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Sedatives of the Future

Thalidomid was thought to be the perfect sedative -until the incidents became obvious.
 
Anyone know anything concrete about gamma-vinyl-GABA or gammacronolactone or the corresponding acyclic compound?
 
Just to pick up on the methaqualone discussion, I have made all those non-scheduled analogs which according to the literature a equally or more potent than MQ. They all turned out to be useless. Lots of work and no reward :(.
 
Dr.Heckyll said:
Just to pick up on the methaqualone discussion, I have made all those non-scheduled analogs which according to the literature a equally or more potent than MQ. They all turned out to be useless. Lots of work and no reward :(.
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for what its worth I had access to mandrax in SA and it isn't all that. unless drooling is your thing. I can drool without methaqualone.. Methaqualone has supposedly got all these desirable effects but I think selective memory might be at work, if you can remember ludes in the 70's you weren't there.
 
I remember NegroGesic stating that many of the old timers thoughtful accounts of 'ludes were unfounded as they aren't that much better than benzos. I personally find benzos and the few barbs I have tried to be non recreational, even compared to ethanol.

Edit: I forgot to mention I haven't had a chance to give GHB a whirl, although it sounds like it might be a sedative I would enjoy.
 
Helios. said:
No, I think invented all of them.
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It shows, gamma chloro butyric acid is going to be an alkylating drug & therefore potential carcinogen/mutagen. The activity of GHB analogues seems to be dependant upon a free OH group, so the ether versions are likely to be worth their weight in crap!

The best bet for GHB analogues is either in modification of the carbon chain, keeping the same number of carbon atoms between the COOH & OH groups or esterification of both groups eg ethyl gamma acetoxy butanoate (but GBL achieves both of those in a simple molecule and isn't as well accepted as GHB)
 
I was doing a google search on GCB (does this nomenclature work?), and a 3 year old alt.drugs discussion was dropping some references that suggested that GCB did not have such properties and in fact retarded the growth of cancerous cells. When I have more time, I'll try and dig up these references.

ebola
 
Yeah, alkylating drugs do retard cancerous cell growth, but in a non-cancerous person they increase the risk by alkylating DNA. The reason they work with tumours is that they're generally fast growing and as such are more susceptable to alkylating drugs as they're reproducing much faster than other tissues (also why anti-cancer drugs normally exhibit side effects in tissues that have a fast cell turnover eg digestive tract, hair follicles etc).

Any halogen attached to an alkyl (as opposed to aryl) group is a potential alkylator - related to action of alkyl halides on ammonia to produce amines (or on primary amines to secondary amines etc).

R-Cl + NH3 = R-NH2 + HCl

The alkyl halides attack the nitrogens of the purines/pyrimidines of DNA bases and as such can cause transcription errors (leading to cancers if in the right place)
 
Ah.
Looks like the alt.drugs people were rather confused then.
And the take home message, for laypeople such as myself, is that GCB is unfit for human consumption.

ebola
 
CH3CH2OH is so old, socially accepted and easy to make that I predict it will retain its place as a sedative in the human recreational pharmacopoeia for years to come.
 
Helios. said:
CH3CH2OH is so old, socially accepted and easy to make that I predict it will retain its place as a sedative in the human recreational pharmacopoeia for years to come.
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Unless the world is over taken by eastern asians, who don't find ethanol to be very nice compared to westerners. (lack of acetaldehyde dehydrogenase IIRC)
 
>>Unless the world is over taken by eastern asians, who don't find ethanol to be very nice compared to westerners.>>

I wouldn't make a blanket statement like these. Many of the Japanese can DRINK.

ebola
 
Today, after eating a pita with leftover avocado, and having eaten a lot of guacamole, I thought to myself that I felt rather sedated, but kind of dismissed it before getting curious and going to pubmed.

Apparently, persea americana (avocado) does actually have relaxant and anticonvulsant properties, especially in the leaf:

Anticonvulsant effect of Persea americana Mill (Lauraceae) (Avocado) leaf aqueous extract in mice.
http://www.ncbi.nlm.nih.gov/entrez/..._uids=16775810&query_hl=4&itool=pubmed_docsum

Antispasmodic effects of Persea cordata bark fractions on guinea pig ileum.
http://www.ncbi.nlm.nih.gov/entrez/..._uids=17174038&query_hl=4&itool=pubmed_docsum

Vasorelaxant action of aqueous extract of the leaves of Persea americana on isolated thoracic rat aorta.
http://www.ncbi.nlm.nih.gov/entrez/..._uids=15990249&query_hl=4&itool=pubmed_DocSum

More intriguing plants:
Analgesic and anticonvulsant properties of Tetrapleura tetraptera (Taub) (Fabaceae) fruit aqueous extract in mice.
http://www.ncbi.nlm.nih.gov/entrez/...Retrieve&dopt=abstractplus&list_uids=16372367

Anticonvulsant activity of Harpagophytum procumbens DC [Pedaliaceae] secondary root aqueous extract in mice.
http://www.ncbi.nlm.nih.gov/entrez/...Retrieve&dopt=abstractplus&list_uids=16464685
Analgesic, antiinflammatory and antidiabetic properties of Harpagophytum procumbens DC (Pedaliaceae) secondary root aqueous extract.
http://www.ncbi.nlm.nih.gov/entrez/...Retrieve&dopt=abstractplus&list_uids=15742343

Anticonvulsant properties of the methanolic extract of Cyperus articulatus (Cyperaceae).
http://www.ncbi.nlm.nih.gov/entrez/...Retrieve&dopt=abstractplus&list_uids=11390127
 
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