1-Methyl-Benzodiazepine RC's

[trip407]

So is there currently any RC Benzodiazepine with a 1-Methyl subtitution available? I think diclazepam is the only one available and i don't like that very much.

But why don't they release 1-methyl-Clonazepam or some 3-Hydroxy derivatives with methyl substitution like 3-hydroxy-Flunitrazepam rathern then all these triazolo analogues that are highly amnesic, toxic and too potent/hypnotic.

I am also waiting for water soluble analogues of midazolam. I can understand that these are maybe not potent enough, but how i loved the short rush of midazolam ampoules.

 

[Solipsis]

If they will be temazepam-like I am SO on board :D

Which triazolos are toxic tho? Toxic how?

 

[roi]

There's Cloniprazepam which should metabolize into 1-methylclonazepam.

 

[Solipsis]

How so? Prazepam metabolizes into desmethyldiazepam, not diazepam. Fat chance the cyclopropyl is cleaved but not the methyl / cyclopropylmethyl substituted for a random methyl..

Unless I am mistaken you might wanna correct that in the cloniprazepam thread..

 

[aced126]

Yeah I don't think cloniprazepam would be metabolised to the 1-methyl derivative. Dealkylation of that might be harder than just demethylation, I'm thinking maybe the cyclopropyl undergoes ring opening hydroxylation...

 

[Solipsis]

Like I said, prazepam is known to metabolize to the descyclopropylmethyl (well yeah and also 3-hydroxylation first)... so metabolism on the 1-position of cloniprazepam is not likely to be different, aced.

OK so not sure if nordazepam is favored or oxazepam as metabolite, may have been wrong about that - but that's not really that relevant.

http://www.tandfonline.com/doi/abs/10.3109/00498257309151546

 

[roi]

Right, so it would be a straight clonazepam prodrug?

In that case diclazepam is the only 1-methyl (non-triazolo) benzodiazepine RC available right now.

 

[XANAX XR]

If they will be temazepam-like I am SO on board :D

Which triazolos are toxic tho? Toxic how?

Woaaah, settle down there.

What is the hype of temazepam about...? What characteristic does it have that, per say, xanax and clonazepam do not have?

 

[Solipsis]

Hype? Well I wasn't speaking for anyone but myself there... But I've sampled plenty of benzos and while I appreciate the anxiolytic action of xanax and clonazepam there seems to be much less focus on benzos that are muscle relaxant and that can 'hit' you in a certain way. Examples would be temazepam, nitrazepam and flunitrazepam. Definitely not all benzo's make you as woozy when they kick in. Also midazolam perhaps but that is also seriously hypnotic. A different one for different occasions, to be sure: pyrazolam is selective for the anxiolytic side and IME nitrazepam is relatively selective for muscle relaxation as far as benzos go.. I think clonazepam is nice by the way but it annihilates my short term memory so hard that it's just not funny anymore.

So talking of characteristics, but not of hypes.. not all benzos are created equal of course, without judging really they may vary in the degree that they act as:
- anxiolytic
- hypnotic
- (skeletal) muscle relaxant
- anti-convulsant

Feel free to choose your own poison! Although anti-convulsants hardly seem that relevant unless you are a person who is having convulsions

I do feel like I should add that we ought to be thankful for the RC benzos being made available, not every type of drug has very successful RC candidates available these days..

 

[XANAX XR]

Interesting... Do you think Nifoxipam would carry similar characteristics to flunitrazepam?

 

[Solipsis]

In my experience, nifoxipam has some of the feel of flunitrazepam but is milder by comparison.. Nifoxipam goes a bit into the oxazepam direction. Still a damn nice find but as a hypnotic and certainly as a muscle relaxant it's a little 'diluted', compromising to become anxiolytic as well. So the answer would be: partially yes..

 

[clubcard]

Flutemazepam and why no 1-methyls? LAZY CHEMISTS

 

[Solipsis]

Lazy IYO as in 'too lazy to think of the value in it', or as in 'too lazy to bother to do azepine methylations' cause they are particularly bothersome for some synth reason?

 

[clubcard]

Lazy -adding the 1-methyl to the benzophophenone gives quantitative yield..... but it's 1 (simple) extra step... a LITTLE EXTRA WORK Is TOO MUCH FOR THEM!