N&PD Moderators: Skorpio
Chemicals to upregulate receptors..
rickolasnice
Bluelighter
What chemicals can upregulate what receptors?
St John Wort upregulates serotonin, right?
I'm particularly interested in GHB, GABA and DA (dopamine) upregulation..
Of course, these chemicals should be safe to consume 
Swerlz
Bluelight Crew
What do you mean by upregulate?
Rogue Robot
Bluelight Crew
Homeless -> BDD
jamesmartin
Bluelighter
you mean produce more dopamine , etc ?
try Tryosine for dopamine
and there are also certain foods which contain dopamine boosters like cheese and dairy products (like mature cheese )
and for serotonin there is 5-htp and also foods rich in it like almonds , meats and protein
Psychedelic Jay
Bluelighter
When you say up-regulate, do you mean make them more sensitive?
Bavanai
Bluelighter
down-regulating means desensitizing the receptors so logic would dictate "yes"
Psychedelic Jay
Bluelighter
Is that even possible to do without abstinence from those types of drugs?
dokomo
Ex-Bluelighter
Generally, no. There are always exceptions, but usually up/down-regulation occurs through receptor trafficking, where the number of receptors is changed, rather than the sensitivity of a set number of receptors. The body is always striving for homeostasis so it will Increase/decrease receptors appropriately depending upon how much of a substance is present.
rickolasnice
Bluelighter
^So how does St John Wort work?
Mod.. could you please move this to ADD as most people here don't seem to grasp what i mean?
sarsXdave
Bluelighter
Perhaps the dopamine antagonists would work for DA upregulation, then. Something like Seroquel, if you don't mind sleeping all day. It's a D1, D2, D3, and D4 receptor antagonist, as well as an antagonist of many other receptors.
Of course, I don't know how much time you'd have to spend knocked out on Seroquel before it'd have a significant effect.
EDIT: Apparently Seroquel rapidly dissociates from the D2 receptor. I'm not sure on the specifics, but that may mean it's not that effective for this purpose. I dunno. Some more knowledgeable bros should.
Psilo707
Bluelight Crew
Bdd -> add
edit: oops nevermind, i see its already there. Damn fast mods always taking the fun.
Yes, hypericum upregulates 5HT1A and 5HT2A receptors and is succesfully used to reverse mdma tolerance.
i can't think of a way to upregulate any kind of receptor without depriving the cell of a ligand. maybe gene therapy? these things are highly controlled by negative feedback mechanisms and gene expression. if you did force a normal cell to make more receptors it might just end with cell death due to over excitation and/or apoptosis.
you can do things that will increase the amount of neurotransmitters in the synapse, but that doesn't always turn out as nice as people hope. you have to increase dopamine in just the right places to get positive effects. more dopamine everywhere would be no fun at all.
People really don't seem to be following this thread...
Downregulate = decrease in sensitivity to a drug or neurotransmitter due to stimulation of receptors through high levels of the neurotransmitter or use of agonist drugs.
Upregulate = increase in sensitivity to a drug or neurotransmitter due to a lack of stimulation (or antagonism) toward the receptor.
Increasing levels of a neurotransmitter may feel good for a while, but will downregulate the receptor - this is a major cause of tolerance.
The idea of downregulating receptors is to take something that is an antagonist to your drug of choice while abstaining from the drug, and hence will help reverse your tolerance. This will only be reasonable, of course, if antagonizing the receptor in question doesn't make you feel like shit
All i've heard of for this use is SJW, which is an 5HT2A/B antagonist, and hence should work to treat long-term tolerance to MDMA/entactogens and psychedelics.
rickolasnice
Bluelighter
Another question:
How long do 5-HT, GHB, GABA and DA take to upregulate if said person abstains from agonists of those neurotransmitters? (If possible to estimate)..
rickolasnice
Bluelighter
I'm trying to right the wrongs i've caused myself through drug abuse.. mainly alcohol, gbl, amphetamine and MDMA..
lolwhatzdrugs
Bluelighter
They wouldn't up-regulate if you merely abstained from the agonists, they will REVERSE the down-regulation which created tolerance, and you will be at baseline. There will be no up-regulation, just returning to normal.
As for the time it takes to return your tolerances to 0, I'm sure this number differs with each receptor and each drug.
Several days of abstaining from marijuana will quadruple the intensity of my high, the same does not go for opiates. It usually takes two weeks to make large reductions in tolerance, again this is for me. Everyone is different.
IMHO just antagonizing (blocking) receptors is not a working way most of the time. There are some interesting substances though.
Sulpiride, amisulpride and sultopride seem to directly up-regulate GHB-receptors.
Proglumide and other cholecystokinin antagonist seem to to slow down development of opioid tolerance.
St. John's wort and tianeptine could be useful for SRA-substance related tolerance.
Atypical antipsychotics with 5HT2A affinity are not useful for reversing LSD, psilocybin, mescaline, etc. tolerance. 5HT2A downregulates upon exposure to agonist or antagonist.
I don't understand how tyramine would be able to reverse stimulant tolerance, since tyramine indeed causes spontaneous monoamine release, somewhat like amphetamines. It is not able to cross BBB either.
So far, the only guaranteed way to reverse substance tolerance is abstaining from drug use although I can see some interesting development on these substances.
Good point.
Tianeptine wont work as it doesnt lower serotonin.
