Question: On one hand, I read so much furor about GHB that it doesn’t seem worth trying. On the other hand, I see compounds such as acetyltyrosine, acetylcarnitine, phosphatidylcholine, xanthinol nicotinate, amino chelates, etc. all designed to improve absorption. I have a hard time believing that there is no similar compound of GABA (probably unpatentable) which gets it into the blood stream and across the blood-brain barrier. I think I rattled off 3 or 4 different mechanisms above, there must be more. Any comments? ——SDH

Answer: N-acetyl-GABA eh? Or maybe cyclic-GABA (2-pyrrolidone, i.e., gamma-butyrolactam)? This latter compound is a cyclic version of GABA which could be hydrolyzed to GABA, if such a reaction were sufficiently favored. But it doesn’t appear to be so. First of all, polyvinylpyrrolidone (a vinyl polymer containing lots of pyrrolidone residues) does not appreciably hydrolyze, even when lots of it is used as a blood plasma extender. Secondly, pyrrolidone is a monomer for the production of Nylon-4, a polymer known for its stability in water and resistance to alkali hydrolysis. Nylon-4 is really a GABA chain (see illustration), linked in an acid-to-amine configuration. A Nylon-4 dimer (two GABA molecules linked acid to amine) would be very similar to N-acetyl-GABA in basic chemistry, but it is not very clear to me how readily this compound would hydrolyze back to GABA.

Although Dr. Henri Laborit hoped that GHB would be a precursor to GABA, the opposite appears to be the case. When GHB is given to animals, the concentration of GABA in the brain does not appreciably increase. However, when GABA is given, GHB levels increase significantly. This would suggest that GABA might be able to produce a GHB-like state, if you could get enough of it into the brain.

It is possible that low-molecular-weight polymers of GHB may be able to deliver GHB in a time-release manner. Although these have not been synthesized and characterized to my knowledge, GHB genes have been grafted into cotton to produce a “natural” cotton-polyester blend fiber. So far, the GHB-polyester content is only a small fraction of 1% of the cotton, but that may be able to be increased with further efforts.
——SWF