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Phase II Reactions: Methylation Reactions01:17

Phase II Reactions: Methylation Reactions

Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
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Adrenergic Agonists: Mixed-Action Agents

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Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

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CNS Stimulants: Cocaine, Amphetamines and Cannabinoids01:24

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Color Spot Test As a Presumptive Tool for the Rapid Detection of Synthetic Cathinones
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Published on: February 5, 2018

Substituted methcathinones differ in transporter and receptor interactions.

Amy J Eshleman1, Katherine M Wolfrum, Meagan G Hatfield

  • 1Research Service, Veterans Affairs Medical Center, Portland, OR, USA. eshleman@ohsu.edu

Biochemical Pharmacology
|April 16, 2013
PubMed
Summary

Synthetic methcathinones, like those in "bath salts," act as transporter substrates or inhibitors, differing from amphetamines. Their psychoactive effects are primarily linked to dopamine, serotonin, and norepinephrine transporter interactions, not receptor binding.

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Published on: April 23, 2019

Area of Science:

  • Neuroscience
  • Pharmacology
  • Toxicology

Background:

  • Synthetic cathinones, found in
  • bath salts,
  • pose a global health risk.
  • Structurally similar to methamphetamine (METH) and MDMA, they cause severe adverse effects like psychosis and tachycardia.

Purpose of the Study:

  • To investigate the transporter and receptor interaction differences between synthetic cathinones and amphetamine counterparts.
  • To elucidate the primary mechanisms of action for synthetic cathinones.

Main Methods:

  • Radioligand binding assays for human transporters (hDAT, hSERT, hNET).
  • Neurotransmitter uptake inhibition and release assays.
  • Receptor binding assays for serotonin (5-HT) and dopamine receptors.
  • Assays for human vesicular monoamine transporter 2 (hVMAT2) and hSigma1 receptors.

Main Results:

  • Certain cathinones (MDPV, naphyrone) were high-affinity uptake inhibitors but not releasers.
  • Others (4-fluoromethcathinone, mephedrone, methylone) were substrates, inducing neurotransmitter release, particularly at hNET.
  • These compounds showed low affinity for hVMAT2 and weak interactions with 5-HT receptors; no affinity for dopamine receptors was observed.
  • High-nanomolar to mid-micromolar affinity for hSigma1 receptors was noted.

Conclusions:

  • The psychoactive effects of synthetic cathinones are primarily mediated by their interactions with dopamine, serotonin, and norepinephrine transporters, acting as either inhibitors or substrates.
  • Direct interactions with VMAT2 and major neurotransmitter receptors do not fully explain their observed effects.