Jessenius
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TRPV1 antagonist synthesis
Hey, there have been some threads here about TRPV1 modulation, mostly using capsazepine, but I haven’t spotted anyone actually synthesizing such an
antagonist.
This is a report from my home synthesis of A-425619, an even more potent TRPV1 antagonist (IC50 ~ 2 nM), which is not exactly OTC, but it was made
completely in a home lab and I guess some of you might take it as an interesting inspiration.
Enjoy!
[Edited on 22-6-2022 by Jessenius]
[Edited on 22-6-2022 by Jessenius]
Attachment: A-425619_compressed.pdf (730kB)
This file has been downloaded 258 times
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Jessenius
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Please, don’t be afraid to comment on any mistakes in the article, I would love to hear your feedback!
And if you want the original version with high resolution pictures, just tell me and I’ll send it via email.
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xdragon
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Wonderful report, had a blast reading this. Definitely inspiring.
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Diachrynic
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In figure one, the structure is a quinoline, while in the rest of the document it's an isoquinoline. I assume this is an error and should really be an
isoquinoline there as well.
Impressive work!
we apologize for the inconvenience
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Jessenius
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Thanks, this and more corrected.
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Dr.Bob
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Great write up. Maybe this can allow me to finally eat spicy foods better. :-)
Some very nice chemistry, impressive to get hold of triphosgene, its hard to order now even at a research institute. There are a growing number of
chemicals that are getting hard to obtain, sadly. But we must keep going at it.
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clearly_not_atara
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Please be aware that TRPV1 antagonists can cause severe hyperthermia by inhibiting sweating and the ordinary perception of heat.
Internal use is not advised and topical use should not be habitual. Pharmacological development of TRPV1 antagonists for pain relief was halted for
this reason.
[Edited on 04-20-1969 by clearly_not_atara]
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