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.
Yoshio Nishimura +3 more
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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.
Britta Hedlund +2 more
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The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine [PDF]
, 2014 Background: The main source of 5-HT in body is in enterchromafin cells of intestine, different studies mentioned different roles for endogenous 5-HT and receptors involved and it is not clearified the mechanism of action of endogenous 5-HT. Objectives:
Bianchi C +33 more
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Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma? [PDF]
, 2014 The authors acknowledge the medical writing assistance received from Sam Yarwood, PhD, of Complete HealthVizion, in the form of literature searches and preparation and revision of the draft manuscript.Peer reviewedPublisher ...
Fromer, Leonard +4 more
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Genetics‐Based Targeting Strategies for Precise Neuromodulation
Advanced Science, EarlyView.In this Review, the fundamental principles and implementation protocols of genetics‐based precision neuromodulation are first introduced. Then, wireless and low‐invasive strategies based on nano‐transducing materials are highlighted, along with a dissection and analysis of the strengths and weaknesses of representative studies.
Yuyuan He +11 more
wiley +1 more source
Current and Future Issues in the Development of Spinal Agents for the Management of Pain. [PDF]
, 2017 Targeting analgesic drugs for spinal delivery reflects the fact that while the conscious experience of pain is mediated supraspinally, input initiated by high intensity stimuli, tissue injury and/or nerve injury is encoded at the level of the spinal ...
Fisher, Casey J +3 more
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Novel Electroactive Therapeutic Platforms for Cardiac Arrhythmia Management
Advanced Science, EarlyView.Electroactive platforms offer promising applications in cardiac arrhythmia. Based on their energy sources and mechanisms, electroactive platforms are categorized into i) direct electrical stimulation, ii) self‐powered electroactive systems, iii) physical stimuli‐mediated electroactive systems, and iv) conductive systems, and their applications in ...
Juwei Yang +4 more
wiley +1 more source
Cholinergic modulation of dopamine overflow in the rat neostriatum: A fast cyclic voltammetric study in vitro [PDF]
, 1994 Stimulus-evoked dopamine overflow in rat neostriatal slices was determined using fast cyclic voltammetry. The dopamine efflux induced by intrastriatal stimulation increased with stimulus intensity and was found to be enhanced by more than 100% upon ...
Kudernatsch, Martina, Sutor, Bernd
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Understanding the role of long-acting muscarinic antagonists in asthma treatment [PDF]
, 2022 Objective: Long-acting muscarinic antagonists (LAMAs) have been used in the treatment of obstructive pulmonary diseases for years. Long-acting muscarinic antagonists were previously mainly used as bronchodilators in chronic obstructive pulmonary disease,
Gosens, R +3 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; therefore, the analysis of receptor subtypes is complicated, and misinterpretations can occur.
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