AlloP - Liquid Allopregnanolone For Lab/R&D

[katiekeen]

Oleic acid

Thank you!

 

[Mufasa]

For female rats, does it need to be taken only after ovulation (like progesterone), or could it be used in the first 2 weeks of the cycle as well?

 

[haidut]

@haidut
I am very late to the game and am trying to learn a lot. I ordered 5a-DHP already and want to know if there is any reason 5a-DHP could be better or if it is inferior in all ways. Thank you!

I don't know if one is inferior or superior, they interconvert into each other quite effectively so raising the levels of one will raise the levels of the other.

 

[haidut]

What lab do you use to test the purity of your product after it has been synthesized?

We typically use Sigma Aldrich testing services as we have a contract with them.

Testing

We are a leading provider of contract services in the biopharmaceutical industry, supporting every phase of the testing, development and manufacturing process and offering a comprehensive and integrated package of services.

www.sigmaaldrich.com

 

[haidut]

As it seems allopregnanolone also has strong thyroid boosting effects ,aside from its anti-stress actions .
It agonizes the bile a of receptor TGR5 ,which increases energy expenditure, mostly via increasing T4 to T3 conversion .
I just dont know how much mg is needed to achieve micromolar concentrations of allopregnanolone.

"As shown in the present study, TGR5 is also expressed in astrocytes and neurons. Here, TGR5 may act as a neurosteroid receptor, which is activated by nanomolar concentrations of 5β-pregnan-3α-ol-20-one and micromolar concentrations of 5β-pregnan-3α-17α-21-triol-20-one and 5α-pregnan-3α-ol-20-one (allopregnanolone).

The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain - PubMed

TGR5 (Gpbar-1) is a membrane-bound bile acid receptor in the gastrointestinal tract and immune cells with pleiotropic actions. As shown in the present study, TGR5 is also expressed in astrocytes and neurons. Here, TGR5 may act as a neurosteroid receptor, which is activated by nanomolar...

pubmed.ncbi.nlm.nih.gov

Yes, we have a thread on that topic.

How Pregnenolone And Progesterone Raise Metabolism

I know pregnenolone/progesterone work via multiple mechanisms such as inhibiting serotonin, opposing estrogen, lowering FFA, etc. However, this method caught my eye and I thought I'd share it since many people here have trouble converting T4 into T3. As you all know both pregnenolone and...

raypeatforum.com

 

[Mauritio]

Yes, we have a thread on that topic.

How Pregnenolone And Progesterone Raise Metabolism

I know pregnenolone/progesterone work via multiple mechanisms such as inhibiting serotonin, opposing estrogen, lowering FFA, etc. However, this method caught my eye and I thought I'd share it since many people here have trouble converting T4 into T3. As you all know both pregnenolone and...

raypeatforum.com

From that topic:" However, it is only able to do so at micromolar concentrations, which, similarly to the case of the L-VGCCs, are far greater than the low nanomolar concentrations of allopregnanolone estimated to be present in the brain.[15]"

So it seems unlikely to agonize this receptor with allopregnanolone.

 

[haidut]

From that topic:" However, it is only able to do so at micromolar concentrations, which, similarly to the case of the L-VGCCs, are far greater than the low nanomolar concentrations of allopregnanolone estimated to be present in the brain.[15]"

So it seems unlikely to agonize this receptor with allopregnanolone.

The nanomolar concentrations are what is endogenously present. When administering several milligrams (or more) exogenously micromolar concentrations are likley to be achieved. In fact, the antidepressant effect of the FDA-approved Brexanolone is likely (partially) due to stimulating thyroid synthesis and metabolism. The GABA agonism alone is not enough to explain the antidepressant effect as pure GABA agonists such as the benzodiazepine class of drugs do not have antidepressant effects but only antianxiety ones. The increase in dopamine mentioned in a previous comment and antagonism of serotonin (below) are probably also involved in the overall antidepressant effects.

Progesterone, Testosterone, Allopregnanolone Are Serotonin Antagonists

This study shows that some of the gonadal steroids act in a manner similar to the drug ondansetron - i.e. antagonize the 5-HT3 "receptor". While pregnenolone sulfate was not antagonistic to 5-HT3, taking pregnenolone metabolizes mostly into progesterone and allopregnanolone. So, it seems like a...

raypeatforum.com

 

[mogwog]

I wonder how this would stack with Cortinon+ 8:1

 

[Makrosky]

Very nice haidut!! Thanks for keeping up the exciting work!

I have some questions:
1) Is there any risk of supressing endogenous allopregnanolone or anyother hormone synthesis?
2) Is there any risk of upregulating/downregulating any other neurotransmitter, neuropeptide or hormone pathways?

For instance, plain pregnenolone doesn't have any of these risks at any dose AFAWK (as far as we know here in RP forum).

3) I remember you saying some years ago in some posts that too much allopregnanolone could cause some feelings of aggression or anxiety (can't remember exactly). Do I recall correctly?
Edit : Yes, it has a Biphasic u-shaped action curve. Just saw it on wikipedia.

4) Can it have some "feminizing"/anti-androgenic effects like sometimes in some doses for some people progesterone/pregnenolone does?

Thanks a bunch!!!

 

[Makrosky]

Nice , I ordered :)
also asked Peat what he thinks about direct allopregnanolone supplementation. I guess his answer will be:" just supplement progesterone or pregnenolone" , but we will see ...

hahahhah I would bet 50 bucks that's what he will say. Please post it here :)

 

[haidut]

Very nice haidut!! Thanks for keeping up the exciting work!

I have some questions:
1) Is there any risk of supressing endogenous allopregnanolone or anyother hormone synthesis?
2) Is there any risk of upregulating/downregulating any other neurotransmitter, neuropeptide or hormone pathways?

For instance, plain pregnenolone doesn't have any of these risks at any dose AFAWK (as far as we know here in RP forum).

3) I remember you saying some years ago in some posts that too much allopregnanolone could cause some feelings of aggression or anxiety (can't remember exactly). Do I recall correctly?
Edit : Yes, it has a Biphasic u-shaped action curve. Just saw it on wikipedia.

4) Can it have some "feminizing"/anti-androgenic effects like sometimes in some doses for some people progesterone/pregnenolone does?

Thanks a bunch!!!

Can't talk about risks/safety. That is against FDA rules. All I can say is that studies so far do not demonstrate suppression of endogenous synthesis of other steroids of neurotransmitters. There are no reports of hormonal effects either. Unlike progesterone, 5a-DHP, etc allopregnanolone seems to be similar to pregnenolone - i.e. mostly a neurosteroid, devoid of "classical" hormonal effects through receptors such as PR, ER, AR, GR, etc.

 

[Mufasa]

Can't talk about risks/safety. That is against FDA rules. All I can say is that studies so far do not demonstrate suppression of endogenous synthesis of other steroids of neurotransmitters. There are no reports of hormonal effects either. Unlike progesterone, 5a-DHP, etc allopregnanolone seems to be similar to pregnenolone - i.e. mostly a neurosteroid, devoid of "classical" hormonal effects through receptors such as PR, ER, AR, GR, etc.

Does that also mean that it can not alter the menstrual cycle if taken at the wrong time of month like progesterone does?

 

[haidut]

Does that also mean that it can not alter the menstrual cycle if taken at the wrong time of month like progesterone does?

I can't legally make statements on this topic, but AFAIK the clinical trial with Brexanolone did not report issues with the menstrual cycle.

 

[Makrosky]

Can't talk about risks/safety. That is against FDA rules. All I can say is that studies so far do not demonstrate suppression of endogenous synthesis of other steroids of neurotransmitters. There are no reports of hormonal effects either. Unlike progesterone, 5a-DHP, etc allopregnanolone seems to be similar to pregnenolone - i.e. mostly a neurosteroid, devoid of "classical" hormonal effects through receptors such as PR, ER, AR, GR, etc.

Thanks haidut. Totally understand the FDA thing. From wikipedia :
"
Unlike progesterone, allopregnanolone is inactive at the classical nuclear progesterone receptor (PR).[35] However, allopregnanolone can be intracellularly oxidized into 5α-dihydroprogesterone, which does act as an agonist of the PR, and for this reason, allopregnanolone can produce PR-mediated progestogenic effects."

So it seems indirectly it can have progestogenic effects.

 

[Dr. B]

I can't legally make statements on this topic, but AFAIK the clinical trial with Brexanolone did not report issues with the menstrual cycle.

is brexanolone just a patented form or what is the exact ingredients in brexanolone besides allopregnanolone? if you google brexanolone a wikipedia page for allopregnenolone comes up

 

[Dr. B]

I can't legally make statements on this topic, but AFAIK the clinical trial with Brexanolone did not report issues with the menstrual cycle.

Mate does this not apply for things for lab usage. seems very restricted "In the United States, brexanolone is a Schedule IV controlled substance.[7][6] Allopregnanolone is available only through a restricted program called the Zulresso REMS Program that requires the drug to be administered by a healthcare provider in a certified healthcare facility. The REMS requires that patients be enrolled in the program prior to administration of the drug"

also "Exogenous progesterone, such as oral progesterone, elevates allopregnanolone levels in the body with good dose-to-serum level correlations.[57] Due to this, it has been suggested that oral progesterone could be described as a prodrug of sorts for allopregnanolone"

 

[haidut]

Mate does this not apply for things for lab usage. seems very restricted "In the United States, brexanolone is a Schedule IV controlled substance.[7][6] Allopregnanolone is available only through a restricted program called the Zulresso REMS Program that requires the drug to be administered by a healthcare provider in a certified healthcare facility. The REMS requires that patients be enrolled in the program prior to administration of the drug"

also "Exogenous progesterone, such as oral progesterone, elevates allopregnanolone levels in the body with good dose-to-serum level correlations.[57] Due to this, it has been suggested that oral progesterone could be described as a prodrug of sorts for allopregnanolone"

You can buy allopregnanolone openly, without restrictions, from many chemical companies in the US. See below for some links. We are selling it exactly as they are - as a lab product.

5α-Pregnan-3α-ol-20-one solid | Sigma-Aldrich

5α-Pregnan-3α-ol-20-one solid; CAS Number: 516-54-1; Synonyms: Allopregnanolone,3α-OH-DHP,Allopregnan-3α-ol-20-one,Brexanolone,3α-Hydroxy-5α-pregnan-20-one; find Sigma-Aldrich-P8887 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich

www.sigmaaldrich.com

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Allopreganolone supplier | CAS 516-54-1 | Focus Biomolecules

Allopregnanolone (516-54-1) is an endogenous neurosteroid which acts as a positive allosteric modulator of GABAA receptors.

focusbiomolecules.com

BioVision is now part of Abcam | Abcam

We’ve taken steps to ensure you can easily find your BioVision products on our catalog for a seamless transition and minimal interruption to your research.

www.biovision.com

 

[Risingfire]

Have you noticed any weight loss from this, @haidut ?

 

[haidut]

is brexanolone just a patented form or what is the exact ingredients in brexanolone besides allopregnanolone? if you google brexanolone a wikipedia page for allopregnenolone comes up

Brexanolone is just another name for allopregnanolone. As such, it cannot be patented directly, but the entire formulation - the steroid, adjuvants, solvents, IV bag, etc - that is administered to patients can be patented and has been patented under the trade name Zulresso.

Treat Postpartum Depression | ZULRESSO® (brexanolone) CIV

Learn about ZULRESSO®, an FDA-approved treatment for PPD in adults. See full Prescribing Information, Boxed Warning, and Important Safety Info.

www.zulresso.com

 

[Mauritio]

A $34,000 Drug for Postpartum Depression Brings Praise, Price Concerns

The most common complication of postpartum can last for weeks to months. A powerful but pricey new drug could offer quick treatment for affected mothers.

labblog.uofmhealth.org

Brexanolone is just another name for allopregnanolone. As such, it cannot be patented directly, but the entire formulation - the steroid, adjuvants, solvents, IV bag, etc - that is administered to patients can be patented and has been patented under the trade name Zulresso.

Treat Postpartum Depression | ZULRESSO® (brexanolone) CIV

Learn about ZULRESSO®, an FDA-approved treatment for PPD in adults. See full Prescribing Information, Boxed Warning, and Important Safety Info.

www.zulresso.com

Big pharma = 34 000$
Idealabs = 29,99$
??