• Log in with Facebook Log in with Twitter Log In with Google      Sign In    
  • Create Account
  LongeCity
              Advocacy & Research for Unlimited Lifespans

Photo
- - - - -

Inhibition constant of choline uptake by DMAE


  • Please log in to reply
1 reply to this topic

#1 kurt

  • Guest
  • 59 posts
  • 0
  • Location:SE Asia

Posted 21 May 2006 - 04:12 PM


Deanol acetamidobenzoate inhibits the blood-brain barrier transport of choline.

Millington WR, McCall AL, Wurtman RJ.

Competition by deanol (dimethylaminoethanol) with choline for uptake from the bloodstream into the brain was demonstrated by simultaneous intracarotid administration of carbon 14-labeled choline with deanol (plus tritiated water and indium 113m, to calculate a brain uptake index) and by measuring the brain uptake of 14C-labeled choline mixed with sera from rats pretreated with deanol (300 or 500 mg/kg 8 or 30 minutes earlier). The inhibition constant for inhibition of choline uptake by deanol (159 micrograms) was actually lower than the Michaelis constant for choline itself (442 micrograms); hence, the affinity of the carrier mechanism for deanol is at least as great as it is for choline. Deanol administration also elevated blood choline levels; thus, the effect of the drug on brain choline (and acetylcholine) levels is the result of the increase it produces in blood choline and the suppression it causes in choline uptake. These findings may explain discrepant results from laboratories seeking increases in brain acetylcholine or clinical improvement in patients with tardive dyskinesia after deanol treatment.


Does it mean that the amount of choline(transport to the brain) DMAE inihibits is more than the amount of choline elevated by DMAE itself?

If that's the case, I find it weird. I've not been taking anything new(for months) except for DMAE recently. I find it easier to concentrate on stuffs and my short term memory improved. I even had more intense workouts(more powerful muscle contractions) and had better dreams.

#2 kurt

  • Topic Starter
  • Guest
  • 59 posts
  • 0
  • Location:SE Asia

Posted 31 May 2006 - 08:40 AM

Nobody's interested?

I tend to believe that DMAE increases brain choline levels more than it inhibits(the transport of choline to the brain) though honestly I don't quite understand those scientific terms used in that study(somebody please explain?), but I had positive effects from taking it(as said in my previous post). Its takes 2 simple processes, methylation & acetylation(correct me if I'm wrong) for brain DMAE to convert to acetylcholine, so it could be potentionally a cheaper alternative to stuff like Alpha GPC. It has been shown to increase choline in the brains of rats anyway.

Dimethylaminoethanol (deanol) metabolism in rat brain and its effect on acetylcholine synthesis.

Jope RS, Jenden DJ.

Specific methods utilizing combined gas chromatography mass spectrometry were used to measure the metabolism of [2H6] deanol and its effects on acetylcholine concentration in vitro and in vivo. In vitro [2H6]deanol was rapidly taken up by rat brain synaptosomes, but was neither methylated nor acetylated. [2H6]Deanol was a weak competitive inhibitor of the high affinity transport of [2H4]choline, thus reducing the synthesis of [2H4]acetylcholine. In vivo [2H6]deanol was present in the brain after i.p. or p.o. administration, but was not methylated or acetylated. Treatment of rats with [2H6]deanol significantly increased the concentration of choline in the plasma and brain but did not alter the concentration of acetylcholine in the brain. Treatment of rats with atropine (to stimulate acetylcholine turnover) or with hemicholinium-3 (to inhibit the high affinity transport of choline) did not reveal any effect of [2H6]deanol on acetylcholine synthesis in vivo. However, since [2H6]deanol did increase brain choline, it may prove therapeutically useful when the production of choline is reduced or when the utilization of choline for the synthesis of acetylcholine is impaired.



sponsored ad

  • Advert
Click HERE to rent this advertising spot for SUPPLEMENTS (in thread) to support LongeCity (this will replace the google ad above).



0 user(s) are reading this topic

0 members, 0 guests, 0 anonymous users