Muscarinic M1 Receptors
Muscarinic M1 Receptors - Related Videos
01:25
Cholinergic Receptors: Muscarinic
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2023
The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+. Activation...
01:20
Antiasthma Drugs: Muscarinic Receptor Antagonists
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2024
Muscarinic receptor antagonists, also known as antimuscarinic agents, are a class of bronchodilators used to treat asthma, although they are more commonly used to treat COPD. They work by inhibiting the action of acetylcholine (ACh), a neurotransmitter, on muscarinic receptors found in the airways. Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
07:09
Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
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Cited by 7 •
2011
We describe procedures for repeated administration of inhibitors of muscarinic signaling to the levator auris longus (LAL) muscle of young adult mice and for subsequent immunostaining of its neuromuscular junctions (NMJs) in wholemounts. The LAL muscle has unique advantages for revealing in vivo pharmacological effects on NMJs.
11:45
Quantifying Agonist Activity at G Protein-coupled Receptors
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Cited by 10 •
2011
A method for estimating the affinity constant of an agonist for the active state (Kb) of a G protein-coupled receptor is described. The analysis provides absolute or relative measures of Kb depending on whether constitutive receptor activation is measurable. Our method applies to various responses downstream from receptor activation.
10:59
Use of Label-free Optical Biosensors to Detect Modulation of Potassium Channels by G-protein Coupled Receptors
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Cited by 5 •
2014
Optical biosensor techniques can detect changes in mass near the plasma membrane in living cells and allow one to follow cellular responses in both individual cells and populations of cells. This protocol will describe detection of the modulation of potassium channels by G-protein coupled receptors in intact cells using this approach.
FAQs
Activation couples the receptor to Gq/11 proteins, which stimulate phospholipase C. This enzyme increases inositol trisphosphate and diacylglycerol, producing a downstream rise in intracellular calcium. The significance is not simply receptor binding: the signaling sequence links acetylcholine detection to changes in excitability and secretory activity within responsive cells.
These second messengers translate receptor activation into cellular consequences. Inositol trisphosphate and calcium are associated with the intracellular response, while diacylglycerol forms part of the same phospholipase C pathway. Together, they help explain why stimulation can enhance both neuronal excitability and secretion, providing measurable functional outcomes for pharmacological investigation.
Receptor location connects signaling to different physiological functions. In the central nervous system, M1 activity contributes to cognition, learning, and memory through effects on neuronal signaling. In autonomic tissues, the same receptor class can influence glandular activity, including gastric acid secretion. Distribution therefore helps determine both therapeutic opportunities and unwanted effects.
Selectivity is difficult because pharmacological control must distinguish M1 receptors from related muscarinic targets while preserving the desired response. The receptor participates in both central nervous system and autonomic functions, so a compound that affects M1 signaling may influence different physiological processes. This challenge shapes the development of more selective agonists and antagonists.
M1 receptors become relevant when a study focuses on neuronal functions such as cognition, learning, or memory, or on autonomic effects such as gastric acid secretion. Pharmacologists can examine these pathways to assess whether receptor stimulation or blockade produces a useful outcome. Such work supports investigations of potential treatments for neurological and gastrointestinal disorders.
Selective agonists and antagonists provide opposing ways to examine receptor involvement. An agonist can be evaluated for effects associated with M1 signaling, whereas an antagonist can test whether blocking that pathway reduces a response. Comparing these approaches helps connect receptor activity with neuronal or glandular outcomes and informs drug-development strategies.