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Meclonazepam

Chemical compound

Chemical compound

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Meclonazepam ((S)-3-methylclonazepam) is a benzodiazepine derivative similar in structure to clonazepam. It was first discovered by a team at Hoffmann-La Roche in the 1970s. It has sedative and anxiolytic actions like those of other benzodiazepines, and also has anti-parasitic effects against the parasitic worm Schistosoma mansoni.

Meclonazepam was never used as medicine and instead appeared online as a designer drug.

Pharmacology

Its sedative and anxiolytic abilities are attributed to the same mechanism used by other benzodiazepine drugs: modulation of the GABAA receptor in the brain. This psychoactive activity makes it useful for recreational use. The sedating side effect would also make it unsuitable for routine use as an antiparasitical.

Schistosomal parasites do not have an ortholog of the GABAA receptor. Instead, meclonazepam seems to cause a rapid calcium influx, leading to muscle contraction and tegument damage. In 2023, meclonazepam is shown to activate a calcium-permeable schistosome TRP (transient receptor potential), making this TRP a very likely candidate for its parasite receptor.

Some work has been done to produce two meclonazepam derivatives that show less sedation and more anti-parasite activity in mice. They seem to do this by crossing the blood-brain barrier less readily.

References

References

  1. "Benzodiazepine derivatives".
  2. The Lundbeck Institute. "Meclonazepam". Lundbeck.
  3. (1985). "Initial study of methylclonazepam in generalized anxiety disorder. Evidence for greater power in the cross-over design". Psychopharmacology.
  4. (1985). "Central effects in man of the novel schistosomicidal benzodiazepine meclonazepam". European Journal of Clinical Pharmacology.
  5. (May 2016). "Identification of main human urinary metabolites of the designer nitrobenzodiazepines clonazolam, meclonazepam, and nifoxipam by nano-liquid chromatography-high-resolution mass spectrometry for drug testing purposes". Analytical and Bioanalytical Chemistry.
  6. (April 2017). "Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays". Drug Testing and Analysis.
  7. (March 2018). "Experimental versus theoretical log D7.4 , pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances". Drug Testing and Analysis.
  8. (July 2022). "The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines". Forensic Toxicology.
  9. (September 2024). "Development of non-sedating benzodiazepines with in vivo antischistosomal activity". Antimicrobial Agents and Chemotherapy.
  10. "The Misuse of Drugs Act 1971 (Amendment) Order 2017".
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2-chlorophenyl-compounds designer-drugs gabaa-receptor-positive-allosteric-modulators lactams nitrobenzodiazepines
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