Results 11 to 20 of about 43,320 (312)

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 ...
David R. Kelly, Kenneth J. Broadley
doaj   +2 more sources

Investigating the Unbinding of Muscarinic Antagonists from the Muscarinic 3 Receptor. [PDF]

J Chem Theory Comput, 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 PJ, Gehrke S, Badaoui M, Dudas B, Mandana G, Qi T, Bottegoni G, Rosta E.   +7 more
europepmc   +4 more sources

State-Dependent and -Independent Effects of Dialyzing Excitatory Neuromodulator Receptor Antagonists into the Ventral Respiratory Column [PDF]

, 2017
Unilateral dialysis of the broad-spectrum muscarinic receptor antagonist atropine (50 mM) into the ventral respiratory column [(VRC) including the pre-Bötzinger complex region] of awake goats increased pulmonary ventilation (V̇i) and breathing frequency (
Burgraff, Nicholas J., Crumley, Emma, Forster, Hubert V., Hodges, Matthew R., Langer, Thomas M., III, Neumueller, Suzanne E., Pan, Lawrence, Talwar, Sawan   +7 more
core   +2 more sources

A molecular basis for selective antagonist destabilization of dopamine D3 receptor quaternary organization [PDF]

, 2017
The dopamine D3 receptor (D3R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a ...
Caltabiano, Gianluigi, Jiménez-Rosés, Mireia, Marsango, Sara, Millan, Mark J., Milligan, Graeme, Pediani, John D., Ward, Richard J.   +6 more
core   +2 more sources

Cholinergic Regulation of Orexin/Hypocretin Neurons Through M3Muscarinic Receptor in Mice

Journal of Pharmacological Sciences, 2008
The cholinergic system plays an important role in regulation of arousal and REM sleep. In the present study, we showed that a muscarinic receptor agonist, carbachol (CCh), activates almost 20% of orexin-producing neurons (orexin neurons), which play a ...
Kousaku Ohno, Mari Hondo, Takeshi Sakurai   +2 more
doaj   +1 more source

Clinical Factors Associated With Dose Escalation of Solifenacin for the Treatment of Overactive Bladder in Real Life Practice [PDF]

International Neurourology Journal, 2014
PurposeTo determine the baseline clinical characteristics associated with dose escalation of solifenacin in patients with overactive bladder (OAB).MethodsWe analyzed the data of patients with OAB (micturition frequency ≥8/day and urgency ≥1/day) who were
Ji-Youn Chun, Miho Song, Ji-Yeon Han, Selee Na, Bumsik Hong, Myung-Soo Choo   +5 more
doaj   +1 more source

Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]

, 2016
Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed, Al-Abed, Yousef, Coleman, Thomas, Lakshminrusimha, Satyanarayana, Patel, Hardik, VanPatten, Sonya   +5 more
core   +2 more sources

Cholinergic suppression: A postsynaptic mechanism of long-term associative learning [PDF]

, 1986
Food avoidance learning in the mollusc Pleurobranchaea entails reduction in the responsiveness of key brain interneurons in the feeding neural circuitry, the paracerebral feeding command interneurons (PCNs), to the neurotransmitter acetylcholine (AcCho).
Davis, W. Jackson, Kovac, Mark P., Matera, Eugene M., McCormack, Kenneth J., Morielli, Anthony D., Shrum, Richard G.   +5 more
core   +2 more sources

Selective M3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model

Journal of Pharmacological Sciences, 2011
.: 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, Kazumi Koga, Hiroshi Fushiki, Yoko Ueno, Yoshio Ogino, Hisashi Ohta   +5 more
doaj   +1 more source

Muscarinic Acetylcholine Type 1 Receptor Activity Constrains Neurite Outgrowth by Inhibiting Microtubule Polymerization and Mitochondrial Trafficking in Adult Sensory Neurons

Frontiers in Neuroscience, 2018
The muscarinic acetylcholine type 1 receptor (M1R) is a metabotropic G protein-coupled receptor. Knockout of M1R or exposure to selective or specific receptor antagonists elevates neurite outgrowth in adult sensory neurons and is therapeutic in diverse ...
Mohammad G. Sabbir, Nigel A. Calcutt, Paul Fernyhough, Paul Fernyhough   +3 more
doaj   +1 more source