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GABA receptors and Sedative/Hypnotics ("Sleep Meds")

BilZ0r, here is the "Ketamine the Opioid" thread I was referring to earlier, so that you may see at least 2 other studies investigating the opioid properties of Ketamine:
http://www.bluelight.ru/vb/showthread.php?s=&threadid=161358
It is not just kappa agonism I am speaking of, but mu-agonism as well...

On a subjective level, I have only ever found 5 drugs which have such a strong "pull" that it is difficult to moderate my use of them:
Oxycodone, Hydromorphone, Fentanyl, Morphine, and Ketamine (I've never tried Heroin)

I've sampled nearly every recreational drug, and have found other drugs with a "pull" but none of the same qualitative or quantitative nature of these 5. Another commonality is that all 5 put me into a very similar state of inexhaustible energy (mania?).

Ah, you're right, baclofen just prolongs, or worsens experimentally induced absence...
Click to expand...
Out of curiosity, why then is baclofen used as a drug for epileptics? On the subject of practical applications: our OD moderator Negrogesic has been prescribed baclofen to reduce cravings (I've read interesting stuff about baclofen preventing cocaine cravings) and to prevent seizures (possibly caused by trying to taper off his massive diazepam tolerance), is this a good idea? Is there another GABA-ergic drug which would be more appropriate?
 
 
Thanks Blowmonkey...

I stumbled upon this about the GABA-B agonism of Beta-Phenyl-GABA, a substance I am very familiar with. I take 400mg with 100mg of theanine about twice a week to de-stress after a long day of work (or at the tail-end of one), and find that it makes me VERY talkative, although I have not noticed ANY euphoria from this substance at ANY dose. Kinda blows my GABA-B = euphoria theory... Although I still am interested to learn more about the "GHB receptor", especially what makes GHB so damn euphoric... FYI it was Rhodium and one other Hiver (does anybody remember who?) who posted many abstracts about the GHB receptor in a similarly titled thread. I recall that the Erowid GHB abstracts database included some about the dysphoria of GHB.
See: http://www.erowid.org/chemicals/ghb/ghb_journal.shtml
Here's one in particular which stands out:
http://www.erowid.org/chemicals/ghb/ghb_journal1.shtml

Beta-Phenyl-GABA:
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8386087&dopt=Abstract
 
Yeah, I don't buy a single one of those papers... those EEG ones are just a bit shit, I mean, how many levels from the receptor are they removed? Interestingly, some of the papers report respitory depression, which is not common with ketamine, that is to say, ketamine is known not to induce respitory depression... so I don't quite know what to make of that... the Mu2 paper shows an affinity still about 10 times to hight, but thats kinda within errory/high dose ranges... importantly, the IC50 and the Ki are vastly out, which points to me that there is something completely fucked with what they are doing
 
LOL, there is? Ketamine has always been thought that it didn't cause respiratory depression in humans even at aneastethic dosages, though if you hear from reports both on and offline, you'll notice that lot's of people tell you just the opposite. OR there is something completely fucked about THESE articles, OR literature you've been reading has been wrong all along about ketamine not being able to induce respiratory depression.

I think that we're going a bit off-topic now..
 
Indeed, I just noticed, but one of the papers you cited says it in its 2nd sentance "this agent does not produce opioid-like respiratory depression"

Like this paper in humans, and this one in monkeys... Finally, 4mg/kg in over 1,000 children caused 1 case of respitory depression.

If I had time I'd find a nice review (which I think there might be one in JAMA, but I've lost the university password)
 
I'm no clinician, but I'd geuss, if a doctor new someone was a "drug addict" and they were going to tapper, and they might be prone to seizures, he'd WANT to give them diazepam, but he'd "know" he couldn't give him that, so he'd try a GABA-B agonist, vs a GABA-A 'agonist'. Importantly, GABA-B agonists can prolong absence seizures, but they help shorter tonic-clonic seizures.
 
BilZ0r, couldn't he use one, or a cocktail of, non-abused anti-convulsants (Depakote, Lamictal, etc.)? I don't see why a benzo would be necessary, although this isn't an area I have much knowledge in (I've just taken anti-convulsants for Bipolar and have some knowledge of a few).
 
I might geuss that he felt that because epilepsy and withdrawal induced seizures were etiologically different, that they needed to be treated differently... I don't really know, I'm just trying to explain it.
 
Thanks for the clarification (even though I don't understand it :))...I really know absolutely nothing about different types of seizures, or anything about seizures in general. I only know about certain anticonvulsants because I have taken them for off-label uses, mainly for my Bipolar disorder.
 
Hmm...a benzodiazepine with minimal hypnotic effects and is a strong anxiolytic and anti-convulsant...one particular product comes to mind:

Frisium (clobazam)

It's the first 1,5 structure benzo which supposedly affects the motor functions less than the 1,4 benzos. I've had quite a lot of these, since it's relatively cheap. It's quite long lasting and while it's not as strong and clonazepam in the anxiolytic and anti-convulsant department, it's not too bad either - in higher doses. Comes in 10 x 10 mg blister and the patent is still held by Hoechst, I believe.
 
I'm not that into the complexities of drugs/substances -n- their receptors in which they effect but I do kno the basics -n- then sum. Wut I'm gettin @ it as with Ambien/Lunesta which effect tha sleep GABA receptor (gaba-a or sumphin) seems to make perfect since why they would cause subconsience/dream-like effects or halluciations since that experience pretty much sums up REM sleep but when u still awake that would explain it all occuring then. Pretty basic analysis but jus thought of this -n- found it simply a no-brainer when one would think about it. Most of yall here already have come the same conclusion but jus wanted to state that for sum reason since there are a lot of sumwut-naive peeps on here who would find it interesting [I guess]. I'm pretty bored as well -n- jus postin ish so don't mind me if u educated in all this -n- find it insulting to your intelligence.... lol
 
sixthseal.com said:
Hmm...a benzodiazepine with minimal hypnotic effects and is a strong anxiolytic and anti-convulsant...one particular product comes to mind:

Frisium (clobazam)

It's the first 1,5 structure benzo which supposedly affects the motor functions less than the 1,4 benzos. I've had quite a lot of these, since it's relatively cheap. It's quite long lasting and while it's not as strong and clonazepam in the anxiolytic and anti-convulsant department, it's not too bad either - in higher doses. Comes in 10 x 10 mg blister and the patent is still held by Hoechst, I believe.
Click to expand...

Interesitng, Clobazam is a benzo I've yet to come across. You liken it to Clonazepam in terms of duration when you say "It's quite long lasting". Do you happen to have the half-life numbers for Clobazam and Clonazepam so an accurate comparison can be made?

What is considered a "higher dose"?

-Vaya
 
Ah I'm sorry, I forgot about benzo.org.uk. I can answer the first of my questions,for those interested:

Half Lives

Clobazam - 12-60 Hours

Clonazepam - 18-50 Hours

So by those calculations, Clobazam has the potential to be longer lasting than Klonopin, and to a lesser degree, Valium (which can reach 100 hour half lives, but has a minimum of 20 hrs.)

But again... 0.5mg of Clonazepam is equivelant to 20mg of Clobazam, so my question is, (and for the sake of simplicity let us assume in a non-tolerant individual, though I've got a monster one at the moment...) What would be a higher dose? 40mg? 60? 80, perhaps?

Thanks for any information you can provide me.
 
For a benzo naive person, you wouldn't need to go above 60mg... 40 would be enough for me.
 
Vaya said:
So by those calculations, Clobazam has the potential to be longer lasting than Klonopin, and to a lesser degree, Valium (which can reach 100 hour half lives, but has a minimum of 20 hrs.)

But again... 0.5mg of Clonazepam is equivelant to 20mg of Clobazam, so my question is, (and for the sake of simplicity let us assume in a non-tolerant individual, though I've got a monster one at the moment...) What would be a higher dose? 40mg? 60? 80, perhaps?

Thanks for any information you can provide me.
Click to expand...

I've used Clobazam many times, when I had no tolerance to benzos, but also when I had a huge tolerance.
From my experience, Clonazepam lasts a bit longer (maybe Clobazam stays longer in the system than Clonazepam, but the effects last shorter).

For someone with no tolerance to benzos, 40mg is a good starting dose.
When you have a big tolerance, it's hard to get effects from Clobazam. It's a pretty weak benzo... For someone who needs 10mg Clonazepam to get high, 10x20mg Clobazam tablets won't be enough to feel an effect.

(I think Clobazam is useful only as an anticonvulsant. It doesn't really have any recreationnal properies, unlike other benzos, and it doesn't even work very well as an anxiolytic or sedative...)
 
Again, thank you for your answer/response. Clobazam does not sound like something I'd find myself actively seeking out.
 
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