Comment · Thu, March 7, 2013 · Ceretropic
Questions about acetylcholine receptor antagonism and various interactions
Original post in this thread
amirrorbehind · 1 points
I take Tramadol and I'm trying to understand what exactly it's doing to my body and what I might stack with it to alleviate anything unwanted.
* What are, in general, the consequences of acetylcholine receptor antagonism? By preventing ACh from binding from its receptors (nicotinic [alpha-7] and muscarinic [m1, m3]) is ACh actually not doing its job? Or doing its job less?
* Should I be supplementing choline in this situation? It seems like antagonism would prevent choline (and then ACh) from performing its functions, so perhaps choline supplementation would be a waste?
* In this situation, what would an acetylcholinesterase inhibitor do? I'm looking at Huperzine-A.
I'm looking at the table just under here[1] and I'm wondering, for M1 and M3, by antagonising these receptors, am I preventing those actions from occuring ? Or at least somewhat?
[1] http://en.wikipedia.org/wiki/Muscarinic_acetylcholine_receptor#Difference_in_G_proteins
Thanks for any and every response :).
What they were answering
Direct reply to the original post — see the thread post above.
u/MisterYouAreSoDumb · Ceretropic
Basically ACh receptor antagonists, especially muscarinic, are used as cognitive blockers. Scopolamine is one used a lot in rat studies to gauge the effectiveness of nootropic compounds. They stop the body's ability to learn and operate normally. You will notice lower cognitive ability when on them.
Tramadol has many other effects than just ACh antagonism. You have opioid agonism, serotonin release, NE reuptake inhibition, NMDA antagonism, etc. It affects a lot of systems.
* Should I be supplementing choline in this situation? It seems like antagonism would prevent choline (and then ACh) from performing its functions, so perhaps choline supplementation would be a waste?
* In this situation, what would an acetylcholinesterase inhibitor do? I'm looking at Huperzine-A.
If you are antagonizing the receptors, then adding in more choline or preventing it's breakdown is not going to be effective. You need substances that allosterically modulate the ACh receptors, or indirectly lead to increases in muscarinic receptor transmission. Luckily, most of the racetams have been proven to reverse ACh receptor antagonist effects, as most are tested against scopolamine. This may lower the effectiveness of the Tramadol, though. What are you using it for?