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Related Concept Videos

Local Anesthetics: Chemistry and Structure-Activity Relationship01:30

Local Anesthetics: Chemistry and Structure-Activity Relationship

Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
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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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Prokinetic agents are specialized medications that stimulate gastrointestinal (GI) motility, promoting food movement through the GI tract. Dopamine, an inhibitory neurotransmitter, plays a significant role in this process, reducing GI motility and indirectly controlling the speed of digestion. Dopamine receptor antagonists, such as metoclopramide and domperidone, offer a unique advantage as prokinetic agents. By blocking the dopamine receptors, these drugs increase GI motility, improving food...
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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: May 29, 2026

A Planarian Motility Assay to Gauge the Biomodulating Properties of Natural Products
07:13

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Published on: May 30, 2020

Minimal structural requirements of alkyl γ-lactones capable of antagonizing the cocaine-induced motility decrease in

Debra Baker1, Sean Deats, Peter Boor

  • 1Department of Biology, West Chester University, West Chester, PA 19383-2112, USA.

Pharmacology, Biochemistry, and Behavior
|September 1, 2011
PubMed
Summary

Certain lactones can block cocaine

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • Parthenolide, a natural cyclic lactone, and its analogs were previously shown to prevent cocaine-induced behavioral effects in planarians.
  • The γ-lactone ring of parthenolide was identified as crucial for this antagonistic effect.

Purpose of the Study:

  • To investigate the structure-activity relationship of alkyl γ-lactones in antagonizing cocaine's effects.
  • To determine the optimal alkyl chain length for γ-lactone compounds to inhibit cocaine-induced behaviors in planarians.

Main Methods:

  • Planarians were exposed to 200 microM cocaine to induce decreased motility.
  • A series of alkyl γ-lactones with varying carbon chain lengths (1-8) were tested for their ability to antagonize these cocaine-induced effects.
  • Planarian motility and behavioral responses were monitored.

Main Results:

  • Alkyl γ-lactones with alkyl chains up to 4 carbons did not affect planarian motility or antagonize cocaine's effects.
  • γ-Nonalactone, featuring a 5-carbon alkyl chain, successfully prevented cocaine-induced behavioral changes.
  • Alkyl γ-lactones with carbon chains longer than 5 carbons failed to exhibit antagonistic properties.

Conclusions:

  • A γ-lactone ring with a 5-carbon functional group represents the optimal structural feature for antagonizing cocaine's effects in planarians.
  • This finding provides insights into the specific structural requirements for lactone-based cocaine antagonists.