Merck
CN
Search Within

M105

应用筛选条件
关键词:'M105'
显示 1-30 共 48 条结果 关于 "M105" 范围 论文
T L Borella et al.
British journal of pharmacology, 155(8), 1256-1263 (2008-09-30)
Recent evidence has suggested that pilocarpine (ACh receptor agonist) injected peripherally may act centrally producing salivation and hypertension. In this study, we investigated the effects of specific M(1) (pirenzepine), M(2)/M(4) (methoctramine), M(1)/M(3) (4-DAMP) and M(4) (tropicamide) muscarinic receptor subtype antagonists
Lisbeth E Gómez-Martínez et al.
Behavioural brain research, 203(2), 247-255 (2009-05-20)
The role of cholinergic neurotransmission in male rat sexual behavior at the brain level has been studied by several researchers. However, little is known about its role at the spinal cord level. In this study, the effects of the intrathecal
Andrei N Tsentsevitsky et al.
Neuroscience letters, 649, 62-69 (2017-04-15)
Muscarinic cholinoreceptors regulate the neurosecretion process in vertebrate neuromuscular junctions. The diversity of muscarinic effects on acetylcholine (ACh) secretion may be attributed to the different muscarinic subtypes involved in this process. In the present study, the location of five muscarinic
Laura Nadal et al.
Developmental neuroscience, 38(6), 407-419 (2017-04-27)
The development of the nervous system involves the initial overproduction of synapses, which promotes connectivity. Hebbian competition between axons with different activities leads to the loss of roughly half of the overproduced elements and this refines connectivity. We used quantitative
Joe S Matarlo et al.
Cell chemical biology, 26(8), 1133-1142 (2019-06-04)
Identification of RNA-interacting pharmacophores could provide chemical probes and, potentially, small molecules for RNA-based therapeutics. Using a high-throughput differential scanning fluorimetry assay, we identified small-molecule natural products with the capacity to bind the discrete stem-looped structure of pre-miR-21. The most
Clarissa Muere et al.
Respiratory physiology & neurobiology, 205, 7-15 (2014-09-30)
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), glycine, and GABA concentrations
Elaine Campana Sanches Bornia et al.
Journal of anesthesia, 23(4), 513-519 (2009-11-19)
We investigated whether presynaptic facilitatory M1 and/or inhibitory M2 muscarinic receptors contributed to pancuronium- and cisatracurium-induced tetanic fade. Phrenic nerve-diaphragm muscle preparations of rats were indirectly stimulated with tetanic frequency (75 +/- 3.3 Hz; mean +/- SD). Doses of pancuronium
Mary A Lung
American journal of rhinology & allergy, 25(2), e60-e65 (2011-06-18)
Acetylcholine (ACh) has been shown to induce nasal congestion via vasorelaxation of intranasal posterior collecting veins (PCV) coupled with vasocontraction of extranasal outflow veins (dorsal nasal vein [DNV] and sphenopalatine vein [SPV]). The aim of this study was to characterize
Binding and functional characterization of the cardioselective muscarinic antagonist methoctramine.
Giraldo E
Journal of Pharmacology and Experimental Therapeutics, 244(3), 1016-1020 (1988)
Yoshihiro Matsumoto et al.
Urology, 79(5), 1184-1184 (2012-03-06)
To evaluate the role of M2 and M3 muscarinic acetylcholine receptor (mAChR) subtypes in the activation of bladder afferent pathways in rats with chronic spinal cord injury (SCI). Adult female Sprague-Dawley rats were spinalized at the T9 level. Continuous cystometry
Dina M Jragh et al.
Medical principles and practice : international journal of the Kuwait University, Health Science Centre, 20(6), 530-537 (2011-10-12)
Carbachol-induced contraction of the rat colon is impaired in rats with trinitrobenzene sulfonic acid (TNBS)-induced colitis. The main objective of this study was to examine the effect of colitis on the expression and function of muscarinic (M) receptor subtypes in
G Villetti et al.
The Journal of pharmacology and experimental therapeutics, 335(3), 622-635 (2010-09-02)
The novel quaternary ammonium salt (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino]carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407) showed subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2), and M3 (hM3) receptors and dissociated very slowly from hM3 receptors (t(½) = 166 min) with a large part of the receptorial
Kyungpyo Park et al.
Molecular immunology, 56(4), 583-587 (2013-08-06)
Impairment of gastrointestinal tract (GI) function, including delayed gastric emptying and colonic dysmotility, are common features of primary Sjögren's syndrome (SS). However, the pathogenesis remains largely unknown. The aim of the current study was to investigate the role of functional
J Wess et al.
Naunyn-Schmiedeberg's archives of pharmacology, 338(3), 246-249 (1988-09-01)
The antimuscarinic effects of methoctramine (N, N'-bis[6-[(2-methoxybenzyl)amino]hexyl]-1, 8-octanediamine tetrahydrochloride), a polymethylene tetraamine endowed with high cardioselectivity in vitro, were assessed in two in vivo preparations. Methoctramine (300 micrograms/kg i.v.) strongly inhibited the methacholine- and muscarine-induced bradycardia in the anaesthetized an
Megan C Wright et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 29(47), 14942-14955 (2009-11-27)
Muscarinic acetylcholine receptors (mAChRs) modulate synaptic function, but whether they influence synaptic structure remains unknown. At neuromuscular junctions (NMJs), mAChRs have been implicated in compensatory sprouting of axon terminals in paralyzed or denervated muscles. Here we used pharmacological and genetic
John S Young et al.
BJU international, 110(8 Pt B), E397-E401 (2012-03-01)
To determine whether muscarinic receptor antagonism affects stretching-induced release of ATP. Mucosal strips, dissected from guinea pig (male, 450g; n = 10) urinary bladders, were placed in horizontal organ baths and superfused with Ca(2+) -free Tyrode's solution. Superfusate samples were
Elisabetta Coppi et al.
Journal of neurochemistry, 157(4), 1182-1195 (2020-10-09)
The Nucleus Basalis of Meynert (NBM) is the main source of cholinergic neurons in the basal forebrain to be crucially involved in cognitive functions and whose degeneration correlates with cognitive decline in major degenerative pathologies as Alzheimer's and Parkinson's diseases.
Polymethylene tetraamines: a novel class of cardioselective M2-antagonists.
C Melchiorre
Medicinal research reviews, 10(3), 327-349 (1990-07-01)
Maddalena Zini et al.
Chemico-biological interactions, 181(3), 409-416 (2009-07-07)
Methoctramine and its analogues are polymethylene tetramines that selectively bind to a variety of receptor sites. Although these compounds are widely used as pharmacological tools for receptor characterization, the toxicological properties of these polyamine-based structures are largely unknown. We have
Jan Jakubík et al.
Molecular pharmacology, 86(2), 180-192 (2014-05-30)
Methoctramine (N,N'-bis[6-[[(2-methoxyphenyl)-methyl]hexyl]-1,8-octane] diamine) is an M(2)-selective competitive antagonist of muscarinic acetylcholine receptors and exhibits allosteric properties at high concentrations. To reveal the molecular mechanisms of methoctramine binding and selectivity we took advantage of reciprocal mutations of the M(2) and M(3)
Presynaptic Muscarinic Acetylcholine Receptors and TrkB Receptor Cooperate in the Elimination of Redundant Motor Nerve Terminals during Development.
Nadal L
Frontiers in Aging Neuroscience, 9, 24-24 (2017)
J Di Salvo et al.
The Journal of pharmacology and experimental therapeutics, 360(2), 346-355 (2016-12-15)
Although the physiologic role of muscarinic receptors in bladder function and the therapeutic efficacy of muscarinic antagonists for the treatment of overactive bladder are well established, the role of β
Ryo Orii et al.
Bioscience trends, 4(5), 260-266 (2010-11-12)
Information about the muscarinic receptor subtype(s) mediating pulmonary circulatory vasodilator responses to acetylcholine (ACh) is limited. The aim of this study was to pharmacologically characterize the muscarinic receptors associated with ACh-induced pulmonary vasodilation in a pulmonary hypertension model. Vasodilation of
Christian Moro et al.
Urology, 78(6), 1442-1442 (2011-10-18)
To investigate the effects of tissue stretch and muscarinic receptor stimulation on the spontaneous activity of the urothelium/lamina propria and identify the specific receptor subtype mediating these responses. Isolated strips of porcine urothelium with lamina propria were set up for
Neus Garcia et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 30(49), 16514-16522 (2010-12-15)
The neurotrophin brain-derived neurotrophic factor (BDNF), neurotrophin-4 (NT-4) and the receptors tropomyosin-related kinase B (trkB) and p75(NTR) are present in the nerve terminals on the neuromuscular junctions (NMJs) of the levator auris longus muscle of the adult mouse. Exogenously added
Tatiana S Filatova et al.
Journal of physiology and biochemistry, 73(2), 167-174 (2016-11-20)
Electrophysiological effects produced by selective activation of M3 cholinoreceptors were studied in isolated left atrium preparations from rat using the standard sharp glass microelectrode technique. The stimulation of M3 receptors was obtained by application of muscarinic agonist pilocarpine (10
Klaus Deckmann et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 32(6), 2903-2910 (2018-02-07)
We have recently identified a cholinergic chemosensory cell in the urethral epithelium, urethral brush cell (UBC), that, upon stimulation with bitter or bacterial substances, initiates a reflex detrusor activation. Here, we elucidated cholinergic mechanisms that modulate UBC responsiveness. We analyzed
Aclidinium inhibits human lung fibroblast to myofibroblast transition.
Milara J
Thorax, 67(3), 229-237 (2012)
Da-wei Sun et al.
Chinese medical journal, 122(9), 1049-1055 (2009-06-06)
Ca(2+) in the central nervous system plays important roles in brain physiology, including neuronal survival and regeneration in rats with injured facial motoneurons. The present research was to study the modulations of intracellular free Ca(2+) concentrations by cholinergic receptors in
Yulia V Dobryakova et al.
Acta neurobiologiae experimentalis, 78(2), 132-139 (2018-07-19)
Muscarinic acetylcholine receptors (mAChR) are known to be related to learning and memory processes. Inactivation of mAChR by cholinergic antagonists have been shown to produce amnesia in a variety of behavioral tasks. In this study, we investigated the role of
1/2