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Related Concept Videos

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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Amines with low molecular weight are usually gaseous at room temperature, while those with high molecular weight are liquid or solids in nature. Usually, low molecular weight amines have a rotten fish-like smell. Diamines typically have a pungent smell. For instance, cadaverine and putrescine, depicted in Figure 1, are two molecules responsible for decaying tissue.
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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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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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Anticholinesterases, also known as cholinesterase inhibitors, work by blocking the breakdown of acetylcholine, leading to its accumulation in the synaptic cleft. This accumulation indirectly enhances both muscarinic and nicotinic actions. These agents are classified as reversible or irreversible based on their mechanism of action.     
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Related Experiment Video

Updated: Jul 3, 2025

In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing &#946;-galactosidase
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Antitrypanosomal Chloronitrobenzamides.

Angela K Carrillo1, Tara Man Kadayat2, Jong Yeon Hwang3

  • 1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.

Journal of Medicinal Chemistry
|February 16, 2024
PubMed
Summary
This summary is machine-generated.

A new drug candidate, compound 52, shows promise for treating Human African Trypanosomiasis (HAT). This orally bioavailable agent is effective against Trypanosoma species and well-tolerated in animal studies.

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Bioluminescence Imaging to Detect Late Stage Infection of African Trypanosomiasis
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Area of Science:

  • Parasitology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Human African Trypanosomiasis (HAT) is a neglected tropical disease affecting millions.
  • Current HAT treatments suffer from low efficacy, drug resistance, and toxicity issues.

Purpose of the Study:

  • To synthesize and evaluate chloronitrobenzamides (CNBs) as potential antitrypanosomal agents.
  • To identify potent and orally bioavailable drug candidates for HAT treatment.

Main Methods:

  • Synthesis of chloronitrobenzamides (CNBs).
  • In vitro evaluation of compounds against Trypanosoma species.
  • In vivo pharmacokinetic and efficacy studies in rodent models.

Main Results:

  • Compound 52 identified as a potent and selective orally bioavailable antitrypanosomal agent.
  • Compound 52 demonstrated favorable pharmacokinetics and was well tolerated in vivo.
  • Treatment with compound 52 significantly extended survival in infected mice.

Conclusions:

  • Compound 52 is a promising lead compound for developing new treatments for HAT.
  • Further development of compound 52 could address unmet needs in human and animal trypanosomiasis.