• All new members please introduce your self here and welcome to the board:
    http://www.professionalmuscle.com/forums/showthread.php?t=259
Buy Needles And Syringes With No Prescription
M4B Store Banner
spc
Riptropin Store banner
Generation X Bodybuilding Forum
Buy Needles And Syringes With No Prescription
Buy Needles And Syringes With No Prescription
Mysupps Store Banner
IP Gear Store Banner
Anabolic Hormones Store Banner
Ganabol Store Banner
Spend $100 and get bonus needles free at sterile syringes
Professional Muscle Store open now
LandmarkChem Email Banner
Medtech Store Banner
Bruce Labs Store banner
qtropin
Professional Muscle Store open now
over 5000 supplements on sale at professional muscle store
sunrise
ESPECIL-2
Buy Needles And Syringes With No Prescription
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store
over 5000 supplements on sale at professional muscle store

Memantine as a Dopamine agonist/Prolactin inhibitor?

ShZ

New member
Registered
Joined
Dec 12, 2015
Messages
69
Hey guys,

I just came across some pretty interesting studies after researching Memantine for a while.

Memantine agonist action at dopamine D2High receptors.

Memantine is reported to improve symptoms in moderate cases of Alzheimer's disease and Parkinson's disease, but is also known to trigger psychosis in some Parkinson patients. Because these clinical features suggested a possible dopamine component of memantine action, we measured the potency of memantine on the functional high-affinity state of dopamine D2 receptors, or D2(High). Using [(3)H]domperidone to label D2 receptors, the memantine dissociation constant at D2(High) was 917 +/- 23 nM for rat striatal D2 receptors and 137 +/- 19 nM for human cloned D2Long receptors. The memantine dissociation constant for striatal N-methyl-D-aspartate (NMDA) receptors labeled by [(3)H]MK 801 was 2200 +/- 400 nM. Memantine stimulated the incorporation of [(35)S]GTP-gamma-S into D2-expressing Chinese Hamster Ovary cells with a dissociation constant of 1200 +/- 400 nM. Memantine, between 200 and 2000 nM, directly acted on D2(High) to inhibit the release of prolactin from isolated anterior pituitary cells in culture. Because the memantine potencies at NMDA receptors and dopamine D2(High) receptors are of a similar order of magnitude, it is likely that the clinical features of memantine can be attributed to its action at both types of receptors.

Memantine-induced dopamine release in the prefrontal cortex and striatum of the rat--a pharmacokinetic microdialysis study.

Memantine (1-amino-3,5-dimethyl-adamantane) has therapeutic potential in Parkinson's disease and dementia. However, its effect on dopaminergic activity in the central nervous system is still unclear. Therefore, we studied the effect of memantine on dopamine release in prefrontal cortex and striatum, using in vivo microdialysis. Memantine (5, 10 and 20 mg/kg i.p.) caused a dose-dependent increase in dopamine release up to nearly 50% over basal levels. The output of the metabolites was of later onset and longer duration in prefrontal cortex and in striatum. After administration of 10 and 20 mg/kg, in both brain areas memantine levels could be detected over the investigated period of 160 min. The maximal concentrations (Cmax) differed dose dependently, whereas the time to reach this maximum (tmax) was almost identical (68.5 +/- 3.4 min). From the flat elimination profile a half-life of 2.8 +/- 0.5 h (range 2-3.4 h) was calculated. These data demonstrate enhanced dopamine release and metabolism after memantine treatment and support the assumption of an interaction between noncompetitive NMDA-receptor antagonists and dopaminergic systems.

Chronic administration of NMDA antagonists induces D2 receptor synthesis in rat striatum.

Dopamine D2 receptor gene expression was examined in rat striatum after chronic treatment with N-methyl-D-aspartate (NMDA) receptor antagonists (ketamine at 15 mg/kg/day or MK-801 at 0.1, 0.2 and 0.4 mg/kg/day per os, for 50 days). The long-isoform mRNA, as well as the total D2 mRNA expression were induced. No change was noticed in striatal dopamine release or turnover. D2 binding studies carried out in MK-801 chronically treated (0.3 mg/kg/day per os, for 50 days) and control rats revealed an increased receptor density in treated animals without a significant change in receptor affinity. These results suggest that the synthesis of both striatal D2 receptor isoforms is postsynaptically regulated at the transcriptional level, by events triggered by glutamate through the NMDA-type receptor.


So, it directly reduces prolactin levels while synthesising new dopamin receptors. If the effect on prolactin inhibition is strong enough, this would mean we no longer had to deal with caber, prami or bromo and its nasty side effects! Besides that, due to its NMDA antagonism, Memantine is able to reduce or even reverse tolerance to a various number of drugs.
 

Matsuo Munefusa

Well-known member
Kilo Klub Member
Registered
Joined
Sep 21, 2010
Messages
2,296
an NMDA antagonist would not be my first choice to upregulate dopamine receptors/increase dopamine activity. I understand it is also a dopamine agonist too. It is quite the promiscuous drug as a matter of fact (binding to multiple different axes).

Have you researched l-dopa? That would be my first choice as long as dosage is carefully controlled from my experience and research it seems to be the least side effects of any anti-prolactin therapy. It is a donator past the rate limiting step for dopamine and very very effective at lowering prolactin.

I am assuming we are discussing this solely in light of prolactin issues? You mentioned tolerance reversal at the end there..........another popular tolerance reversal agent has been ketamine among heroin users. The NMDA antagonism of ketamine upregulates mu opioid receptors and reverses heroin tolerance. It has never been as effective as one might think though.

There are studies on NMDA antagonism and stimulant tolerance reversal also but the only conclusive studies combined NMDA antagonism and ABSTINENCE from the drug, which to me makes the studies beyond inconclusive.
 
Last edited:

ShZ

New member
Registered
Joined
Dec 12, 2015
Messages
69
an NMDA antagonist would not be my first choice to upregulate dopamine receptors/increase dopamine activity. I understand it is also a dopamine agonist too. It is quite the promiscuous drug as a matter of fact (binding to multiple different axes).

Have you researched l-dopa? That would be my first choice as long as dosage is carefully controlled from my experience and research it seems to be the least side effects of any anti-prolactin therapy. It is a donator past the rate limiting step for dopamine and very very effective at lowering prolactin.

I am assuming we are discussing this solely in light of prolactin issues? You mentioned tolerance reversal at the end there..........another popular tolerance reversal agent has been ketamine among heroin users. The NMDA antagonism of ketamine upregulates mu opioid receptors and reverses heroin tolerance. It has never been as effective as one might think though.

There are studies on NMDA antagonism and stimulant tolerance reversal also but the only conclusive studies combined NMDA antagonism and ABSTINENCE from the drug, which to me makes the studies beyond inconclusive.
I've tried Mucuna Pruriens before which is supposed to contain L-Dopa but haven't had success with it. Nonetheless, I'll give Memantine a try. Let's see what my bloodwork says.
 

Matsuo Munefusa

Well-known member
Kilo Klub Member
Registered
Joined
Sep 21, 2010
Messages
2,296
I cannot give you a source since it conflicts with the board rules but there is pure l-dopa available. I wouldn't trust a natural product to contain anywhere close to a standardized amount of a drug that NEEDS to be dosed extremely accurately.

But why start the thread if you were just going to do it anyway? It is not a great idea....but go for it.

Check out NMDA antagonism + neurotoxicity....leads to permanent changes in the brain.
 

LK3

Verified Sponsor
Kilo Klub Member
Registered
Sponsors
Joined
Mar 17, 2009
Messages
6,577
bro...
learn some respect for all this brain fuckery!
ppl take all this waaaayyyy too lightly.

i used to as well.

these meds fuck with brain chems that the makers dont even fully understand.
look at the big pic, you get some kookie side effects.

plus playing with d1-2 receptors for some is like playing with fire.

treat "prolactin" meds of all kinds with lots of care and respect.

fear maybe. lol
:star:wars
 

Thebigone

New member
Kilo Klub Member
Joined
Oct 28, 2009
Messages
3,621
bro...
learn some respect for all this brain fuckery!
ppl take all this waaaayyyy too lightly.

i used to as well.

these meds fuck with brain chems that the makers dont even fully understand.
look at the big pic, you get some kookie side effects.

plus playing with d1-2 receptors for some is like playing with fire.

treat "prolactin" meds of all kinds with lots of care and respect.

fear maybe. lol
:star:wars
I agree. My psychiatrist said cabergoline can induce psychosis. I can't believe I used it for 7 years straight.
 

LK3

Verified Sponsor
Kilo Klub Member
Registered
Sponsors
Joined
Mar 17, 2009
Messages
6,577
I agree. My psychiatrist said cabergoline can induce psychosis. I can't believe I used it for 7 years straight.
lol
see wtf i mean!!!
and you wonder why you at the fuckin shrink! lol
just playin

you know im crazy too:banghead:

also dude.. not even gona say the 7 year thing.
but...
in general terms for THAT you basically hit your brain with chemistry kinda sorta similar to rec drugs of the dopamine variety.. its gona take real work to fix that shit...
 
Last edited:

needthepump

New member
Registered
Joined
Dec 20, 2016
Messages
328
I agree. My psychiatrist said cabergoline can induce psychosis. I can't believe I used it for 7 years straight.
There is a link with high dopamine levels and schitzophrenia. Antipsychotics lower dopamine levels, and can raise prolactin. Dopamine levels aren't something to mess with as too low of a level leads to all sorts of movement disorders some which can be permanent.

Illegal drugs send dopamine through the roof hence the high. Dopamine boosters like caber raise it. Over time the body stops naturally producing dopamine and it's not a good thing.
 
Last edited:

Matsuo Munefusa

Well-known member
Kilo Klub Member
Registered
Joined
Sep 21, 2010
Messages
2,296
I agree. My psychiatrist said cabergoline can induce psychosis. I can't believe I used it for 7 years straight.
check out the official side effects for cabergoline.....sex addiction, gambling, CROSS DRESSING (lol)....excess dopamine makes people do some WHACKY shit.

Now, you're probably not going to be a sex addict gambling cross dresser taking some dopamine meds but LK3s warning is a good one. Care should be taken with this stuff, more than any other bodybuilding ancillary dopamine meds need to be taken VERY carefully (and cycled off).
 

Thebigone

New member
Kilo Klub Member
Joined
Oct 28, 2009
Messages
3,621
I always treated caber like an anti E where I figured I could just take it all the time since I'm always on GH. My doses were extremely low compared to actual doses given to patients who need the medication. I was only taking around 1mg per week at most. A few years ago I went off of it and got blood work done a month later and prolactin was at 0. So then another two months later I got it checked again and prolactin was in normal range. I have no idea what damage it could've done. I have borderline personality disorder which I've had way before I even started AAS in general and technically no medication fixes that as cognitive therapy is the only true method. My doctor still has me on 1200mg Trileptal, 200mg lamictal and 20mg lexapro. That combo worked really well for helping me control violent outbursts. But now that I have kids and I've matured a lot since that time I actually think the cognitive therapy I did helped me even more. In fact the past few months I tapered down my meds and now I'm just on the 20mg lexapro, only 100mg lamictal and only 300mg trileptal. In another month I will just be on lexapro. I literally have noticed no difference whatsoever from dropping the Lamictal and Trileptal which leads me to believe I never needed it in the first place.
 
Last edited:

LK3

Verified Sponsor
Kilo Klub Member
Registered
Sponsors
Joined
Mar 17, 2009
Messages
6,577
dude, real quick..
i have been "diagnossed" bipolar and borderline.

i know this shit well..

the dr meds for me are no good at all.
happy to get into all this further if you like.

but MM post is scarey true for you!

my issuese relate much mroe to dopamine then anything else.

drs n all that are waaay off in my opinion
 

Forum statistics

Total page views
503,858,250
Threads
123,749
Messages
2,365,366
Members
155,266
Latest member
xsyst
Top