108 replies to this topic

[PWAIN]

Complain to Anthony about the availability of nicotinamide riboside. I brought it to his attention and said he's looking into it but I don't think he fully grasps its potential as a supplement yet or how many people are interested.

I just found this from a strange source... sorry it took a while FunkOdyssey.

I am arranging a sample for testing.

A

Let us know how this goes...very intrested.

[JChief]

This was a very informative thread. Any current reports of niacinamide use providing beneficial results?

[3AlarmLampscooter]

I took 500mg of Nicotinamide today, and noticed effects within about a half hour. My response was a fairly strange combination of increased concentration and alertness combined with anxiolysis and a sort of calm, sluggish physical feeling. Reminded me a lot of benzos, except being with clear nootropic action. I'd combine with stimulants, as I personally like being a little speedier; but it looks like a great alternative to benzos for anxiety.

Edit: Also an effective anti-acne medication (I've tried topically, supposedly orally also) and in high concentrations a safe skin bleaching agent.

Edited by 3AlarmLampscooter, 28 June 2013 - 11:07 PM.

[anagram]

Taking Niacin supplements increases prostaglandin synthesis? http://www.ncbi.nlm....pubmed/21774590 Does this mean that Niacin can effect hair loss?

[3AlarmLampscooter]

Niacin and Niacinamide are two different chemicals. For one, Niacinamide causes no "flush".

[ta5]

Nicotinamide Riboside is being produced by Chromadex under the name Niagen.

It's available in this product called HPN NR:
http://www.tigerfitn...en-p/niagen.htm
It lists 250mg Nicotinamide Riboside

[garcia]

Nicotinamide Riboside is being produced by Chromadex under the name Niagen.

It's available in this product called HPN NR:
http://www.tigerfitn...en-p/niagen.htm
It lists 250mg Nicotinamide Riboside

Has anyone tried this yet? Does it live up to the hype?

[alan.r]

I've been wanting to experience niacin flush for the hell of it. What's the best form and at what dose?

Any plain old niacin. Just look for a bottle that doesn't say "time release" or "anti-flushing". I forget what the dosages are, but I used to take niacin daily on the theory that it must help with circulation and "flushing out toxins".

One time I took it after eating a couple of bananas and wound up terribly nauseous, which put me off both bananas and niacin.

[jakord]

Scienceguy pointed out that nicotinamide might be neurotoxic. Also, it seems like it's a bad idea to take sert-releaser while on it.

Abstract
gamma-Aminobutyric acid (GABA) modulation of triazolam and nicotinamide binding to benzodiazepine (BDZ) receptors in vitro was compared with the neurotoxicity and anticonvulsant activity of these two drugs in vivo. GABA had no significant effect on the inhibitory potency of triazolam in [3H]flunitrazepam receptor binding, whereas GABA decreased the inhibitory potency of nicotinamide. When administered to mice, both triazolam and nicotinamide [niacinamide] exhibited neurotoxicity by the rotorod test and anticonvulsant activity by the pentylenetetrazol seizure threshold test. This suggests that GABA modulation of the receptor binding of a BDZ ligand in vitro is not a reliable predictor of the pharmacologic activity of the ligand.

PMID: 2859562




-Deoxy-D-glucose prevents and nicotinamide [niacinamide] potentiates 3, 4-methylenedioxymethamphetamine-induced serotonin neurotoxicity.

Hervías I, Lasheras B, Aguirre N.

Source
Department of Pharmacology, University of Navarra Medical School, Pamplona, Spain.

Abstract
Neurotoxicity induced by different substituted amphetamines has been associated with the exhaustion of intracellular energy stores. Accordingly, we examined the influence of 2-deoxy-D-glucose (2-DG), a competitive inhibitor of glucose uptake and metabolism, and nicotinamide, an agent that improves energy metabolism, on 3, 4-methylenedioxymethamphetamine (MDMA)-induced 5-hydroxytryptamine (5-HT; serotonin) deficits. Administration of MDMA (15 mg/kg i.p.) produced a significant hyperthermia, whereas 2-DG caused a profound hypothermia that lasted throughout the experiment. When MDMA was given to 2-DG-treated rats, an immediate but transient hyperthermia occurred and was followed by a return to hypothermia. 2-DG had no effect on 5-HT concentrations in the frontal cortex, hippocampus, and striatum but prevented the neurotoxicity induced by MDMA. When rats were injected with 2-DG/MDMA and were warmed to prevent hypothermia, the protection afforded by 2-DG was abolished. Nicotinamide had no effect on body temperature of the rats, and the hyperthermia induced by the nicotinamide/MDMA treatment was similar to that of the saline/MDMA-treated rats. However, the long-term 5-HT deficits induced by MDMA were potentiated by nicotinamide [niacinamide] in all the brain regions examined. Finally, no change on ATP concentrations in the frontal cortex, hippocampus, and striatum was observed up to 3 h after a single dose of MDMA. These results suggest that an altered energy metabolism is not the main cause of the neurotoxic effects induced by MDMA.

Edited by homopharma, 21 December 2013 - 10:13 PM.

[jakord]

Anyone have experience if Niacinamide helps with OCD or obsessive thinking in general?

[mikey]

 

I've been wanting to experience niacin flush for the hell of it. What's the best form and at what dose?

Any plain old niacin. Just look for a bottle that doesn't say "time release" or "anti-flushing". I forget what the dosages are, but I used to take niacin daily on the theory that it must help with circulation and "flushing out toxins".

One time I took it after eating a couple of bananas and wound up terribly nauseous, which put me off both bananas and niacin.

 

 

Quick-release niacin will cause flushing in doses for some people as low as 35 mg, but if one wants to be sure to experience a flush 100 mg will assure it.

 

However, it was used in treatment of schizophrenics with some reported success by Abram Hoffer, MD, Ph.D, (in biochem) in the 50's and 60's at doses as high as 3,000 mg/day, which causes tremendous skin flushing for the first few days of taking it.

 

Interestingly, Hoffer was a champion of high-dose niacin used therapeutically.

 

He also experimented with LSD, reporting successful treatment of alcoholics, as well as other controversial treatments with nutritional therapies that were widely criticized by conventional medical organizations, but have been shown recently to have potential merit. See: http://www.scienceda...20308224524.htm

and http://www.medscape....warticle/821971

 

Funny how conservative medical folks end up looking like fools sometimes after they've committed themselves to close-mindedness and as Steven Colbert once said, "Tight assholes." 

 

And by the way, I wake myself up every morning by taking 500 mg of niacin with my coffee and have, basically taken daily high doses of niacin for over 46 years, since I first read of Hoffer's work.

[OneScrewLoose]

BTW, I was finally able to have a Niacin flush. The first time I kept taking doses of 300mg, until I reached 900mg, before it finally kicked in. The second time it only took 300mg. This was a while ago and I have no idea what it would be like now.

[mikeinnaples]

I can do 2g of niacin and not flush. Besides, one should simply take aspirin to avoid the flush if it is an issue for them plus it keeps NA serum levels higher for a longer period of time. Here is a quick and general summary from the other, and quite long thread, on the subject. Keep in mind that as of this post, the timing of supplements still needs to be worked out in regards to circadian rhythm as that has quite a profound effect.

 

Interestingly, the coadministration of aspirin with nicotinic acid mitigates the annoying episodes of flushing that occur with this drug, and it increased the apparent bioavailability of the drug by yielding greater and prolonged nicotinic acid plasma concentrations for a given dose. - source

 

 

Personally, I liked the flush and its unfortunate I no longer do it. I still believe NA is an alternative to NR with the side affect of improving your lipid profile. The question is which is going to be the most effective considering dose/price/safety points. Interestingly enough, NA is actually better at increasing NAD+ levels in some cells as compared to NR.

 

 1hupmd.jpg.gif   20.97KB   6 downloads

 

On a side note, nicotinamide is not an option as far as I am concerned for health reasons, not to mention, it is less effective than NA at increasing NAD+.

 

 

Build up the precursor supply with NA and Aspirin:

 

NA -> NaMN -> NaAD -> NAD+

 

or NR:

 

NR -> NMN -> NAD+

 

 350px-NAD_metabolism.svg.png   7.6KB   4 downloads

 

 

Open up the NAD+ flood gates by inhibiting CD38 - source

 

Apigenin, Quercetin, Cyanidin 3-glucoside, Luteolin

 

PARP 1 Inhibition to Increase NAD+ levels:

 

Resveratrol

 

Methyl donors if supplementing NA (maybe with NR too but less so) and/or you are an under-methylator

 

TMG, SAM-e, Methylcobalamin, Methylfolate

 

Increase AMPK to increase NAD+

 

Exercise, Resveratrol, Metformin, Quercetin, ECGC, Curcumin, Garlic

 

[Darryl]

mikeinnaples:

 

NR may also offer lipid benefits. Indeed the lipid benefits with high-dose NA may arise mostly through its effects on the NAD⁺/sirtuin system.

 

Although the G protein–coupled receptor GPR109A was linked to the effects of niacin, an increase in NAD⁺ could also contribute, especially considering the central role of sirtuin enzymes in lipid metabolism. Arguing in favor of the latter hypothesis is the fact that high doses of niacin (grams/day) are required for lipid lowering, while the EC₅₀ for GPR109A (i.e., concentration to activate 50% of the receptor; 250 nmol/L) is rather low. Interestingly, supplementation with NR decreased the LDL/HDL ratio in mice without activating GPR109A, suggesting that this may be true. This would circumvent the GPR109A-mediated adverse effects, such as flushing, observed upon high-level niacin intake.  Houtkooper, Riekelt H., and Johan Auwerx. "Exploring the therapeutic space around NAD+." The Journal of cell biology 199.2 (2012): 205-209.

 

 

If true, that means improvement in lipid profile from baseline may offer a very rough gauge of NAD⁺/Sirt1 activation with any intervention.

 

Aspirin, or more correctly salicylate, has a three fold benefit with NA:

 1) directly activates AMPK (↑ PGC-1α phosphorylation, required for Sirt1 activity; increases Nampt expression, favoring NAD⁺ salvage from nicotinamide)

 2) it competes with NA for glycine conjgation, and hence maintains higher serum levels

 3) reduces flushing from NA

The first benefit of aspirin should apply to NR supplementation as well.

 

After I discovered I could donate a pint of blood in 4 minutes with 1 g/d aspirin, I opted for magnesium salicylate instead. Aspirin irreversibly inactivates COX and impairs clotting in the 20 minutes its present, which accounts for the gastric and intracerebral bleeding issues. Its metabolite salicylate hangs around longer, and is responsible for the AMPK activation (and perhaps the anti-cancer benefit); ie, the benefit I'm seeking without the risk of bleeding out in an accident. Magnesium salicylate is an over-the-counter backache remedy, branded as Doan's and inexpensive as drug store brands. I still take 1 baby aspirin. Prescription salsalate is still better for maintaining high serum salicylate, but is rather expensive for an old generic.

Edited by Darryl, 15 April 2014 - 04:05 PM.

[mikeinnaples]

mikeinnaples:

 

NR may also offer lipid benefits. Indeed the lipid benefits with high-dose NA may arise mostly through its effects on the NAD⁺/sirtuin system.

 

Although the G protein–coupled receptor GPR109A was linked to the effects of niacin, an increase in NAD⁺ could also contribute, especially considering the central role of sirtuin enzymes in lipid metabolism. Arguing in favor of the latter hypothesis is the fact that high doses of niacin (grams/day) are required for lipid lowering, while the EC₅₀ for GPR109A (i.e., concentration to activate 50% of the receptor; 250 nmol/L) is rather low. Interestingly, supplementation with NR decreased the LDL/HDL ratio in mice without activating GPR109A, suggesting that this may be true. This would circumvent the GPR109A-mediated adverse effects, such as flushing, observed upon high-level niacin intake.  Houtkooper, Riekelt H., and Johan Auwerx. "Exploring the therapeutic space around NAD+." The Journal of cell biology 199.2 (2012): 205-209.

 

 

If true, that means improvement in lipid profile from baseline may offer a very rough gauge of NAD⁺/Sirt1 activation with any intervention.

 

Aspirin, or more correctly salicylate, has a three fold benefit with NA:

 1) directly activates AMPK (↑ PGC-1α phosphorylation, required for Sirt1 activity; increases Nampt expression, favoring NAD⁺ salvage from nicotinamide)

 2) it competes with NA for glycine conjgation, and hence maintains higher serum levels

 3) reduces flushing from NA

The first benefit of aspirin should apply to NR supplementation as well.

 

After I discovered I could donate a pint of blood in 4 minutes with 1 g/d aspirin, I opted for magnesium salicylate instead. Aspirin irreversibly inactivates COX and impairs clotting in the 20 minutes its present, which accounts for the gastric and intracerebral bleeding issues. Its metabolite salicylate hangs around longer, and is responsible for the AMPK activation (and perhaps the anti-cancer benefit); ie, the benefit I'm seeking without the risk of bleeding out in an accident. Magnesium salicylate is an over-the-counter backache remedy, branded as Doan's and inexpensive as drug store brands. I still take 1 baby aspirin. Prescription salsalate is still better for maintaining high serum salicylate, but is rather expensive for an old generic.

 

My understanding is that NA works through a different pathway to affect the lipid profile.

 

See this, that was attached earlier:

 

 post-3050-1227441321.gif   80.09KB   4 downloads

 

Regarding the Magnesium Salicylate, I wonder how safe that would be to take long term. Depending on how much we would need to take to get the intended effect, it may or may not be expensive. Most of what I see in the stores around here is a box of 24 capsules for around $6 ... each containing the equivalent of 467mg of mag salicylate.

[aribadabar]

 

 3) reduces flushing from NA

 

 I can anecdotally report that I had the most intense niacin flush ever when combining my usual 500mg NA dose (which I sometimes don't feel at all) with 580mg percogesic (=467 Mg salicylate OTC backache remedy).

Usually I only feel the flush in my head/face but this time my face,neck, shoulders, arms and isolated patches on my torso have been flushing red as if I have been sunbathing all day on the beach on a hot summer day. 

 

Any idea what or which compounds can contribute to this opposite effect? 

 

Thanks!

Edited by aribadabar, 23 April 2014 - 02:56 PM.

[Darryl]

Typically, for prevention of flush, the aspirin/salicylate is taken 0.5 to 1 hour before the NA, giving time for its COX inhibition to take effect.

 

I too have noticed more intense flushing with coingestion, which I presume is just a sign of competition for glycine conjugation and higher levels under the curve. As I've been dosing twice a day, every day, my prostaglandin D2 levels are somewhat exhausted, leading to the usual higher tolerance. 

[aribadabar]

Dephasing the salycilate intake with 0.5h did indeed the trick with the elimination of the flushing.

 

Thank you, Darryl!

[aribadabar]

A follow-up question: Тoday, after taking the usual 500mg niacin no flush occurred until after consuming some some walnuts ~3h later (caused by omega-3?). Usually, the flush is coming much sooner, or not at all. I noticed similar delayed flush effects after eating certain foods.  I am wondering if the niacin needs certain catalyst(s)to boost its action/efficiency and if the flush is an indicator of or just a concurrent (and not necessarily proportional) effect of its NAD-boosting capability?

 

Does this make sense or my reasoning is faulty?

 

Thanks!

Edited by aribadabar, 04 July 2014 - 04:30 AM.