New benzo agonists with simple structure

[Deleted member 170540]

I found a recent, interesting article about the BZD receptor binding and anxiolytic effects of several sulfamide compounds:

http://www.ncbi.nlm.nih.gov/pubmed/22056620

N,N'-dicyclohexylsulfamide and N,N'-diphenethylsulfamide are anticonvulsant sulfamides with affinity for the benzodiazepine binding site of the GABA(A) receptor and anxiolytic activity in mice.

Abstract

A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-diphenethylsulfamide (10), competitively inhibited the binding of [(3)H]-flunitrazepam to the benzodiazepine binding site with K(i)±SEM values of 27.7±4.5μM (n=3) and 6.0±1.2μM (n=3), respectively. The behavioral actions of these sulfamides, i.p. administered in mice, were examined in the plus-maze, hole-board and locomotor activity assays. Compound 7 exhibited anxiolytic-like effects in mice evidenced by a significant increase of the parameters measured in the hole-board test (at 1 and 3mg/kg) and the plus-maze assay (at 1 and 3mg/kg). Compound 10 evidenced anxiolytic activity in the plus-maze and the hole-board tests at 1mg/kg. Locomotor activity of mice was not modified by compound 7 or 10 at the doses tested. Flumazenil, a non selective benzodiazepine binding site antagonist, was able to completely reverse the anxiolytic-like effects of these sulfamides, proving that the GABA(A) receptor is implicated in this action. Anxiety represents a major problem for people with epilepsy. The use of anxiolytic and anticonvulsant sulfamides would be beneficial to individuals who suffer from both disorders.

(I also have access to the full text, if someone wants to see it)

It seems surprising to me that something with this simple structure can effectively act as a benzo... These compounds are also probably easy to synthesize, maybe this is a promising new candidate for the RC market...

 

[Epsilon Alpha]

Looks like it might cause severe allergies to some people with issues with sulfamide antibiotics, tread very carefully...

 

[Deleted member 170540]

Yes there's certainly no way to know what side effects these compounds could have, but at least its mentioned in the full text that no neurotoxicity was observed in a previous study.

The full text mentions that the compounds tested didn't affect locomotor function like diazepam, so these could be 'anxioselective', causing no sedation. Whether these drugs support self-administration or cause benzo-like physical dependence is still unclear.

 

[atrollappears]

The full text mentions that the compounds tested didn't affect locomotor function like diazepam, so these could be 'anxioselective', causing no sedation.

!!!
This sounds extremely promising, both in terms of therapeutic and recreational use. I wonder whether these compounds affect cognitive function as much as diazepam---the long-term cognitive damage that results from daily benzo use is one of the scariest things about them IMO.