Thymol as a Potential Natural Antiemetic: Insights From In Vivo and In Silico Studies. [PDF]
According to the study, thymol (THY) greatly decreased retches and enhanced latency in a model of chick emesis; the highest effectiveness was shown at 20 mg/kg. According to molecular docking, THY binds strongly to important emetic receptors (5‐HT3A, D2, M3, and H1), indicating a multi‐target mechanism.
Akbor S+11 more
europepmc +2 more sources
Identification and Molecular Characterization of m3 Muscarinic Receptor Dimers [PDF]
Several studies suggest, but do not prove directly, that muscarinic receptors may be able to form dimeric or oligomeric arrays. To address this issue in a more direct fashion, we designed a series of biochemical experiments using a modified version of the rat m3 muscarinic receptor (referred to as m3') as a model system.
Fu-Yue Zeng, Jürgen Wess
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Expression of M3 muscarinic acetylcholine receptors in gastric cancer
Gastric cancer represents a real public health problem as far as incidence, aggressiveness and unfavorable prognosis are concerned. The autonomous nervous system might be one of the major factors involved in the onset, progression, and metastasis, both sympathetically and parasympathetically.
Mehedinţeanu, Alina Maria+9 more
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Solifenacin-induced acute psychosis: a case report
Solifenacin is a muscarinic receptor antagonist that has been used to treat overactive bladder since 2004. It has a great affinity for the detrusor M3 receptor, which must be stimulated for bladder muscle contraction, and demonstrates the most selective ...
Betul Kirsavoglu+2 more
doaj +1 more source
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
doaj +1 more source
Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi+5 more
doaj +1 more source
Targeting M3 Muscarinic Receptors for Colon Cancer Therapy [PDF]
Expression and activation of subtype-3 muscarinic receptors (M3R) plays an important role in the progression of colorectal neoplasia.Herein, we describe the role of muscarinic receptors in colon cancer, focusing specifically on M3R, illustrate how M3R over-expression and activation of post-receptor signaling pathways potentiates tumor progression, and ...
Shien Hu+2 more
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Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa+3 more
core +1 more source
.: In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). Alteration of tumor growth
Nozomi Ami+5 more
doaj +1 more source
Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]
Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa+3 more
core +2 more sources