Selective Progestin Receptor Modulators

smash1904

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So I was doing some research on tren, it's origins and actions, and read about its progestin receptor binding. So if this binding is what causes those side effects that perhaps there might a drug like serms and sarms that bind to these receptors to keep something else from binding to them. Low and behold there are actually a few:

Ulipristal acetate ("Ella")
Asoprisnil (J867; status uncertain)
CDB-4124 (Proellex, Progenta; under development)

I took deca and it messed me up, ED has been an ongoing problem, but I'm being told tren is pretty much mandatory for bodybuilding. I haven't tried prami, but caber has only kind of worked for me and I'm figuring it won't work much better. So really what I'm wondering is has anyone tried sprms or know if they work? Are they available as research chemicals?
 

00S4Boy

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Sorry to hijack but hahahahaha you said sprms where the female members at to comment?
 
jbryand101b

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So I was doing some research on tren, it's origins and actions, and read about its progestin receptor binding. So if this binding is what causes those side effects that perhaps there might a drug like serms and sarms that bind to these receptors to keep something else from binding to them. Low and behold there are actually a few:

Ulipristal acetate ("Ella")
Asoprisnil (J867; status uncertain)
CDB-4124 (Proellex, Progenta; under development)

I took deca and it messed me up, ED has been an ongoing problem, but I'm being told tren is pretty much mandatory for bodybuilding. I haven't tried prami, but caber has only kind of worked for me and I'm figuring it won't work much better. So really what I'm wondering is has anyone tried sprms or know if they work? Are they available as research chemicals?
You would be better looking for androgens that bind to the progestin receptor without interacting with it, like winstrol
 
smash1904

smash1904

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You would be better looking for androgens that bind to the progestin receptor without interacting with it, like winstrol
Ya I read about that, as well as a debate about whether tren acts as a sprm or not. They were saying that the reason why tren causes gyno is that it upregulates estrogen receptors causing even normal levels to be potentially problematic.
 
TRIGUY

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Ya I read about that, as well as a debate about whether tren acts as a sprm or not. They were saying that the reason why tren causes gyno is that it upregulates estrogen receptors causing even normal levels to be potentially problematic.
Gyno from TREN is from stimulating the progesterone receptor.

progesterone is responsible for tren's deca dick issue


Ulipristal acetate .......this stuff is not good on the liver, can this be made into a transdermal?
 
TRIGUY

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1. Ulipristal acetate or a metabolite thereof may be administered by any convenient route, including oral, buccal, parenteral, transdermal, vaginal, uterine, rectal, etc.
[0028]
For a brief review of present methods for drug delivery, see, Langer, Science 249:1527-1533 (1990), which is incorporated herein by reference. Methods for preparing administrable compounds are known or are apparent to those skilled in the art and are described in more detail in, for example, Remington's Pharmaceutical Science, 17th ed., Mack Publishing Company, Easton, Pa. (1985), which is incorporated herein by reference, and which is hereinafter referred to as "Remington."


2. Transdermal delivery systems comprising a penetration enhancer and an occlusive backing are of use to deliver ulipristal acetate or a metabolite thereof. Examples of penetration enhancers include dimethyl sulfoxide, dimethyl acetamide and dimethylformamide.

3. In calculating the dosage for individuals one has to take into consideration the weight of the individual and the mode of administration. The following guidelines provide levels of ulipristal acetate which are clinically effective.
[0038]
Presuming an average weight of 120 pounds or 53 kilograms, the daily unit dosage of ulipristal acetate is preferably between 5 to 15 mg per day. Surprisingly enough, the reduction of fibroid volume is more important with an oral dose of 10mg, compared to 20mg. An oral dose of 10mg per day is thus most preferred. A lower dosage is also contemplated, e.g. between 1 mg and 10 mg daily, preferably between 5 and 10mg daily. The oral route is preferred. Other routes of administration can be suitable in comparison with oral routes using blood levels to provide clinical success

**solubility DMSO: 5 mg/mL, clear (warmed). .....got this from sigma Aldrich website

In February 2018, the European Medicines Agency released a report concerning reports of serious liver injury associated with long term ulipristal. The EMA have advised monthly liver tests and against further people being started on the medication for uterine fibroids until further review is completed.[24]

https://patents.google.com/patent/EP2684565A1
 
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