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Related Concept Videos

Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

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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+....
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Cholinergic Receptors: Nicotinic01:15

Cholinergic Receptors: Nicotinic

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Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
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Cooperative Allosteric Transitions01:58

Cooperative Allosteric Transitions

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Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
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The Two-State Receptor Model01:29

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
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Transmembrane Domain Oligomerization Propensity determined by ToxR Assay
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Muscarinic receptor oligomerization.

Sara Marsango1, Richard J Ward1, Elisa Alvarez-Curto1

  • 1Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK.

Neuropharmacology
|November 18, 2017
PubMed
Summary

G protein-coupled receptors (GPCRs), like muscarinic acetylcholine receptors, are increasingly understood to form dimers and oligomers, not just monomers. This review explores their quaternary arrangements and functional significance.

Keywords:
DimerizationLigand regulationMuscarinic acetylcholine receptorOligomerizationQuaternary structure

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Area of Science:

  • Neuroscience
  • Molecular Pharmacology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) were traditionally viewed as monomers.
  • Recent evidence suggests GPCRs form dimers and higher-order oligomers.
  • The structure and function of GPCR oligomerization are still under investigation.

Purpose of the Study:

  • To review current knowledge on the quaternary arrangements of muscarinic acetylcholine receptors.
  • To explore the functional implications of GPCR oligomerization.
  • To synthesize findings from traditional biochemical and modern biophysical techniques.

Main Methods:

  • Literature review of studies on muscarinic acetylcholine receptor oligomerization.
  • Analysis of data from biochemical approaches.
  • Evaluation of findings from biophysical techniques.

Main Results:

  • Muscarinic acetylcholine receptors, a class A GPCR, exhibit diverse quaternary arrangements.
  • Evidence supports the formation of dimers and oligomers for these receptors.
  • Oligomerization influences receptor function in the central and peripheral nervous systems.

Conclusions:

  • GPCRs, including muscarinic acetylcholine receptors, exist as oligomers.
  • Understanding GPCR quaternary structure is crucial for neuropharmacology.
  • Further research is needed to fully elucidate the molecular basis and functional roles of GPCR oligomerization.