Dopamine agonists

[perfectphase]

8-OH-PBZI: A Highly Selective Dopamine (D3) Agonist

8-OH-PBZI is a potent selective agonist for D3 receptors, some info is provided at this page: http://www.sciencedirect.com/science/article/pii/S0014299997013721. In humans the Dopamine D3 receptor is found in high concentrations in the Mesolimbic region of the brain. Activation of these receptors is perhaps one of several pathways to the experience of reward and pleasure upon taking many types of drugs. An interesting article in the journal Neuropsychopharmacology found here provides some information on D3 receptor antagonists. This is mere speculation but this compound could potentially offer a unique feeling of pleasure without causing as powerful of a come down as other Dopaminergics such as Cocaine and Amphetamines due to its rather different mechanism of action. I don't think there is enough research done but it seems that this compound could have activity without significantly affecting SERT or DAT which would make it very unique. I welcome any discussion, insight or information related to 8-OH-PBZI and/or the D3 receptor as I'm certainly not an expert on the matter...

 

[specialspack]

What are dopamine agonists like? Most recreational dopaminergic drugs are re-uptake inhibitors or releasers, yes? I know lots of drugs have partial dopmamine agonism as part of their effects, but non work via agonism in the way the psychedelics do with 5HT-2A?

Wikipedia says they have a range of side effects, some of which sound potentially recreational, but the list of substances they all seem to be treatments for Parkinsons, with nothing noted on the psychoactive effects.

http://en.wikipedia.org/wiki/Dopamine_agonist

 

[perfectphase]

Yes I was wondering the same things, having never tried a selective Dopamine agonist I can't offer any input. Theoretically these could be very interesting assuming they work in a similar way to other receptor agonists (like 5-HT2A agonist psychedelics). I'm wondering if anyone here has any experience with them.

 

[MyDoorsAreOpen]

What are dopamine agonists like? Most recreational dopaminergic drugs are re-uptake inhibitors or releasers, yes? I know lots of drugs have partial dopmamine agonism as part of their effects, but non work via agonism in the way the psychedelics do with 5HT-2A?

Wikipedia says they have a range of side effects, some of which sound potentially recreational, but the list of substances they all seem to be treatments for Parkinsons, with nothing noted on the psychoactive effects.

http://en.wikipedia.org/wiki/Dopamine_agonist

This.

Most centrally-acting dopamine receptor agonists have little to no recreational merit. Many of them do have psychoactive side effects, more so in some patients than others. But these effects don't fall under most people's definitions of 'fun' or 'productivity enhancing'. These drugs are poorly tolerated by a lot of patients put on them therapeutically.

By way of analogy, if you wanted more output from a water wheel, you'd open the sluice gates and let more water in. Getting a group of people to come push segments of the wheel as if there were water flowing through it isn't going to achieve the same effect. Of course if you open the sluice gates, your reservoir empties faster, but that's another problem altogether.

Edit: interestingly enough, most centrally acting serotonin receptor agonists don't fit a lot of people's definition of fun either, although they're undeniably psychoactive for most people. And again as with dopamine, they're not nearly as intrinsically appealing as drugs that jack up the synaptic concentrations of serotonin.

 

[crOOk]

the current and hopefully ongoing d3r antagonist research sounds a lot more promising to me personally. a regulatory system that has only 2 known functions, one of them apparently playing a key role in substance addiction, seriously gives me a tiny bit of hope that my downward spiral of substance abuse can some day gain wider acceptance by society as a clearly defined pathological mechanism that can be contrary to all other aspects of the person suffering from it. It will hopefully lead to promising results in pharmacological addiction treatment that might allow a life without constantly having to fight off overwhelming impulses and often inexcplicable urges, that seem to be extremely resistant towards any form of inhibition.

There is a promising d3 antagonist being tested on non human primates atm for this purpose, but it is not selectively targetting an isoform of d3r that is considered responsible for the positive reinforcement mechanism that plays a leading role in substance seeking behaviour and is seemingly very resistant against inhibition through influences of other behaviour determining variables. instead it might worsen tardive dyskinesia which is still assuemed to be caused by hypersensitive d2r receptors.
I'm just wondering if and how said d3 antagonist might affect glutamate mediated neuroplasticity and the ability to learn through positive outcomes of decision making. does anyone know more?

 

[basement_shaman]

You sound a lot like me, crook. I have the same urges, the same wants, the same constant need. I too wonder if what I am 'suffering' from will one day be looked upon society as a disability of my brain instead of my mind. As though my force will is the same as other people's, as it truthfully is. I hope whatever trials they have going end up successful. I believe that, within my lifetime, real tangible progress will be made. Neurochemistry as a field of science is less than a lifetime old, and look at the progress that has been made thus far. I myself am studying to become a medicinal chemist, hoping to one day help synthesize the drug that cures addiction as a whole.

 

[crOOk]

Hehe studying medicine myself and am planning to head the same way. Maybe we end up working together in ten years, you never know. Much from Germany and all the needed strength to hold up the balance needed to pull through!