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Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

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

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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.
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Nondepolarizing (Competitive) Neuromuscular Blockers: Mechanism of Action01:17

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Nondepolarizing neuromuscular blockers induce paralysis by competitively blocking nicotinic acetylcholine receptors at the muscle end plate. Examples include pancuronium, mivacurium, vecuronium, and rocuronium. These quaternary ammonium derivatives are administered intravenously, are poorly absorbed, and are excreted via the kidneys.
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Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
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Cholinergic Receptors: Nicotinic01:15

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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.
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Isodrimenine Derivatives Selectively Inhibit Human α7-Containing Nicotinic Acetylcholine Receptors via Negative

Han-Shen Tae1, Marcelo O Ortells2, Alexandru Ciocarlan3

  • 1Molecular Horizons/Faculty of Science, Medicine and Health, University of Wollongong, Wollongong, NSW2522, Australia.

ACS Chemical Neuroscience
|December 17, 2025
PubMed
Summary

Three isodrimenine derivatives were found to inhibit human nicotinic acetylcholine receptors (nAChRs), particularly the α7 subtype. These compounds act as negative allosteric modulators, suggesting potential therapeutic applications for neuropsychiatric disorders.

Keywords:
drimane sesquiterpenoidelectrophysiologyisodrimeninemolecular dockingnegative allosteric modulationnicotinic acetylcholine receptor

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Area of Science:

  • Natural Products Chemistry
  • Neuropharmacology
  • Molecular Biology

Background:

  • Drimane sesquiterpenoids are a class of biologically active compounds with diverse natural sources.
  • Nicotinic acetylcholine receptors (nAChRs), especially the α7 subtype, are crucial in neurological functions and implicated in neuropsychiatric disorders.

Purpose of the Study:

  • To synthesize and evaluate the activity of three isodrimenine derivatives against various human nicotinic acetylcholine receptor (nAChR) subtypes.
  • To elucidate the mechanism of action and binding site of these compounds on nAChRs.

Main Methods:

  • Chemical synthesis of 5,6-dehydro-7-keto-isodrimenine (DH7KID), 7-keto-isodrimenine (7KID), and 7-acetoxy-isodrimenine (7AID).
  • Two-electrode voltage-clamp electrophysiology to assess nAChR activity.
  • In silico structural analysis to predict binding interactions.

Main Results:

  • All synthesized isodrimenine derivatives showed inhibitory effects on nAChRs, with a notable selectivity for α7-containing receptors.
  • DH7KID and 7KID exhibited noncompetitive and voltage-independent inhibition, suggesting allosteric modulation at a nonluminal site.
  • In silico analysis supported DH7KID's interaction with allosteric sites on the α7 nAChR.

Conclusions:

  • Isodrimenine derivatives act as negative allosteric modulators of α7-containing nAChRs.
  • The selective inhibition of α7 nAChRs by these compounds holds potential for treating neuropsychiatric disorders.