RCs Carbamate derivatives safety?

[neal301]

Hello all,

I have been researching trying to find tranquilizers that are non toxic and easy to obtain.

I came across the carbamate derivatives because they are all available directly from manufacturers and are unschedueled (exception soma and meprobamate).

However, I realize that carbamate and many of its relative chemicals are extremely toxic and carcinogenic, so I was wondering if it would be worth it to experiment with any of these substances.

Some examples: Lorbamate, Tybamate, Nisobamate etc...

Thank you also, if you know of any other regularly available legal compounds that are safe and are tranquilizers please let me know.

 

[neal301]

bump

 

[falsifiedhypothesi]

If you know some derivatives are toxic and these chemicals are largely untested I wouldn't risk it. Unless you can find information either from the manufactures or online about the safety of these drugs you probably shouldn't touch them, do some of your own research and don't just trust answers people give you in an online forum.

 

[sekio]

Just because carbamate (ethyl carbamate) is toxic does not mean all compounds with a carbamate functional group is a carcinogen.

Citalopram has a -CN group but it does not have the toxicity of cyanide.

The diversity of carbamate drugs means you can't make generalized statements about their safety or toxicity. Look up the individual drugs in the literature to find LD50 and effective doses as well as contraindications etc. Many carbamate drugs are old enough that there is at least a little body of literature relating to their usage.

 

[Euphorogenesis]

The carbamates have been shown to have barbiturate like effects with some of them even being able to activate GABAergic neurons in the absence of GABA itself. If you ask me i'd say this property would make them especially dangerous when combined with other CNS deppresants, however the efficacy of these effects seems to vary widely from derivative to derivative. I wouldn't be able to tell you anything about a safe dose but i would advise you to proceed with caution under any circumstance.

Have a look at this interesting study about the pharmacology of felbamate and meprobamate.

Felbamate and meprobamate are structurally related propanediol dicarbamates that possess distinct pharmacological profiles. Felbamate is a minimally sedative, broad-spectrum anticonvulsant, whereas meprobamate is a strong sedative-anxiolytic agent. Previously, we reported that felbamate potentiates gamma-aminobutyric acid(A) (GABA(A)) receptor Cl- currents and inhibits N-methyl-D-aspartate (NMDA) receptor currents. Here we further characterized the interaction of the two dicarbamates with GABA(A) receptors to determine the basis for their pharmacological differences. In whole-cell voltage-clamp recordings from cultured rat hippocampal neurons, meprobamate enhanced GABA-evoked responses in a concentration-dependent manner and, at high concentrations (>1 mM), exhibited a separate channel-blocking effect that limited the magnitude of GABA(A) receptor potentiation. At equivalent concentrations, meprobamate produced substantially greater potentiation than did felbamate. Furthermore, meprobamate (but not felbamate), in the absence of GABA, directly activated Cl- currents that could be attenuated by the GABA(A) receptor antagonists bicuculline and picrotoxin. The mean deactivation time constant of whole-cell currents evoked by 10 mM meprobamate (110 ms) or 1 and 3 microM GABA (180 ms) were faster than the deactivation time constant of 10 mM meprobamate (490 ms) or 3 mM felbamate (470 ms) in the presence of GABA. Meprobamate and felbamate prolonged the mean burst duration of GABA-activated unitary currents in excised outside-out membrane patches. In addition, at high (supratherapeutic) concentrations, meprobamate blocked NMDA-activated currents. We conclude that felbamate and meprobamate have barbiturate-like modulatory actions on GABA(A) receptors, but meprobamate has greater activity and, unlike felbamate, is able to directly activate the receptor.

http://www.ncbi.nlm.nih.gov/pubmed/9067327

 

[neal301]

Thank you for the informative replies, the main compound that interests me is tybamate as it is a prodrug for meprobamate like carisprodol. has anyone heard of/seen this compound?

 

[blowjay]

Are the carbamate functional groups primarily responsible for the action of the drugs or would - in the case of carisoprodol and meprobamate - 2-Methyl-2-propyl-1,3-propanediol be responsible for the actions?

 

[meprobamatedowned]

I have heard of Emylcamate, which was patented in 1961 for anxiety, but i'll have to look further for litterature around its developement and effects on humans. It's making its way to the surface of the market i think

edit: i just looked a bit into those drugs from the same class (they are not carbamate chemically speaking but they were studied for the same effects, in 1959-1960 i think) : Phenaglycodol, Fenpentadiol, they were both sedatives, the second one was marketed under the name Tredum or Trefedum. Analogs would be rather easy to imagine...

 

[Asante]

Ots interesting to note that when you heat an alcohol with urea, noxious fumes are given off and the carbamate results.

But seriously, the functional group is carcinogenic. Better not touch.

 

[meprobamatedowned]

Ots interesting to note that when you heat an alcohol with urea, noxious fumes are given off and the carbamate results.

But seriously, the functional group is carcinogenic. Better not touch.

i mean if you wanna get into rc's.... everything is pretty much considered carcinogenic until the oposite is proven