Meclonazepam
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Meclonazepam[1] ((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.[2] It has sedative and anxiolytic actions like those of other benzodiazepines,[3] and also has anti-parasitic effects against the parasitic worm Schistosoma mansoni.[4]
Meclonazepam was never used as medicine and instead appeared online as a designer drug.[5][6][7][8]
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.[7] The sedating side effect would also make it unsuitable for routine use as an antiparasitical.[9]
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.[9]
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.[9]
Legal Issues
United Kingdom
In the UK, meclonazepam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs.[10]
See also
References
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Further reading
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