dormouse (Member)
04-19-00 02:35
No 122748
      Sodium gamma-Hydroxyvalerate, a new potent GHB analog -Rhodium  Bookmark   

Author Topic:   Sodium gamma-Hydroxyvalerate, a new potent GHB analog
Administrator posted 09-03-98 06:08 PM          
I have recently synthesized and personally bioassayed the effects of the
GHB analog 4-hydroxyvalerate (4-Methyl GHB), which to my knowledge is the
first GHB designer drug made.

In J. Med. Chem. 31(5), 893-897 (1988), in vitro GHB receptor binding
studies showed that 4-hydroxyvalerate was an approximately 15% more potent
GHB receptor agonist than GHB itself, and with a potency very near that of
T-HCA (trans-4-hydroxy-crotonic acid).

The synthesis was carried out as follows:

8 grams (0.2 moles) of sodium hydroxide was dissolved in 50 ml of methanol
with gentle heating, and some insolubles was filtered off. 20 grams of
gamma-hydroxy-valerolactone (0.2 moles) was added as fast as the exothermic
reaction allowed, the solvent was evaporated in vacuo, and the wet, soapy
residue was dried in a desiccator over CaCl2. The crude product was finely
ground in a mortar, placed in a buchner funnel, washed with 200 ml of
acetone and sucked as dry as possible at the pump. After drying over CaCl2,
the Sodium gamma-Hydroxy-Valerate, a deliquescent, white, crispy and
slightly soapy powder, weighed 26.9 grams (96% of theory) and had a
pleasant aromatic odor, and a taste not unlike that of Sodium GHB itself.

The Sodium 4-hydroxyvalerate was dissolved in a glass of water, and ingested
on an empty stomach. As anticipated, the taste wasn't too great, and it
reminded me of Sodium GHB. Within about ten minutes the first effects of
the material was felt, and the effects developed gradually during the first
30 minutes to at that point be clearly felt and distinguishable. The peak
effects are attained around an hour after ingestion. The first effects
noted are muscle relaxation, and a sense of calmness. At the half hour
point, a sedation can be felt, but the feeling is in part unlike that of
GHB itself, this feeling is more like natural sleepiness than the feeling
gotten from GHB and other sedating pharmaceuticals. At the same time, the
muscle relazation was attenuated, and the body felt very heavy. During
one experiment, with 1 gram of the material, I took a nap (voluntarily)
at about the one hour point, and when I spontaneously woke up an hour
later, I felt very relaxed and refreshed, and the sleep had been very fine.
At the two hour point, the muscle relaxation is diminished, as well as the
sedation. The effects gradually dissipates during the following hours, and
in my opinion, the duration of the effects is slightly longer, say 30-60
minutes, than with GHB.

When compared with GHB, there is more muscle relaxation, and the sedative
and anxiolytic effects are noticably more potent, preliminary, I'd say
that the compound is subjectively around 1.5 times stronger on a weight
basis. The mood elevating and sociabilizing effects are in my opinion
weaker than with GHB itself. The dosage levels tried so far has been
1000-2500mg of the dry sodium salt. No side effects has been noted,
except perhaps a slight nausea at the peak, but this can also be due to
the facts that all trials has been conducted on an empty stomach.


Administrator posted 09-03-98 07:30 PM          
Can you clarify what you mean by 'gamma-hydroxy-valerolactone'. Strike finds no listing for it in any database including, Chemsources USA, Chemsources International, ChemConnect database or Allured's.

Strike finds lots of sources for 'gamma-valerolactone'.

Are they the same?

Administrator posted 09-03-98 10:41 PM          
Yes, I cited the wrong name above, what I referred to was of course gamma-Valerolactone.