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What are SERMS?

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2 years ago #1
Administrator Posts: 1004  Reviews: 46  Threads: 88 

SERMs (Selective Estrogen Receptor Modulators) - Block estrogen from acting on tissue.

Nolvadex (tamoxifen citrate)
10mg tablets = 15.2mg of tamoxifen citrate which is equivalent to 10mg of tamoxifen.
20mg tablets = 30.4mg of tamoxifen citrate which is equivalent to 20mg of tamoxifen.

Raloxifene: Raloxifene is a selective estrogen receptor modulator that produces both estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

Clomiphene Citrate (Clomid, Clomifen, Serophene): Clomid is capable of reacting with all of the tissues in the body that have estrogen receptors. It influences the way that the four hormones GnRH, FSH, LH and estradiol, relate and interrelate. It appears that Clomid fools the body into believing that the estrogen level is low. This altered feedback information causes the hypothalamus to make and release more gonadotropin releasing hormone (GnRH) which in turn causes the pituitary to make and release more FSH and LH. More follicle stimulating hormone and more luteinizing hormone should result in increased testosterone production. Like Nolvadex, Clomid is not a steroid but a triphenylethylene with anti-oestrogenic properties. The two compounds are structurally similar and their mechanism of action is also similar. The general consensus though, is that Clomid is best left as a post-cycle natural testosterone recovery product and a more appropriate anti-oestrogen found, as Clomid does not seem to be as effective in this role.

Droloxifine (experimental)

Idoxifene (experimental)

Toremifene Citrate (experimental): Less toxic than tamoxifen citrate and better on lipids and bone density. Discussions: 1 2

AIs (Aromatase Inhibitors): Aromatase is the enzyme that causes the conversion of testosterone into estradiol and androstenedione into estrone. Aromatase inhibitors lower the amount of estrogen in post-menopausal women who have hormone-receptor-positive breast cancer. The hormone estrogen delivers growth signals to the hormone receptors. With less estrogen in the body, the hormone receptors receive fewer growth signals, and cancer growth can be slowed down or stopped.

6-OXO (chemical name: 3,6,17-androstenetrione): A suicide inhibitor of aromatase. Binds to the aromatase enzyme in a permanent and irreversible manner, rendering it inactive. The result of this is an eventual diminishment of aromatase enzyme in the body and a concomitant reduction in estrogen levels. A corresponding increase in testosterone production is usually experienced as well.

Arimidex (chemical name: anastrozole): Type 2 "non-steroidal inhibitors." They also stop the activity of the aromatase enzyme, but not permanently. Arimidex is the perfect choice for when using high doses of aromatising steroids, or indeed even for moderate doses if the individual is prone to gyno. It is thought that it may be possible to lower oestrogen levels too much with Arimidex and for this reason blood tests are recommended to determine whether the dosing schedule is correct for maximum results, as it is theorised that some oestrogen presence is required to keep the androgen receptors 'open'. Arimidex has excellent binding qualities at the receptor and therefore only low doses are required. The main downside is its price; it's very expensive. Dosing: Arimidex is supplied in 1mg tablets. Usual dose is between 0.25 - 1mg per day. In most cases 0.5mg per day is sufficient.

Letrozole (Femara): An oral, anti-estrogen drug used for treating postmenopausal women with breast cancer. Letrozole prohibits the enzyme in the adrenal glands (aromatase) that produces the estrogens, estradiol and estrone. Can be taken with or without food.

Aromasin (chemical name: exemestane): Type 1 "steroidal inhibitor," which stops the activity of the aromatase enzyme forever.

Chrysin: Chrysin is a flavonoid that has been purported especially in the bodybuilding world

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2 years ago #2
Contributing Member
Contributing Member Posts: 358  Reviews: 1  Threads: 18 

Discussion on running SERM inverse to ATD

Estrogen only "rebounds" based on the mechanism of suppression. SERM, for example, only masks estrogen expression by occupying receptors but estrogen production is left unchecked and actually increases as testosterone levels increase. AI's like letro inhibit inducible enzymes and just like a leaky faucet, they body will eventually try to balance the equation with increased aromatase activity. Steroidal AI's like Teslac, Exemestane, and ReboundXT will not result in 'rebound' phenomena because the inhibition is non-competitive and irreversible. They act as false substrates, so aromatase is still happy to act on them (instead of androstenedione) and the body keeps no record of an imbalance. There is no leaky faucet. In fact, after prolonged use, steroidal AI's often produce a protracted anti-e benefit even after being discontinued. This is why I suggest an inverse taper with SERM and RXT for PCT with an abrupt stoppage of RXT at the end. As the SERM elevates androgen/estrogen production, the AI dose is increased to compensate while the SERM is phased out. It works quite well to use this approach and rebound is not encountered. Adding LX and/or DHEA also really makes for a killer PCT in this scheme. This is a typical example of my PCT:

wk1: Clomid 150mg/d, RXT 25mg/d, DHEA 200mg/d, LX 75mg/d
wk2: Clomid 100mg/d, RXT 25mg/d, DHEA 200mg/d, LX 50mg/d
wk3: Nolva 60mg/d, RXT 50mg/d, DHEA 200mg/d, LX 25mg/d
wk4: Nolva 40mg/d, RXT 50mg/d, DHEA 100mg/d
wk5: Nolva 20mg/d, RXT 75mg/d, DHEA 100mg/d
wk6: RXT 75mg/d, DHEA 100mg/d

Notice I phase the Clomid out and introduce the Nolva later. This helps prevent sides from developing from accumulation of estrogenic metabolites from the Clomid and also acts to minimize the use of Nolva, which is more liver toxic than Clomid. Rebound is very unlikely and estrogen biosynthesis will likely be significantly lowered for 3+ wks even after the end of this PCT. I do long ones, as you can see.

The list below determines when you should start Clomid. Select from the list any steroids you've used in your cycle and whichever one has the latest starting point is the time to commence Clomid. For example, if Dianabol, Sustanon and Winstrol were cycled, the time for administering Clomid should be 3 weeks post cycle, as Sustanon remains active in the body for the longest period of time. Read the discussion here.

Time after last administration Length of clomid cycle
Anadrol50/Anapolan50 8 - 12 hours 3 weeks
Deca durabolan 3 weeks 4 weeks
Dianabol 4 - 8 hours 3 weeks
Equipoise 17 - 21 days 3 weeks
Finajet/Trenbolone 3 days 3 weeks
Primabolan depot 10 - 14 days 2 weeks
Sustanon 3 weeks 3 weeks
Testosterone Cypionate 2 weeks 3 weeks
Testosterone Enanthate/Testaviron 2 weeks 3 weeks
Testosterone Propionate 3 days 3 weeks
Testosterone Suspension 4 - 8 hours 2-3 weeks
Winstrol 8 - 12 hours 2-3 weeks

Other products to help increase natural testosterone or aid workouts during PCT:

Tribulus, Fenugreek, Forskolin, DHEA, Rebound XT, Rebound Reloaded, Reduce XT, ActivaTe, Anabolic Xtreme PCT, Retain (reduce cortisol), Lean Extreme (reduce cortisol), CEE (Creatine Ethyl Ester). Nitric Oxide (NO2), Ultra H.O.T., Ultra HOTTER

ActivaTe - Should be used starting the last wk or 2 wks of a cycle and continued for no longer than 8 total weeks into PCT. 6 weeks seems perfect to me. The first and last week of dosing should consist of a half dose, and the weeks in between full doses. It's okay to take more than the full dose too because it's effects are non-toxic and dose dependent.

Products to help with blood pressure and cholesterol regulation / liver and support:

Liver: K-R-ALA, NAC ( N-Acetyl-Cysteine), Milk Thistle (80% standardized Silymarin), Lecithin

Cholesterol: Sesathin, Guggul, Red Yeast Rice*, CoEnzyme Q10*, Flax Seed Oil, Safflower Oil*, Policosanol*, Niacin, Garlic, Hawthorn Ber

2 years ago #3
Junior Member
Junior Member Posts: 35  Reviews: 0  Threads: 8 

excellent info, thanks to both of u

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