zarrin77

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"...Nicotinamide 4 had modest potency (IC50 = 350 nM) and was suprisingly unbound (rat plasma protein binding (PPB), 13.2% free) given the measured log D7.4 (3.2). Ligand efficiency was high as measured per heavy atom count (0.46) and moderate as measured by ligand lipophilicity efficiency30 (LLE = pIC50 − logD = 3.3). Sulfonamide 5 was more potent (IC50 = 200 nM) although less impressive in terms of ligand efficiency per heavy atom count (0.33) or ligand lipophilicity efficiency (2.8). The permeability of both was high as measured in a CACO-2 assay with no evidence of efflux."

Just have to point out that when they say “Nicotinamide 4 had modest potency (IC50 = 350 nM)....”, they are not acutally using niacinamide, but actually “compound 4” that they were tesing in the study (image below). They did not test niacinamide in this study.

ABA4DB29-0C21-4C6D-A802-C0E93A0EF547.jpeg
 

ddjd

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Jul 13, 2014
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any other suggestions for things that could lower 11b-HSD1?
 

Dr. B

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Mar 16, 2021
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@haidut

Mate i do think its anti cortisol but im convinced niacinamide and a lot of these fatty acid inhibitor supplements actually have catabolic effects?

If youre into bodybuilding you may recognize a specific sensation you get in your muscles particularly the arm muscles like biceps and triceps. Its a specific type of muscle burning that only occurs if you don’t consume enough protein, or if you do excessive cardio, or both. It has nothing to do with the burning sensation you get while actually lifting weights.

Anyway niacinamide and a few other supplements, i think aspirin as well, cause that same muscle burning sensation that i would get from doing extreme cardio or going a day or two without eating proper protein.

I think its because cortisol is meant to step in to prevent the body from breaking down its own tissues for energy? So if the metabolism goes too high, normally cortisol will also rise to some extent?
And the thing is niacinamide doesn’t really increase sugar cravings or appetite for me so it’s tough to attempt to stuff a lot more carbs while using niacinamide or aspirin, to attempt to possibly offset their muscle burning effect.

I am also wondering about effects on sleep… so naked juice brand sells a certain vitamin fortified juice which contains added niacinamide, b5, b6, and b12. The dunkin donuts refresher contains this same mix of added vitamins.

I doubt its b6 since that is used as a sleep aid. However one or more of the other b vitamins, causes a severe sleep problem. Far beyond even caffeine. Like if i take that mixture of b3, b5,b6 and b12 i wouldnt be able to sleep until 15+ hours after drinking it. So im not sure which vitamin but something in those four b vitamins causes issues falling asleep
 

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