Using benzo antagonists to reset benzo tolerance

[Ivanhoe]

Two easily available substances are Benzo Receptor Antagonists.

They are Caffeine and Theophylline.

If I use one of them during a week, will my benzo tolerance be reduced?

 

[morphiquet]

these two substances aren't benzo/gaba-antagonists, but adenosine-receptor antagonists.

 

[BilZ0r]

And even if they were benzodiazepine antagonists (at least I don't think they are), they shouldn't reverse tolerance.

 

[Ivanhoe]

There are monographs bout drugs that are considered as the reference here in France (so they are in french).
It clearly say for both caffeine and theophylline that they are benzodiazepines antagonists....

 

[BilZ0r]

Learn something every day... still, I suspect it's pretty weak, and completely irrelevant to human doses and as I said, even if you do get significant effects, benzo antagonists wont help you reverse tolerance.

Acta Pharmacol Toxicol (Copenh). 1982 Oct;51(4):300-8.
Binding of beta-carbolines and caffeine on benzodiazepine receptors: correlations to convulsions and tremor.
Saano V, Airaksinen MM.

Neurosci Lett. 1982 May 28;30(2):161-6.
Effects of caffeine and theophylline on adenosine and benzodiazepine receptors in human brain.
Boulenger JP, Patel J, Marangos PJ.

 

[fastandbulbous]

^ BilZ0r, are the beta-carbolines antagonists or inverse agonists?

To anybody interested, there's a difference - look up benzos, inverse agonists and the Cl- channel if you want to know more, I'm off to bed.

 

[BilZ0r]

*shrug* an inverse agonist might reverse tolerance... yeah, but it would also put your at risk for seizures, panic and other assorted nasty shit.

 

[brainiacthemaniac]

I assume an inverse agonist acting on the chloride channel (Cl-) would essentially be the same thing as the action of naloxone on the mu-receptor for opioids?

 

[BilZ0r]

Well I'm not sure how constitutively active the Mu-opioid receptor is, and hence whether you can have real inverse agonist effects... however, some reports say that it is, an naloxone is an inverse agonist.

But inverse agonists at the benzodiazepine site on GABA-A receptors should decrease GABA affinity and decrease bursting.

 

[brainiacthemaniac]

Cool, thanks....