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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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Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
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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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Drug Discovery: Overview01:26

Drug Discovery: Overview

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Antidotes01:17

Antidotes

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Antidotes are medicinal substances used to counteract the harmful effects of toxins or drugs in the body. They function in various ways, each uniquely designed to combat specific toxic compounds.
Specific antidotes operate by inhibiting the enzymes that control biochemical pathways, reducing the production of harmful metabolites.
An example of an antidote is atropine, which counteracts the detrimental effects of cholinesterase inhibitors. It achieves this by deactivating muscarinic receptors,...
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Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

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

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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.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
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Related Experiment Video

Updated: Jul 19, 2025

Author Spotlight: Discovering New Alkaloids in Plants with Advanced Mass Spectrometry Techniques
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Author Spotlight: Discovering New Alkaloids in Plants with Advanced Mass Spectrometry Techniques

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Quinolizidine-Type Alkaloids: Chemodiversity, Occurrence, and Bioactivity.

Willy Cely-Veloza1, Massuo J Kato2, Ericsson Coy-Barrera1

  • 1Bioorganic Chemistry Laboratory, Facultad de Ciencias Básicas y Aplicadas, Universidad Militar Nueva Granada, Campus Nueva Granada, Cajicá 250247, Colombia.

ACS Omega
|August 14, 2023
PubMed
Summary

Quinolizidine alkaloids (QAs) are natural compounds with diverse structures and significant biological activities. This review highlights their potential for drug and agrochemical development.

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Area of Science:

  • Natural Product Chemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Quinolizidine alkaloids (QAs) are specialized metabolites found in plants and animals.
  • They represent a diverse class of nitrogen-containing natural products.

Purpose of the Study:

  • To review the chemical diversity and biological activities of QAs over the past three decades.
  • To assess the potential of QAs for pharmacological and agrochemical applications.

Main Methods:

  • Comprehensive literature review of QAs reported in the last 30 years.
  • Analysis of isolated QA structures and their associated biological activities.
  • Evaluation of drug-likeness properties of identified QAs.

Main Results:

  • 397 QAs belonging to 20 classes have been identified.
  • Common QAs include matrine, lupanine, and cytisine.
  • QAs exhibit potential cytotoxic, antiviral, antimicrobial, insecticidal, anti-inflammatory, antimalarial, and antiacetylcholinesterase activities.

Conclusions:

  • QAs possess a wide range of biological activities and favorable drug-likeness.
  • Further research into QA structural and biological diversity is warranted for developing new drugs and agrochemicals.