Author Topic: NMDA Antagonists From Anti-Depressants?!  (Read 2574 times)

0 Members and 1 Guest are viewing this topic.

Bwiti

  • Guest
NMDA Antagonists From Anti-Depressants?!
« on: November 29, 2001, 06:39:00 PM »
What's up folks?! Ever since I was 16 years-old, I've been battling major depression, OCD, pessimism, and anxiety. Knowing this, it's safe to assume that I've tried just about every anti-depressant out there, but I've never taken the time to take a look at their chemical structures, until now. Check-out the structure of Effexor(Venlafaxine Hydrochloride): R/S)-1-[2-(Dimethylamino)-1-(4-Methoxyphenyl)Ethyl]Cyclohexanol Hydrochloride. I'm a HUGE fan of ketamine, tiletamine and other PCP-analogues, so naturally this excites me! Effexor and it's metabolite(O-desmethylvenlafaxine) are potent inhibitors of serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake, and hardly have any muscarinic cholinergic effects. What the fuck's up with that? When I looked at it's chemical structure, I was surprised that this isn't an n-methyl-d-aspartate receptor antagonist. What part of this compound is preventing this action? I know that 4-methoxyphenyl-cyclohexyl-dimethylamine would most likely put me into a sweet k-hole, so is it that ethyl on Effexor that prevents dissociation? What would you do if you wanted to convert this compound into an NMDA receptor site antagonist? There must be some way....In order to get goods from this, I need to know what's "wrong" with it. I'm sure that some of you have Effexor or similar drugs laying around, that never worked out for you, and I'd hate to see this feedstock go to waste. Any suggestions would be much appreciated. Btw, a picture of Effexor, it's major metabolite, and it's two minors can be found in Pat. EP1135359,

http://l2.espacenet.com/dips/viewer?PN=EP1135359&CY=gb&LG=en&DB=EPD

on page 4. Peace! 8)

  Split a piece of wood and I am there. Lift a stone and you will find me.

Bwiti

  • Guest
Re: NMDA Antagonists From Anti-Depressants?!
« Reply #1 on: November 30, 2001, 02:36:00 PM »
The paperwork that goes with a box of this stuff says that venlafaxine has virtually no NMDA antagonist effects. Hmmmm, maybe they're full of shit, or maybe in vitro studies are fucking unreliable, because here's the abstract of an interesting patent I found:

Use of substances capable of blocking the production of glutamate for treating tension-type headache
EP1132082


Abstract:
Tension-type headache is treated by interacting with neuronal transmission in relation to pain in connection with headache in a way that prevents or decreases sensitization of second order nociceptive neurons. In particular, treatment is performed by administration of an effective amount of a substance which prevents or decreases central sensitization. Important examples of such substances which interacts with glutamate neurotranmissions, such as glutamate receptor antagonists, such as NMDA receptor antagonists, such as MK-801 or Amitriptylline or Imipramine or Desipramine or Mirtazaprine or Venlafaxine. According to a broader aspect of the invention, tension-type headache is treated by administration of substances which are effective in preventing or decreasing pain in connection with tension-type headache, such as the substances mentioned above.


  Split a piece of wood and I am there. Lift a stone and you will find me.

timsong

  • Guest
Re: NMDA Antagonists From Anti-Depressants?!
« Reply #2 on: November 30, 2001, 03:03:00 PM »
I've been on Effexor before, it is quite a nasty AD if you want to get off of it. Although doctors say that it is not addictive, the body certainly craves for it when you stop taking it,leaving me with whoshing noises in my head and agression attacks for 3 weeks after stopping. The best AD i've been prescribed was Zispin, this had no side effects for me and I stopped using it no problem.

The best treatment for depression is cognitive methods, but if you suffer bi-polar depression you will need medicine.

I have investigated lots of AD's that i've been on, but none of them have been any good for turning into anything more stimulating !

Keep Happy  ;D  :)  ;D  :)  ;D

Bwiti

  • Guest
Re: NMDA Antagonists From Anti-Depressants?!
« Reply #3 on: December 01, 2001, 02:31:00 AM »
"but none of them have been any good for turning into anything more stimulating !"

  Speaking of "stimulating", I flat-out quit speed, coke and other drugs like them, and as a result, my life is better. MDMA, Ketamine, Weed and tiletamine are all good!
  How could I get helpful info on Effexor? Should I email the company that produces it, and ask what it is that makes it a serotonin/noradrenaline re-uptake inhibitor, and not an NMDA antagonist? What should I do? Rhodium? Peace!
8)

  Split a piece of wood and I am there. Lift a stone and you will find me.

Rhodium

  • Guest
Re: NMDA Antagonists From Anti-Depressants?!
« Reply #4 on: December 01, 2001, 09:15:00 AM »
I guess that doing a search on medline for a SAR on venlafaxine-like compounds would give you some hints. If that doesn't help, then just email them and ask...

Bwiti

  • Guest
Re: NMDA Antagonists From Anti-Depressants?!
« Reply #5 on: December 02, 2001, 09:03:00 PM »
I'm searching for info, but I can't find anything useful on effexor-like drugs. Medline? Is it easy to hack artilces from them? What's their url? Peace! 8)

  Split a piece of wood and I am there. Lift a stone and you will find me.