Phenibut a GABAb for anxiety?

[Mystery Brew]

Obviously Im not a expert on mechinism of substance.
But phenibut caught my eye.

Ive just skim thru a few pages.
Shulgina says phenibut binds to GABAa specifically

But Lapin (2001) real recent says it binds to GABAb...and may binds to A at high dose

Having rread baclofen is a analog binds to B. I have doubts about its anti-anxiety effects

Having said that Ive taken essecive aamounts of baclofen side effect wise (young n dumb)...phenibut an baclofen have similar effect...atleast from what i read..severe dizzyness, nausea, vomiting

my thoughts is its only GABAb binds from phenibut. Althought= theres alot of confusion and conflicted thoughts. so I cant be sure.

Im sure yall have a better understanding with this.

Can yall explain?

Tryna find something for general anxiety..that nervous tension,
So far im thinkin valerian reading that it binds to GABAa like benzos, would be perfect...but I have no idea what biochemistry goes on with this...

valerian and L-thenine

 

[MagickalKat777]

Unfortunately, phenibut builds an extremely rapid tolerance. It is not for general anxiety use. It is just as addictive, if not moreso, as a true benzodiazepine but can build tolerance in a few days rather than the weeks it generally takes benzos.

Valerian, on the other hand, is non-addictive but extremely light unless taken in very high doses. I had purchased an 80% Valerenic acid extract and it still took me 500mg of the stuff just to get the effects of *maybe* 3-5mg of Valium.

When it comes to general anxiety and nervous tension, magnesium is one of the few supplements that works quite well. Also in high doses.

 

[atara]

It's kind of hard to think of any anxiolytics that don't build a rapid tolerance, phenibut and baclofen certainly do not qualify. Exercise is I guess the obvious answer.

Aniracetam, perhaps, though some people hate racetams.

 

[Mystery Brew]

excercise definatly. Just workin my ass off n too tired after wards.

Shoot, I just got some valerian...before I read that even extracts could barely touch ya. But I have no tolerance to benzos now a days.

1mg of xanax recently taken puts me to a semiconious awareness. Cant remember how I got to bed when I woke up. but was consious before sleepiin

magikalkat: you have tolerance to benzos? or even in the past have you ever develop a tolerance?

atara: what were the rapid tolerance anxioytics were you thinking about?

AlsoI read somewhere in this forum L-thenine was supposedly good

 

[MagickalKat777]

Mystery Brew - Yes, I do currently have a (rather low) tolerance to benzos. I take 10mg twice a day of Valium. Quite low for a drug taker, although I started at 60mg and have had a smooth taper down. When I went to Valerian, I had a tolerance to 3mg of Xanax a day but still, Valerian's half-life, or rather, valerenic acid, has a half-life that is similar (from personal, not scientific experience), to that of Xanax. It doesn't last long and requires redosing except Xanax is one pill, Valerian, even extracted, stinks to high heaven and thensome and requires more - MUCH more. If we were counting milligrams, I would say that 80% Valerenic acid against 1mg of Xanax... I'd say 750-1000mg is equipotent. It would just be cheaper to have Xanax.

 

[Mystery Brew]

One of the chemicals in valerian is intresting.... valerenic acid. (not valeric acid)
Supposedly valerenic acid is a strong GABA a agonist. acting mainly at α1β2 and α1β3 subtypes. same as benzo. But the amounts of those in valerian is low probably...eh.

Valerenic acid from what I hear has definatly a benzo-feel to it. Intresting chemical none the less.

I dont know how people feel euphoria from benzodiazpine. Sadly other find that differnt. Being a heavy opiate user..benzo has no recreational value to me. People abusing this medication is giving me hell.

Currently Im on Celexa, Neurontin, Wellbutrin. Celexa is worthless, Neurontin makes me feel/react retarded (slow), Barely does anyything anxiety-wise. Wellbutrin makes me have more energy to get tru my day..but it seems like it just counter acts the other medication lethagic feeling. But also addes more nevous energy

The side effect is not worth it and asexuality is not worth it

Just that nervous energy is rediculous. I feel edgy when I wake up, I feel edgy when I sleep. Ive had anxiety issues since elementary school. An recently I have panic attacks. Im too scared to talk to strangers, even harder to talk to pretty girls. Scared. overanalyze social situations, Thinking everybody is talking shit about me., Scared of what people think about me = social anxiety. Its ruin my life. Ive been trying to get out of my comfort zone.

Opiates is my anxiolytics. But Of course the practicality is zero to none. Gives me energy, self-confidence, no anxiety, basically very reinforcing effects for someone like me.

Binding to opioid receptors, I suppose release dopamine, and uses endorphins. Not sure if serotonin is effected. Theres probably more it does if anyone can enlighten me...

My question is does endorphins, binding of opioid receptors, etc...does it have any effect on anxiety?

 

[basement_shaman]

Wow, cool to see this here, knowing that I was the one who found the Lapin article and added the information to the wiki page :D
Although you of course might have just searched for articles and found the same one as me, it's still cool.

Honestly, I think phenibut is the most anxiolytic substance I have ever tried. In doses of 1.2-1.8 grams it makes me extremely calm and serene, very much at ease with myself and everything. Not overly self-confident, just relaxed and energized at the same time. If I do 2 grams or more, I get a hangover the next day, nausea, dizziness, drowsiness. I think 1.6 grams is my sweet spot.

I think I can "feel" the very thing about it being selective for GABAb but binding to GABAa as well at higher doses - because it seems like there are two plateaus or levels of phenibut intoxication - there is the talkative, calm, anxiolytic "today is a good day for some reason" effect from 1-2 grams, and then you have the sedating, hypnotic, amnesic "whoah which way is up" effect from 2+ grams that leads to a hangover.

I wonder exactly what the Lapin paper means by "phenethylamine receptor antagonist". But if you look at phenibut's molecular structure.. wait, let me just launch Chem3D, hold on, I'll make a picture:

As you can see, the electromagnetic forces of the molecules are such that if you add a methyl or (to a lesser degree) an ethyl group to the beta carbon of phenethylamine, it changes the conformation away from the basic phenethylamine conformation (all structures in my image are MM2 minimized for minimum energy conformations), but the addition of a carboxylgroup changes it back to the basic shape. So I can imagine phenethylamine binding to sites where phenethylamine would normally bind - unable to be broken down by MAOs, it rests there, not activating the receptor but keeping phenethylamine from binding and activating.