7 replies to this topic

[Picard]

Does it upregulate or downregulate GABA(A) receptors over time? I've seen user experiences citing sedative-like properties, which makes me wonder whether it's actually a GABA agonist.

What are your experiences with this?

[kevinseven11]

it is an opioid agonist so id say it down regulates, but I am unsure of its antagonistic activities.

[nupi]

If it is GABAergic, it is weak (as in, cannot feel the effects) so any downregulation would probably not be all that big an issue. It is definitely serotonergic, though which could also explain sedation.

[Raza]

Reading the abstract of the study people were citing for its upregulation of GABA receptors, I'm not at all convinced that it does this when its use isn't actively preventing seizures experienced by an epileptic control group.

I haven't seen anything on it being a GABAergic either, though. Other, better established MoA explain its sedative properties well enough. I agree with nupi that if it is, it probably isn't a strong enough one to cause downregulation.

So as far as I'm ware, neither.

Edited by Raza, 28 December 2012 - 10:02 AM.

[Dissolvedissolve]

It's my understanding that 5-HT1a agonism (and possibly 5-HT release) is primarily responsible for the effects, so I wouldn't think GABA should be dramatically up- or down-regulated. I have seen the study that raza refers to suggesting GABA upregulation.

[Acetylnordopatoninol]

it is an opioid agonist so id say it down regulates, but I am unsure of its antagonistic activities.

i haven't heard of it being an opioid agonist before; can you cite your sources?

[kevinseven11]

http://scholar.googl...l=en&as_sdt=0,5

[xeon]

I started a new topic about Bacopa and the Opoid system here.