The 0.5 mg tabs are fameliar.
The dosage has raised of the recent Pyrazolam pelllet's to 3 mg at which it gets a little sedating. Can you compare it to Clobazam whichh seems unigue in its lack of sedative effects.
Clobazam is uniquely a 1,5-benzodiazepine and binds to the γ2/3δ2 domains.
Once you reach 20mg [BID] you result in almost 100% receptor occupation. I did post a link somewhere on the supraclinical dosing of patients suffering myoclonus and their was no difference they could find except longer duration.
But in the UK at least, their are only 2 benzodiazepines licenced for the use of myoclonus - clobazam [BID] and clonazepam [TID] an unusual selection to say the least.
I have boxes and boxes of clobazam lying around (due to doctor f*cking up and even though the instructions say 'two tablets mornings and evenings ' they gave me twice as many.
Clobazam doesn't appear to cause abstinence syndrome. Yes, the myoclonus returns, but none of the symptoms people associate with benzo withdrawal.
For a long time I have believed that clobazam should be a [P] rather than a [POM] since it's only half as active as diazepam, doesn't appear to produce dependence or addiction and is very useful for people in the short-term management of anxiety,
I should add that people have produced related 1,5-benzodiazpines such as arfendazam and lofendazam (both prodrugs of clobazam) and CP-1414S which has an 8-nitro instead of an 8-chloro. Human studies suggest that it's more sedating and extrapolating from the patent, is twice as potent.
Researchers produced the triazolo derivatives but I couldn't find any activity data. BUT if you find a derivative that has a plateau that is more like 40mg of diazepam... it would be of interest.
As well as pyrazolam, we also had pynazolam and pyeyzolam made for us:
https://ibb.co/KKsngWd
Can someone who knows how to make the images appear on the page please fix this for me.
Pyrazolam you all know, pyeyzolam is the alcohol mimic professor Nutt's compaby 'GABA industries' bought off me BUT pynazolam is the best by far, It's well known that the nitrobenzodiazepines are serotonin releasers (and more recently that they are dopamine deregulators) BUT sharing the anxiolytic properties of pyrazolam, pynazolam proved to be a potent serotonin releaser which obviously increases the anxiolytic properties but also produced a potent anti-depressant activity beginning at 20 minutes and lasting for about 6 hours.
For medical purposes obviously a sustained release formulation or possibly further modification of the drug would be needed. I would have liked to have tried removing the 2-methyl as it's oxidation is the main metabolic pathway. When etizolam was modified in such a manner it's potency halved but it's duration was longer and if it's the serotonin release isn't altered, it might be the better option...
Because every single person who sampled pynazolam asked for more. Everyone appreciated the value of pyrazolam and anything that mimics alcohol will be popular. BUT it was the pynazolam everyone asked for.
BTW Anyone wonder why pyrazolam has a 7-bromo? Because we used bromazepam as our starting point. It's the ONLY benzo to have a 2-pyridyl in place of a benzene or '2 substituted benzene.
That pyridine is why it took years for anyone to copy. I figure that either someone else spotted that OR someone went though the nightmare of staring from the bromazepam precusrors.
So if you ever see pynazolam for sale, let me know. It's my personal favourite benzodiazepine (and seemingly 41 others) but at the moment you only have my word on that and I would like honest feedback from a larger group.