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Curcumin acts as a positive allosteric modulator of 7-nicotinic acetylcholine receptors

curcumin nicotinic acetylcholine

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#1 Galaxyshock

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Posted 23 February 2018 - 08:54 AM


Curcumin acts as a positive allosteric modulator of α7-nicotinic acetylcholine receptors and reverses nociception in mouse models of inflammatory pain

 

Effectsof curcumin, a major ingredient of turmeric, were tested on the function of α7 subunit of the human nicotinic acetylcholine (α7 nACh) receptor expressed in Xenopus oocytes and on nociception in mouse models of tonic and visceral pain. Curcumin caused a significant potentiation of ACh (100 μM)-induced currents with an EC50 value of 0.2 µM. The effect of curcumin was not dependent on the activation of G-proteins and protein kinases and did not involve Ca2+-dependent Cl- channels expressed endogenously in oocytes. Importantly, extent of curcumin potentiation was enhanced significantly by decreasing ACh concentrations. Curcumin did not alter specific binding of [125I]-bungarotoxin. In addition, curcumin attenuated nociceptive behavior in both tonic and visceral pain models without effecting motor and locomotor activity and without producing tolerance. Pharmacological and genetic approaches revealed that the antinociceptive effect of curcumin was mediated by α7 nACh receptors. Curcumin potentiated the antinociceptive effects of the α7 nACh receptor agonist PNU282987. Collectively, our results indicate that curcumin is a positive allosteric modulator of α7 nACh receptor and reverses nociception in mouse models of tonic and visceral pain.

→ source (external link)

 

Full article:

http://jpet.aspetjou...245068.full.pdf



#2 Mind_Paralysis

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Posted 23 February 2018 - 10:19 AM

Fascinating... curcumin is a positive modulator of immunologic activity as well, yes? I suppose this is another evidence pointing towards Acetylcholine affecting the immune-system in a modulating manor.

 

(we did a whole spiel about this in a thread regarding a fellow whom O.D-ed on Acetylcholine which then altered his dysautonomia - we found other connections between dysautonomia and alpha-7-receptors)



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#3 prunk

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Posted 23 February 2018 - 10:49 AM

Very interesting, thanks! I've noticed some cognitive enhancing effects from curcumin, but cos of its libido decreasing effects I've used it only few times. Gotta buy it again.

Edited by prunk, 23 February 2018 - 10:55 AM.






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