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Related Concept Videos

Preparation and Reactions of Thiols02:33

Preparation and Reactions of Thiols

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Thiols are prepared using the hydrosulfide anion as a nucleophile in a nucleophilic substitution reaction with alkyl halides. For instance, bromobutane reacts with sodium hydrosulfide to give butanethiol.
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Phase II Reactions: Sulfation and Conjugation with α-Amino Acids01:19

Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

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Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
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Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation01:22

Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation

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Glutathione, a tripeptide made up of glutamate, cysteine, and glycine, is a critical player in the detoxification of drugs and xenobiotics via a process known as glutathione conjugation or mercapturic acid formation. This phase II biotransformation reaction involves the covalent binding of glutathione to a drug or its metabolite, enhancing the compound's water solubility and enabling its excretion.
Several distinctive characteristics distinguish glutathione conjugation from other phase II...
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Conversion of Alcohols to Alkyl Halides02:48

Conversion of Alcohols to Alkyl Halides

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This lesson delves into the conversion of alcohols to corresponding alkyl halides and the mechanism of action for different reagents. Typically, the hydroxyl group is first protonated to convert it to a stable leaving group. Consequently, based on the starting alcohol, the mechanism undergoes either of the nucleophilic substitution routes, SN1 or SN2. Tertiary alkyl halides are made using the two-step SN1 mechanism that occurs via a carbocation intermediate, which is stabilized by...
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Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

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Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
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Phase II Reactions: Miscellaneous Conjugation Reactions01:19

Phase II Reactions: Miscellaneous Conjugation Reactions

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Phase II biotransformations are detoxification mechanisms that conjugate xenobiotics with endogenous substances, neutralizing their toxicity.
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
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Related Experiment Video

Updated: Aug 5, 2025

Chronic Intermittent Ethanol Vapor Exposure Paired with Two-Bottle Choice to Model Alcohol Use Disorder
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Disulfiram: Mechanisms, Applications, and Challenges.

Jenna Lanz1, Nicholas Biniaz-Harris1, Mara Kuvaldina1

  • 1Lyme & Tick-Borne Diseases Research Center, Department of Psychiatry, Vagelos College of Physicians and Surgeons, Columbia University Irving Medical Center, Columbia University, New York, NY 10032, USA.

Antibiotics (Basel, Switzerland)
|March 29, 2023
PubMed
Summary

Disulfiram shows promise for repurposing beyond alcohol use disorder, potentially treating addictions, infections, and cancers. However, its significant side effects and pharmacokinetic variability necessitate further research for safe and effective use.

Keywords:
AntabuseLyme diseaseaddictiondisulfiramdrug repurposingrisks

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Murine Drinking Models in the Development of Pharmacotherapies for Alcoholism: Drinking in the Dark and Two-bottle Choice
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Area of Science:

  • Pharmacology
  • Drug Repurposing
  • Clinical Medicine

Background:

  • Disulfiram, approved for alcohol use disorder since the 1940s, is being investigated for new therapeutic applications.
  • This review synthesizes current research on disulfiram's potential beyond its primary indication.

Purpose of the Study:

  • To explore the potential clinical applications of disulfiram through drug repurposing.
  • To identify associated risks and challenges of using disulfiram for non-alcohol-related conditions.

Main Methods:

  • A narrative review of in vivo studies on disulfiram was conducted using PubMed.
  • Search terms included "disulfiram" and "Antabuse," encompassing animal, in vitro, and human studies.

Main Results:

  • Disulfiram shows potential in treating cocaine addiction, various infections (bacterial, viral, parasitic), inflammatory conditions, neurological diseases, and cancers.
  • Significant inter-subject pharmacokinetic variability and a range of side effects, from minor to life-threatening, were noted.

Conclusions:

  • Disulfiram demonstrates potential as a repurposed drug, but its safety profile requires careful consideration.
  • Further animal studies and well-controlled clinical trials are essential to evaluate efficacy and safety for new indications.