical industry. Moreover, insect mAChRs… read more here.
Keywords: machr; anopheles gambiae; pharmacological molecular; insect machrs ... See more keywords
Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes
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DOI: 10.1126/science.aaw5188
Abstract: Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs. For… read more here.
Keywords: protein; microscopy; muscarinic acetylcholine; receptor ... See more keywords
Pharmacological Profiling of a Brugia malayi Muscarinic Acetylcholine Receptor as a Putative Antiparasitic Target
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DOI: 10.1128/aac.01188-22
Abstract: The diversification of anthelmintic targets and mechanisms of action will help ensure the sustainable control of nematode infections in response to the growing threat of drug resistance. G protein-coupled receptors (GPCRs) are established drug targets… read more here.
Keywords: malayi; receptor; drug; medicine ... See more keywords