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Related Concept Videos

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

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

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...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.
Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

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...
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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

Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Direct-Acting Cholinergic Agonists: Pharmacokinetics01:31

Direct-Acting Cholinergic Agonists: Pharmacokinetics

Direct-acting cholinergic agonists, such as synthetic choline esters and naturally occurring alkaloids, exert their effects by enhancing the actions of acetylcholine and stimulating the parasympathetic nervous system. Synthetic choline esters share structural similarities with acetylcholine. For example, they have a positively charged quaternary ammonium or onium group, contributing to their hydrophilic characteristics. As a result, they are poorly absorbed in the body through oral...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

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 antagonists are called...

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Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
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Methylacridinium and its cholinergic properties.

Ondrej Soukup1, Jan Proska, Jiri Binder

  • 1Department of Toxicology, University of Defence, Trebesska 1575, Hradec Kralove 500 01, Czech Republic.

Neurotoxicity Research
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10-Methylacridinium iodide (MA) effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Its ability to cross the blood-brain barrier suggests potential applications in treating neurological disorders.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • Cholinesterase inhibitors are crucial for treating conditions like Alzheimer's disease and myasthenia gravis.
  • 10-Methylacridinium iodide (MA) is a known cholinesterase inhibitor.

Purpose of the Study:

  • To investigate the inhibitory effects of MA on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE).
  • To explore MA's interaction with muscarinic M2 receptors.
  • To assess MA's potential for treating neural disorders.

Main Methods:

  • Spectrophotometric Ellman's method at 436 nm using commercial enzymes.
  • Assay of [(3)H]N-methylscopolamine binding to muscarinic M2 receptors.
  • Contractile studies on isolated rat bladder.

Main Results:

  • MA inhibits human recombinant AChE (IC(50) = 1.68 ± 0.14 μM) and human serum BuChE (IC(50) = 3.54 ± 0.27 μM).
  • MA inhibits muscarinic M2 receptor binding (IC(50) = 1.90 μM), potentially allosterically.
  • Functional effects were observed in rat bladder contractile studies.

Conclusions:

  • MA demonstrates potent inhibition of both AChE and BuChE.
  • MA interacts with muscarinic M2 receptors.
  • MA's physicochemical properties (log P = -0.32, PSA = 3.88) suggest it can cross the blood-brain barrier, indicating potential therapeutic use for neurological conditions.