What upregulates postsynaptic 5HT1A receptors?

[Meso]

Specifically of postsynaptic 5HT1A in the limbic system. From searching on Pubmed, hypericum perforatum (SJW), electroconvulsive shock (ECS), and tricyclic antidepressants can do so. Let me know if I missed something.

You can also mention things that would downregulate postsynaptic 5HT1A in the hippocampus and amygdalae, as counteracting those would also yield a net increase in postysnaptic 5HT1A density. I know that glucocorticosteroid hypersecretion downregulates these receptors, as blunting the HPA axis is one of the mechanisms antidepressants work. What else?

[Blueturtle]

Would chronically using something like busiprone or flibanserin (5-ht1a agonists often used for sexual dysfunction) upregulate or downregulate in the long run?

[Meso]

Would chronically using something like busiprone or flibanserin (5-ht1a agonists often used for sexual dysfunction) upregulate or downregulate in the long run?

Buspirone would downregulate the autoreceptor since it's a full agonist. It won't downregulate the postsynaptic heteroreceptors since it's a weak partial agonist.

Flibanserin is selective to only the postsynaptic receptors, bypassing the presynaptic ones. It doesn't affect hippocampal 5HT1A receptors, so it's safe even if it eventually downregulates cortical ones. Pretty good on paper, and I'll try it soon for anhedonia and blunted affect.

[TalkingAnt]

Nicotine, acutely: https://onlinelibrary.wiley.com/doi/abs ... 01.01501.x

E2 + prog (in females): https://www.karger.com/Article/Abstract/54679

Cannabinoids: https://www.sciencedirect.com/science/a ... 2210005099

Rhodiola (not sure if pre/post): https://www.ncbi.nlm.nih.gov.sci-hub.se/pubmed/22921986

SJW (not sure if pre/post): https://www.researchgate.net/publicatio ... _receptors

Tangentially related stuff I stumbled upon:

More postsynaptic 5HT1A causes more neurogenesis: https://www.sciencedirect.com/science/a ... 4016306838

Postsynaptic 5HT1A agonism and 5HT2B antagonism increase Ach: https://onlinelibrary.wiley.com/doi/abs ... 62051804.x

[taarn]

Isn't Binospirone the perfect one for this? Partial agonist for presynaptic atuoreceptors + antagonist for postsynaptic ones.

Either WAY-100635 or WAY-100135. I don't know if they behave differently for pre/post receptors but if they antagonitze each, then it's also good cause there's a great chance either are desensitized.

[Meso]

Isn't Binospirone the perfect one for this? Partial agonist for presynaptic atuoreceptors + antagonist for postsynaptic ones.

For the sake of upregulating postsynaptic receptors? thing is, they won't stay upregulated when one stops taking it. I think a partial agonist at all 5HT1A receptors is better for our condition given that the intrinsic activity is ~70%

[taarn]

@Mesolimbo So you say that after antagonism the receptors will be back to the new (bad) homeostasis? Because of faulty SERT or whatever that keeps them desensitized?

[Jaxx]

Isn't Binospirone the perfect one for this? Partial agonist for presynaptic atuoreceptors + antagonist for postsynaptic ones.

For the sake of upregulating postsynaptic receptors? thing is, they won't stay upregulated when one stops taking it. I think a partial agonist at all 5HT1A receptors is better for our condition given that the intrinsic activity is ~70%

Isnt this the whole reason why people have windows instead of cures in the first place? For instance on SJW many saw benefits, but they disappeared after days-weeks.
Having said that, there are plenty examples where people got cured, while others experienced a rebound on the same substance. Still worth exploring this route more id say.

[nebonym]

Could this be relevant?
From http://www.pssdforum.com/viewtopic.php? ... 4794#p4794

exercise (specifically running) running increases the number of 5-ht1a autoreceptors in the dorsal raphe nuclei (DRN) after 6 weeks of voluntary running, and this causes a significant reduction (40%) in serotonin in the extracellular space in the DRN. read this paper http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4303035/