Thoughts On 5ar And Post Finasteride Syndrome

TubZy

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3-6mg that's it? I was under the impression most people were taking 20-100mg per dosage. I have been experimenting with just a few drops (3-5mg)of progestene (which has dmso) but it can tend to make me too relaxed/spaced out and not focused and energized enough to study. I will play around with adding in a little bit of DHEA though.

So how much dhea are you taking now that you have foudn your thyroid functinning better?


Damn taking a look at that study is pretty interesting. The doses they used were gigantic, 100mg per kg. I would be upwards of 5g of caffiene for a human. The results speak for themselves though, a 65% increase in density is quite remarkable. Hard to say if it is a compensation for decreased GABA detection in the serum or if it a positive feedback, (hopefully the latter)

I just use about 5mg of prog and 5mg of dhea taken together. I did try 100mg before of prog and I felt better but after a few days anti androgenic effects hit in.

On a separate note, I found this caffeine study in regards to allopreg. Pretty interesting, maybe that is why a lot of ppl like doing the 5a-dhp and caffeine combo.

Reversal of caffeine-induced anxiety by neurosteroid 3-alpha-hydroxy-5-alpha-pregnane-20-one in rats
 
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bloom

bloom

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Caffeine in low doses dramatically improves my symptons, calms me down improves my libido
I just use about 5mg of prog and 5mg of dhea taken together. I did try 100mg before of prog and I felt better but after a few days anti androgenic effects hit in.

On a separate note, I found this caffeine study in regards to allopreg. Pretty interesting, maybe that is why a lot of ppl like doing the 5a-dhp and caffeine combo.

Reversal of caffeine-induced anxiety by neurosteroid 3-alpha-hydroxy-5-alpha-pregnane-20-one in rats
 

TubZy

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TubZy

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I also looked into trib a while back b/c it seems some many people got cured from it. Most likely from stimulating the AR in the brain or 5AR. It is just very hard not finding a crappy source. I used to use trib back in high school prior to fin it was actually one of my fav supps.

Tribulus terrestris

The extract is claimed to increase the body's natural testosterone levels and thereby improve male sexual performance and help build muscle.
But T. terrestris has consistently failed to increase testosterone levels in controlled studies. It has also failed to demonstrate strength-enhancing properties. However, many supplement brands have sold products that combine various herbs with T. terrestris, with debatable effects.
T. terrestris has been shown to enhance sexual behaviour in an animal model by stimulating androgen receptors in the brain.
Some body builders use T. terrestris as post cycle therapy or "PCT". After they have completed an anabolic-steroid cycle, they use it under the assumption that it will restore the body's natural testosterone levels.

Animal studies in rats, rabbits and primates have demonstrated that administration of Tribulus terrestris extract can produce statistically significant increases in levels of testosterone, dihydrotestosterone and dehydroepiandrosterone (DHEA), and produces effects suggestive of aphrodisiac activity. On the other hand, one recent study found that T. terrestris caused no increase in testosterone or LH in young men, and another found that a commercial supplement containing androstenedione and herbal extracts, including T. terrestris, was no more effective at raising testosterone levels than androstenedione alone.
The active chemical in T. terrestris is likely to be protodioscin (PTN), a cousin to DHEA. In a study with mice, Tribulus was shown to enhance mounting activity and erection better than testosterone cypionate. This however, is not as convincing as one might think. Although an OTC supplement outpacing a pharmaceutical is big news, testosterone cypionate is a synthetic ester of testosterone engineered for its longer activity. To be effective, its level must build up in the system of the animal using it. This process usually takes 2–3 weeks. Since 2007-11-15 National Institutes of Health retrieved that the proerectile aphrodisiac properties were concluded to likely be due to the release of nitric oxide from the nerve endings innervating the corpus cavernosum penis.

Extacts from T. terrestris standardised for protodioscin content have been demonstrated to produce proerectile effects in isolated tissues and aphrodisiac action in several animal species.
The mechanism for these effects has not been clearly established, and while protodioscin has been demonstrated to trigger release of nitric oxide in corpus cavernosum tissue, and also to produce statistically significant increases in the levels of the hormones testosterone, dihydrotestosterone and dehydroepiandrosterone in animal studies, evidence for efficacy in humans is limited and remains controversial (The effect of five weeks of Tribulus terrestris supplementation on muscle strength and body composition during preseason training in elite rugby league players, 2007).

In a study on rats, brain sections showed NADPH-d positive neurons in the paraventricular region of the hypothalamus. The staining intensity and the number of positive neurons were significantly higher in TT treated group than control. There was a statistically significant increase by 67% in the TT treated group compared to the control (p < 0.05); there was smaller number of AR in the control group compared to the TT treated one (p < 0.05); this increase was 58% in the TT treated group compared to control and was statistically significant (Effect of Tribulus terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain, 2005).
 
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bloom

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I also looked into trib a while back b/c it seems some many people got cured from it. Most likely from stimulating the AR in the brain or 5AR. It is just very hard not finding a crappy source. I used to use trib back in high school prior to fin it was actually one of my fav supps.

Tribulus terrestris

The extract is claimed to increase the body's natural testosterone levels and thereby improve male sexual performance and help build muscle.
But T. terrestris has consistently failed to increase testosterone levels in controlled studies. It has also failed to demonstrate strength-enhancing properties. However, many supplement brands have sold products that combine various herbs with T. terrestris, with debatable effects.
T. terrestris has been shown to enhance sexual behaviour in an animal model by stimulating androgen receptors in the brain.
Some body builders use T. terrestris as post cycle therapy or "PCT". After they have completed an anabolic-steroid cycle, they use it under the assumption that it will restore the body's natural testosterone levels.

Animal studies in rats, rabbits and primates have demonstrated that administration of Tribulus terrestris extract can produce statistically significant increases in levels of testosterone, dihydrotestosterone and dehydroepiandrosterone (DHEA), and produces effects suggestive of aphrodisiac activity. On the other hand, one recent study found that T. terrestris caused no increase in testosterone or LH in young men, and another found that a commercial supplement containing androstenedione and herbal extracts, including T. terrestris, was no more effective at raising testosterone levels than androstenedione alone.
The active chemical in T. terrestris is likely to be protodioscin (PTN), a cousin to DHEA. In a study with mice, Tribulus was shown to enhance mounting activity and erection better than testosterone cypionate. This however, is not as convincing as one might think. Although an OTC supplement outpacing a pharmaceutical is big news, testosterone cypionate is a synthetic ester of testosterone engineered for its longer activity. To be effective, its level must build up in the system of the animal using it. This process usually takes 2–3 weeks. Since 2007-11-15 National Institutes of Health retrieved that the proerectile aphrodisiac properties were concluded to likely be due to the release of nitric oxide from the nerve endings innervating the corpus cavernosum penis.

Extacts from T. terrestris standardised for protodioscin content have been demonstrated to produce proerectile effects in isolated tissues and aphrodisiac action in several animal species.
The mechanism for these effects has not been clearly established, and while protodioscin has been demonstrated to trigger release of nitric oxide in corpus cavernosum tissue, and also to produce statistically significant increases in the levels of the hormones testosterone, dihydrotestosterone and dehydroepiandrosterone in animal studies, evidence for efficacy in humans is limited and remains controversial (The effect of five weeks of Tribulus terrestris supplementation on muscle strength and body composition during preseason training in elite rugby league players, 2007).

In a study on rats, brain sections showed NADPH-d positive neurons in the paraventricular region of the hypothalamus. The staining intensity and the number of positive neurons were significantly higher in TT treated group than control. There was a statistically significant increase by 67% in the TT treated group compared to the control (p < 0.05); there was smaller number of AR in the control group compared to the TT treated one (p < 0.05); this increase was 58% in the TT treated group compared to control and was statistically significant (Effect of Tribulus terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain, 2005).
Yeah lots of reports of improvement from TT. It's interesting that it's mechanism of action could be from its effects on the brain. Do you know of any good quality high Protodioscin TT? Interestingly Phosphatidylserine made me worse in the same way as creatine and sorghum. The Brain all the way.
 
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bloom

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Same, I can tolerate higher doses if I pair it with aspirin or vit C, both of which lower cortisol so that is probably why.

You may like these threads:
A List Of Androgens That Stimulate 5-AR Activity
Chronic Caffeine Ingestion Increases T And DHT Levels
Caffeine Increases DHT By Enhancing 5-alpha Reductase
Yeah i've read that. The study Haidut posted showed increase of 5ar in the brain from caffeine. So im focusing on the Brain exclusively, it's the only method which has worked for me. All other methods of increasing 5ar have failed, everything which seems to increase 5ar in the brain works. I'm going to treat PFS as a neurological condition.
 
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TeslaFan

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haidut mentioned to me some indications that sublingual administration of certain substance seems to target brain better than other routes. Here's the link:

Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D

So, perhaps, trying saturated steroids sublingually may not be a bad thing to try. I personally prefer it that way as mental effects seem stronger, especially with 11-keto and androsterone.
 

Dhair

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Hey guys.
I don't have PFS but I'm still dealing with some terrible side effects from fluoroquinolone toxicity. Apparently quinolones prevent GABA from binding to its receptors.
Is this mechanism of action somewhat similar to what finasteride does in terms of mental sides?
 
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bloom

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Hey guys.
I don't have PFS but I'm still dealing with some terrible side effects from fluoroquinolone toxicity. Apparently quinolones prevent GABA from binding to its receptors.
Is this mechanism of action somewhat similar to what finasteride does in terms of mental sides?
Sorry man, I don't know anything about that drug.
 
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bloom

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haidut mentioned to me some indications that sublingual administration of certain substance seems to target brain better than other routes. Here's the link:

Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D

So, perhaps, trying saturated steroids sublingually may not be a bad thing to try. I personally prefer it that way as mental effects seem stronger, especially with 11-keto and androsterone.
Good stuff, the Blood Brain Barrier is a huge problem.
 
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bloom

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Inflammation compromises the BBB, might be in part why we see improvements when sick. From wiki:

However, not all drugs that are delivered directly to the CSF can effectively penetrate the CSF barrier and enter the brain.[medical citation needed] The blood–brain barrier becomes more permeable during inflammation. This allows some antibiotics and phagocytes to move across the BBB. However, this also allows bacteria and viruses to infiltrate the BBB.[12][15]
 

JoeKool

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@Dhair

It sounds similar... following the trail, 5AR is needed for many conversions including the Preg -> Allo -> GABA... so Fin , unbeknownst to me, can have a profound affect on anxiety in ppl who have the slightest touch of clinical anxiety... it is these people i believe that suffer PFS which is why it's hard to pinpoint who will get it... still, the anxiety state from this GABA receptor downgrade and such could be along the lines of what quinolones did to you....

As I see it on this forum and with the recoveries of PFS, making the body 'right' is the first step... and you don't have to be suffering from an ailment to want to aim for that. Digestion/Diet (no seeds, avoiding PUFA) and baseline building blocks (preg, k2, D3, etc... ) all seem to help the first step. Of which I wouldn't stop when certain ailments subside...

2nd step, as @bloom is checking, is a specific issue and dialing up the supplementation to it... in this case, 5ar expression in the brain and it's cascading benefits (Depression, DHT effectiveness, Erectile issues as PFS sufferers deal with)...

@bloom what are you currently supplementing and looking to achieve , for clarity... increase of GABA via some supplement that crosses the BBB?? 5AR unregulation??
 

sladerunner69

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I also looked into trib a while back b/c it seems some many people got cured from it. Most likely from stimulating the AR in the brain or 5AR. It is just very hard not finding a crappy source. I used to use trib back in high school prior to fin it was actually one of my fav supps.

Tribulus terrestris

The extract is claimed to increase the body's natural testosterone levels and thereby improve male sexual performance and help build muscle.
But T. terrestris has consistently failed to increase testosterone levels in controlled studies. It has also failed to demonstrate strength-enhancing properties. However, many supplement brands have sold products that combine various herbs with T. terrestris, with debatable effects.
T. terrestris has been shown to enhance sexual behaviour in an animal model by stimulating androgen receptors in the brain.
Some body builders use T. terrestris as post cycle therapy or "PCT". After they have completed an anabolic-steroid cycle, they use it under the assumption that it will restore the body's natural testosterone levels.

Animal studies in rats, rabbits and primates have demonstrated that administration of Tribulus terrestris extract can produce statistically significant increases in levels of testosterone, dihydrotestosterone and dehydroepiandrosterone (DHEA), and produces effects suggestive of aphrodisiac activity. On the other hand, one recent study found that T. terrestris caused no increase in testosterone or LH in young men, and another found that a commercial supplement containing androstenedione and herbal extracts, including T. terrestris, was no more effective at raising testosterone levels than androstenedione alone.
The active chemical in T. terrestris is likely to be protodioscin (PTN), a cousin to DHEA. In a study with mice, Tribulus was shown to enhance mounting activity and erection better than testosterone cypionate. This however, is not as convincing as one might think. Although an OTC supplement outpacing a pharmaceutical is big news, testosterone cypionate is a synthetic ester of testosterone engineered for its longer activity. To be effective, its level must build up in the system of the animal using it. This process usually takes 2–3 weeks. Since 2007-11-15 National Institutes of Health retrieved that the proerectile aphrodisiac properties were concluded to likely be due to the release of nitric oxide from the nerve endings innervating the corpus cavernosum penis.

Extacts from T. terrestris standardised for protodioscin content have been demonstrated to produce proerectile effects in isolated tissues and aphrodisiac action in several animal species.
The mechanism for these effects has not been clearly established, and while protodioscin has been demonstrated to trigger release of nitric oxide in corpus cavernosum tissue, and also to produce statistically significant increases in the levels of the hormones testosterone, dihydrotestosterone and dehydroepiandrosterone in animal studies, evidence for efficacy in humans is limited and remains controversial (The effect of five weeks of Tribulus terrestris supplementation on muscle strength and body composition during preseason training in elite rugby league players, 2007).

In a study on rats, brain sections showed NADPH-d positive neurons in the paraventricular region of the hypothalamus. The staining intensity and the number of positive neurons were significantly higher in TT treated group than control. There was a statistically significant increase by 67% in the TT treated group compared to the control (p < 0.05); there was smaller number of AR in the control group compared to the TT treated one (p < 0.05); this increase was 58% in the TT treated group compared to control and was statistically significant (Effect of Tribulus terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain, 2005).


Careful though, as I tried a tribulus supplement a few years ago and it did something seriously strange to my enrves and my lungs. For a whole night I couldnt catch my breath and I had a serious panic attack, the next day I felt a bit mroe testosterone but then for a year or two after I could not eat carbs sugar or caffiene or I would have a giant stress response and subsequent panic attack. I am sitll ot sure what caused that exactly but the supplment I took onyl had tribulus, longjack and oatflower.
 
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bloom

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@Dhair

It sounds similar... following the trail, 5AR is needed for many conversions including the Preg -> Allo -> GABA... so Fin , unbeknownst to me, can have a profound affect on anxiety in ppl who have the slightest touch of clinical anxiety... it is these people i believe that suffer PFS which is why it's hard to pinpoint who will get it... still, the anxiety state from this GABA receptor downgrade and such could be along the lines of what quinolones did to you....

As I see it on this forum and with the recoveries of PFS, making the body 'right' is the first step... and you don't have to be suffering from an ailment to want to aim for that. Digestion/Diet (no seeds, avoiding PUFA) and baseline building blocks (preg, k2, D3, etc... ) all seem to help the first step. Of which I wouldn't stop when certain ailments subside...

2nd step, as @bloom is checking, is a specific issue and dialing up the supplementation to it... in this case, 5ar expression in the brain and it's cascading benefits (Depression, DHT effectiveness, Erectile issues as PFS sufferers deal with)...

@bloom what are you currently supplementing and looking to achieve , for clarity... increase of GABA via some supplement that crosses the BBB?? 5AR unregulation??
Nicotinamide 3g, 5a-DHP, small dose caffeine, L-theanine. B6 is a crucial co-factor for the last step of the synthesis of Dopamine and GABA. I'm currently reading everything I can on the Blood Brain Barrier. Haidut found a study which is at the beginning of this thread which has a list of drugs which increase 5ar in the Brain.
 

JoeKool

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@bloom yes yes, understood... I will be posting my latest supplement regiment over at my PFS thread here... Haidut's posts are genius so whatever he says goes... but here's something interesting...

"Before you take any supplements to repair a leaky blood-brain barrier (BBB), you might first want to test to see if your BBB is actually leaky or not
GABA is a neurotransmitter synthesized in the brain and is responsible for calming or inhibiting over activity. Although some companies sell GABA supplements, the reality is the GABA molecule is too large to pass through an intact blood-brain barrier. The fact that this supplement sells so well is a testament to the integrity of the average American’s blood-brain barrier

So, if several hours after taking 1000 mg of GABA, you feel calm, relaxed or sleepy, you know that GABA, a molecule too large to pass through the blood-brain barrier, has nevertheless made it into your brain and is performing its calming duties. This means your blood-brain barrier has become compromised and your brain is highly susceptible to the immune rampages I discussed above.

Some people, instead of feeling relaxed, will find GABA makes them feel more anxious or jittery. There are other reasons for this that will be discussed in my next book, however any reaction at all indicates a leaky brain barrier.

If you felt no change after taking GABA, that is a good sign that your blood-brain barrier is intact and functioning well. (For accurate results, be sure to take this test during the day and not at bedtime.) "


I haven't tested myself, and i think 1000mg is a small dose to test... perhaps 1.5G or 2G max to really sell yourself... but at night, I was using 750Mg GABA, L-Theanine or just xanax but have since moved to only L-Theanine and 5G Glycine... I actually measured what supplements returned nocturnal erections which indicated to me an increase in GABA was taking place...
 
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bloom

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We could try glue sniffing....

Elevation of steroid 5 alpha-reductase mRNA levels in rat cerebellum by toluene inhalation: possible relation to GFAP expression. - PubMed - NCBI

. Further studies indicated that toluene exposure increased steroid 5 alpha-reductase (5 alpha-R) mRNA levels prior to the elevation of GFAP mRNA in the cerebellum, whereas neither 5 alpha-R nor GFAP mRNA levels in the hippocampus were significantly affected by toluene exposure. These results suggest that toluene inhalation may enhance GFAP gene expression in the rat cerebellum, and propose the possibility that the elevation of 5 alpha-R expression, and hence 5 alpha-reduced metabolites of steroid hormones, is presumably related to toluene-induced GFAP mRNA expression.

From wiki:

Similar to many other solvents such as 1,1,1-trichloroethane and some alkylbenzenes, toluene has been shown to act as a non-competitive NMDA receptor antagonist and GABAA receptor positive allosteric modulator.[29] Additionally, toluene has been shown to display antidepressant-like effects in rodents in the forced swim test (FST) and the tail suspension test (TST).[29]

Toluene is sometimes used as a recreational inhalant ("glue sniffing"), likely on account of its euphoric and dissociative effects.[29]
 

TubZy

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Anyone try lions mane? I used it a while back and it helped mentally and can cross BBB. I don't know if it effects GABA though.

Also alpha GPC too.
 
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bloom

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cAMP and the stimulation of 5ar in glial cells.

Intracellular signalling systems controlling the 5 alpha-reductase in glial cell cultures. - PubMed - NCBI

The effect of the cAMP analogue appears to be specific for the 5 alpha-reductase, since the 3 alpha-hydroxysteroid-dehydrogenase did not show any variation after exposure to the drug. In conclusion, the present data suggest that proteinkinase A (PKA) might be involved in the control of the 5 alpha-reductase in glial cells.
 
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bloom

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OK this study supports my suspicion that Androgens can cause a negative feedback leading to decreased activity of 5ar in the Brain. This study found that testosterone given to male rats decreased activity of 5ar in the Pituitary, I really hope i'm interpreting this correctly.

Regulation of the pituitary 5 alpha-reductase activity by gonadotropin releasing hormone and testosterone in the adult male rat. - PubMed - NCBI

Testosterone administration to intact male rats decreased the pituitary 5 alpha-reductase activity and LH, while administered to castrated rats, it was able to suppress totally the castration-induced increase of the 5 alpha-reductase activity and of the gonadotropin secretion.

These data indicate that the pituitary 5 alpha-reductase enzyme system is controlled by both direct steroidal and indirect GnRH-mediated mechanisms.

@haidut I'd like your thoughts on this
 
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