How To Counteract Against Carbergoline Agonist Affinity For 5-HT2C

[Kunstruct]

How to counteract against Carbergoline agonist affinity for 5-HT2C Serotonin receptor?

Pumping up GABA is not a solution as that will inhibit Dopamine too, which this medications has to raise, but at the same time Carbergoline is a pretty good agonist for 5-HT2C and 5-HT1B

 

[Kunstruct]

Yohimbine seems to work as 5HT1B antagonist and also Adrenergic receptors antagonist. Now sure why then many report pounding heart and anxiety on Yohimbine if it is a Adrenergic receptors blocker. Also seems to be an antagonist on D2 and and D3, which seems to work against Carbergoline in this case.

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Yohimbine - Wikipedia

 

[Sativa]

It would seem that 5-HT2C down-regulates whether an HT2C agonist or antagonist is used.
No need to worry about some HT agonism really, it's all quite taken out of context by people here!

HT1A activation reduces ALL HT receptor activity!
HT2A activation stimulates BDNF release! aka anabolic brain neuron food...

 

[Kunstruct]

Very interesting.

Carbergoline is only a mild agonist for 5-HT1A and 5-HT2B

 

[Kunstruct]

Could Bromocriptine be a better substance for raising D2 and lowering Prolactin comapred to Cabergoline?

I see Carbergoline affinity for D2 receptors not as high as Bromocriptine.

Cabergoline:

D1 214 Binding Affinity (Ki [nM]) Agonist
D2S 0.62 Binding Affinity (Ki [nM]) Agonist
D2L 0.95 Binding Affinity (Ki [nM]) Agonist
D3 0.79 Binding Affinity (Ki [nM]) Agonist
D4 56.2 Binding Affinity (Ki [nM]) Agonist
D5 22.4 Binding Affinity (Ki [nM]) Unknown


Bromocriptine:

D1 682 Binding Affinity (Ki [nM]) Agonist
D2 2.96 Binding Affinity (Ki [nM]) Agonist
D3 5.42 Binding Affinity (Ki [nM]) Agonist
D4 328 Binding Affinity (Ki [nM]) Agonist
D5 496 Binding Affinity (Ki [nM]) Agonist

 

[Kunstruct]

@Sativa
What do you think about the above post?

 

[Sativa]

@Sativa
What do you think about the above post?

Personally i don't think that Carbergoline or Bromocriptine are properly designed, they have such messy pharmacological profiles. There are much more strategic & elegant natural alternatives imho.

I mean geeze, look at this crap! So much crap going on, it's bound to influence the D2 agonism, & contribute questionable pharmacoligcal effects...

...cabergoline is commonly described principally as a dopamine D2 agonist, it also possesses significant affinity for the D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B- receptors, and moderate/low affinity for the D1and 5-HT7 receptors. Cabergoline functions as an agonist at all of these receptors except for 5-HT7 and α2B-, where it acts as an antagonist​

 

[Kunstruct]

Personally i don't think that Carbergoline or Bromocriptine are properly designed, they have such messy pharmacological profiles. There are much more strategic & elegant natural alternatives imho.

I mean geeze, look at this crap! So much crap going on, it's bound to influence the D2 agonism, & contribute questionable pharmacoligcal effects...

...cabergoline is commonly described principally as a dopamine D2 agonist, it also possesses significant affinity for the D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B- receptors, and moderate/low affinity for the D1and 5-HT7 receptors. Cabergoline functions as an agonist at all of these receptors except for 5-HT7 and α2B-, where it acts as an antagonist​

Yes, I know lots of agonizing on tons of things (including Adrengeric receptors) even if the description if of a D2 agonist.

Well I ask these questions as someone has 2 micro adenoma on the pituitary and has very high prolactin for several months, so the prescription was Cabergoline.
Do you think there is a better alternative to this in the given condition of hyperprolactinemia with pituritary adenomas?

 

[Sativa]

If the intention is to lower prolactin, then any natural D2 agonist is ideal. There are many botanicals that perform this action.

 

[Kunstruct]

If the intention is to lower prolactin, then any natural D2 agonist is ideal. There are many botanicals that perform this action.

Which would be those botanicals that are proven to work with studies?
I mean this thing which people do on this forum, saying they "feel prolactin today and less tomorrow" is quite far from someone who's got it proven ultra high for months and has MRI showing adenoma, who also does not even have low thyroid.