estrogen receptors: nootropics and compounds | sci-wiki

Clomifene Citrate

Clomifene citrate is a nonsteroidal selective estrogen receptor modulator marketed since the late 1960s under names such as Clomid and Serophene, and it remains a widely used oral agent for inducing ovulation in anovulatory women, including many with polycystic ovary syndrome. It acts principally at the hypothalamus, where blocking estrogen negative feedback increases pulsatile gonadotropin-releasing hormone and pituitary output of LH and FSH, thereby stimulating follicular development. The marketed drug is a mixture of two isomers with opposing properties; the estrogenic zuclomiphene clears slowly and can accumulate across cycles, whereas the antiestrogenic enclomiphene drives most of the ovulation-inducing effect. In the head-to-head PPCOS II trial the aromatase inhibitor letrozole produced higher live-birth rates than clomifene in PCOS, refining its place in fertility therapy. It is also used off-label in men to raise endogenous testosterone and during recovery after anabolic steroid use, and it appears on the World Health Organization list of essential medicines.

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Hormone

Conjugated Estrogens

Conjugated estrogens, best known by the brand name Premarin, are a medication made from a mixture of estrogen hormones extracted from the urine of pregnant mares [1][2]. They are used mainly as menopausal hormone therapy, to relieve hot flashes and vaginal dryness and to help prevent osteoporosis, and also to treat other conditions of low estrogen [1][2]. Introduced in the 1940s, they act on estrogen receptors throughout the body; landmark trials later clarified that, like other hormone therapies, they carry risks including blood clots, stroke and, in combination with a progestogen, breast cancer [1][3].

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Blend

Cyproterone Acetate + Ethinylestradiol

Cyproterone acetate / ethinylestradiol is a combination medication that pairs cyproterone acetate, a progestin with strong antiandrogen activity, with ethinylestradiol, a synthetic estrogen. Sold under brand names such as Diane-35 and Dianette, it is used mainly to treat androgen-related skin conditions in women, including moderate to severe acne, seborrhea, and excess hair growth (hirsutism), while also acting as a hormonal contraceptive. Because it carries a higher risk of blood clots than some other combined pills, its use is generally reserved for these specific indications rather than contraception alone.

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Hormone

Estradiol

Estradiol, often abbreviated E2, is a steroid hormone and the most potent of the naturally occurring estrogens, the principal group of female sex hormones. Produced chiefly by the ovaries, it governs the development of female secondary sexual characteristics and the menstrual cycle, and it also plays important roles in bone, brain, and cardiovascular health in both sexes. As a medicine it is used in menopausal hormone therapy, hormonal contraception, feminizing hormone therapy for transgender women, and the treatment of certain hormone deficiencies. It is available in many forms, including tablets, patches, gels, and injections.

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Hormone

Estradiol Valerate

Estradiol valerate is an estrogen medication and an ester prodrug of estradiol, the main natural estrogen. Once in the body it is split by enzymes into estradiol and valeric acid, so its effects are essentially those of estradiol itself. It is used in menopausal hormone therapy, as part of some hormonal contraceptives, in feminizing hormone therapy for transgender women, and, historically, in the palliative treatment of prostate cancer. It is taken by mouth as a tablet or given as a long-acting oil injection into muscle.

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SERM

Raloxifene

Raloxifene is a benzothiophene selective estrogen receptor modulator (SERM) that binds both estrogen receptor subtypes with high affinity yet behaves as an agonist in some tissues and an antagonist in others. The molecular basis for this tissue selectivity is elegant: the bound ligand imposes a distinct conformation on the receptor that governs which coactivator or corepressor proteins are recruited at a given gene promoter, so the same drug preserves bone density and improves the lipid profile while blocking estrogen's proliferative signal in breast and endometrial tissue. Clinically it is used to prevent and treat postmenopausal osteoporosis and to lower the risk of invasive breast cancer in higher-risk women, a dual profile supported by the MORE, CORE, RUTH, and STAR trials. Because it does not stimulate the uterus, raloxifene carries a more favorable endometrial safety profile than tamoxifen, though it shares an increased risk of venous thromboembolism.

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