Prami, prolactin, and growth hormone

[aidenmanofrisque]

Do any of the DA's activate the D4 receptors? i know D2,3,4 and usually grouped together when discussed generally

 

[bushleaguechew]

Do any of the DA's activate the D4 receptors? i know D2,3,4 and usually grouped together when discussed generally

Yes they all do slightly, but prami has the highest affinity.

 

[STAUNCHED427]

Actually I believe prami, unlike bromo, does not possess affinity for the 5HT2B subtypes receptors therefore cardiac fibrosis is not an issue (activation of the 5HT2B receptor have been shown to cause cardiac fibrosis/ventricular enlargement ie, fenfluramine, a serotonergic stimulant originally intended for weightloss untill people suffered cardiac fibrosis which was proven to be due to excessive 5HT2B receptor agonism due to the metabolite norfenfluramine).

Also, I think caber does have affinity for the 5HT2B receptor albeit far les than bromo. Not only that but I am pretty sure the doses that were shown to cause 5HT2B agonism/cardiac fibrosis where doses used for parkisons treatment, not low doses used to control prolactin.

 

[simplytim]

great right up, apprecaiate time n effort, thanks!

 

[STAUNCHED427]

Just to back up what I was saying...

Pharmacokinetic evaluation of... [Expert Opin Drug Metab Toxicol. 2011] - PubMed - NCBI

Pramipexole is a non-ergot agonist with selective affinity for dopamine receptors of the D2 subfamily, in particular D3. Pramipexole has a very low affinity for serotoninergic 5-HT2A and 5-HT2B receptors, as well as D1-type receptors. Furthermore, it does not carry the risk to induce valvular heart disease or pulmonary and retroperitoneal fibrosis, seen with long-term use of the ergot-derived dopamine agonists. The recent introduction of a once-daily formulation poses significant advantages for patients, reflected by relatively stable plasma levels. The most obvious benefit is convenience of use and better adherence to treatment schedule. Additional advantages could include the opportunity to provide more continuous drug delivery in a fashion that could help minimize dyskinesia risk, if the drug is used early in the disease course.

 

[bushleaguechew]

Actually I believe prami, unlike bromo, does not possess affinity for the 5HT2B subtypes receptors therefore cardiac fibrosis is not an issue (activation of the 5HT2B receptor have been shown to cause cardiac fibrosis/ventricular enlargement ie, fenfluramine, a serotonergic stimulant originally intended for weightloss untill people suffered cardiac fibrosis which was proven to be due to excessive 5HT2B receptor agonism due to the metabolite norfenfluramine).

Also, I think caber does have affinity for the 5HT2B receptor albeit far les than bromo. Not only that but I am pretty sure the doses that were shown to cause 5HT2B agonism/cardiac fibrosis where doses used for parkisons treatment, not low doses used to control prolactin.

Your correct. We were discussing the activation of dopamine receptors not the serotonin receptors.

 

[STAUNCHED427]

Was referring to this part of one of your posts above dude

And finally bromocriptine has been shown to cause valvular heart disease.

Which is a direct cause of 5HT2B receptor activation.

 

[bushleaguechew]

Was referring to this part of one of your posts above dude



Which is a direct cause of 5HT2B receptor activation.

Gotcha. Didn't mean to come off as rude brotha

 

[STAUNCHED427]

Gotcha. Didn't mean to come off as rude brotha

Me either

 

[aidenmanofrisque]

Also the effect of dopamine agonists on the rewards system is very real. They should not be misused. Their use should be minimal and only as needed or you could end up being sorry as someone above mentioned.

ya i definitely notice when using a DA that I smoke(tobacco) a lot more. Where as i usually smoke out of habit, while driving or after eating, I would just want to smoke for the feeling. I also live in Atlantic City, NJ so the casinos seemed to be calling my name.

 

[Johnboy66]

I know this thread is a few months old, but, a really outstanding read. Makes you stop and think. That's a good thing.