👼 Set your curiosity free with rich, wide-ranging, hyper-connected information.

16α-LE2

Chemical compound

Top 10 16α-LE2 related articles
1 Organic compound
In chemistry, organic compounds are generally any chemical compounds that contain carbon-hydrogen bonds. Due to carbon's ability to catenate, millions of organic compounds are known. The study of the properties, reactions, and syntheses of organic compounds comprises the discipline known as organic chemistry. For historical reasons, a few classes of carbon-containing compounds, along with a handful of other exceptions, are not classified as organic compounds and are considered inorganic. Other than those just named, little consensus exists among chemists on precisely which carbon-containing compounds are excluded, making any rigorous definition of an organic compound elusive.More
2 Steroid
A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes which alter membrane fluidity; and as signaling molecules. Hundreds of steroids are found in plants, animals and fungi. All steroids are manufactured in cells from the sterols lanosterol (opisthokonts) or cycloartenol (plants). Lanosterol and cycloartenol are derived from the cyclization of the triterpene squalene.More
3 Estrogen
Estrogen, or oestrogen, is a category of sex hormone responsible for the development and regulation of the female reproductive system and secondary sex characteristics. There are three major endogenous estrogens that have estrogenic hormonal activity: estrone (E1), estradiol (E2), and estriol (E3). Estradiol, an estrane, is the most potent and prevalent. Another estrogen called estetrol (E4) is produced only during pregnancy.More
4 Estradiol
Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of the estrous and menstrual female reproductive cycles. Estradiol is responsible for the development of female secondary sexual characteristics such as the breasts, widening of the hips, and a female-associated pattern of fat distribution and is important in the development and maintenance of female reproductive tissues such as the mammary glands, uterus, and vagina during puberty, adulthood, and pregnancy. It also has important effects in many other tissues including bone, fat, skin, liver, and the brain. Though estradiol levels in males are much lower than in females, estradiol has important roles in males as well. Apart from humans and other mammals, estradiol is also found in most vertebrates and crustaceans, insects, fish, and other animal species.More
5 Agonist
An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist.More
6 Estrogen receptor alpha
Estrogen receptor alpha (ERα), also known as NR3A1, is one of two main types of estrogen receptor, a nuclear receptor that is activated by the sex hormone estrogen. In humans, ERα is encoded by the gene ESR1.More
7 Scientific method
The scientific method is an empirical method of acquiring knowledge that has characterized the development of science since at least the 17th century. It involves careful observation, applying rigorous skepticism about what is observed, given that cognitive assumptions can distort how one interprets the observation. It involves formulating hypotheses, via induction, based on such observations; experimental and measurement-based testing of deductions drawn from the hypotheses; and refinement of the hypotheses based on the experimental findings. These are principles of the scientific method, as distinguished from a definitive series of steps applicable to all scientific enterprises.More
8 Potency (pharmacology)
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug evokes a given response at low concentrations, while a drug of lower potency evokes the same response only at higher concentrations. Higher potency does not necessarily mean more side effects.More
9 Transactivation
In the context of gene regulation: transactivation is the increased rate of gene expression triggered either by biological processes or by artificial means, through the expression of an intermediate transactivator protein.More
10 Bioassay
A bioassay is an analytical method to determine concentration or potency of a substance by its effect on living cells or tissues. Bioassays are quantitative biological assays used to estimate the potency of agents by observing their effects on living animals or tissue/cell culture systems.More
16α-LE2
Identifiers
CAS Number
ChemSpider
Chemical and physical data
FormulaC20H24O4
Molar mass328.408 g·mol−1
3D model (JSmol)

16α-LE2, or 16α-lactone-estradiol, also known as 3,17β-dihydroxy-19-nor-17α-pregna-1,3,5-(10)-triene-21,16α-lactone, is a synthetic, steroidal estrogen featuring an estradiol core. It is a highly potent and selective agonist of the ERα that is used in scientific research to study the function of the ERα.[1][2] It has 265-fold higher potency in transactivation assays of the ERα relative to the ERβ and 70-fold preference in binding affinity for the ERα over the ERβ.[2]

In rodents, 16α-LE2 has no effect on ovarian follicle development, whereas the highly ERβ-selective agonist 8β-VE2 stimulates follicular growth and to a comparable extent as estradiol, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles.[2][3] In contrast, 16α-LE2 stimulates uterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the uterus.[2] Research has determined through experimental rodent studies with estradiol, 16α-LE2, and 8β-VE2 that the positive, protective effects of estrogens on bone formation resorption and bone mineral density are mediated via the ERα, whereas the ERβ does not appear to be involved.[4]

16α-LE2 Intro articles: 9
1 Estrogen receptor beta
Estrogen receptor beta (ERβ) also known as NR3A2 is one of two main types of estrogen receptor—a nuclear receptor which is activated by the sex hormone estrogen. In humans ERβ is encoded by the ESR2 gene.More
2 Ligand (biochemistry)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. The instance of binding occurs over an infinitesimal range of time and space, so the rate constant is usually a very small number.More
3 Ovarian follicle
An ovarian follicle is a roughly spheroid cellular aggregation set found in the ovaries. It secretes hormones that influence stages of the menstrual cycle. Women begin puberty with about 400,000 follicles, each with the potential to release an egg cell (ovum) at ovulation for fertilization. These eggs are developed once every menstrual cycle.More
4 8β-VE2
8β-VE2, or 8β-vinylestradiol, also known as 8β-vinylestra-1,3,5(10)-triene-3β,17β-diol, is a synthetic estrogen featuring an estradiol core. It is a highly potent and selective agonist of the ERβ that is used in scientific research to study the function of the ERβ. It has 190-fold higher potency in transactivation assays of the ERβ relative to the ERα and 93- (rat) and 180-fold (human) preference in binding affinity for the ERβ over the ERα.More
5 Uterus
The uterus or womb is a major female hormone-responsive secondary sex organ of the reproductive system in humans and most other mammals.it has the shape of a Hyperbolic triangle in humans when not carrying. In the human, the lower end of the uterus, the cervix, opens into the vagina, while the upper end, the fundus, is connected to the fallopian tubes. It is within the uterus that the fetus develops during gestation. In the human embryo, the uterus develops from the paramesonephric ducts which fuse into the single organ known as a simplex uterus. The uterus has different forms in many other animals and in some it exists as two separate uteri known as a duplex uterus.More
6 Animal testing on rodents
Rodents are commonly used in animal testing, particularly mice and rats, but also guinea pigs, hamsters, gerbils and others. Mice are the most commonly used vertebrate species, due to their availability, size, low cost, ease of handling, and fast reproduction rate.More
7 Ossification
Ossification in bone remodeling is the process of laying down new bone material by cells called osteoblasts. It is synonymous with bone tissue formation. There are two processes resulting in the formation of normal, healthy bone tissue: Intramembranous ossification is the direct laying down of bone into the primitive connective tissue (mesenchyme), while endochondral ossification involves cartilage as a precursor. In fracture healing, endochondral osteogenesis is the most commonly occurring process, for example in fractures of long bones treated by plaster of Paris, whereas fractures treated by open reduction and internal fixation with metal plates, screws, pins, rods and nails may heal by intramembranous osteogenesis.More
8 Bone resorption
Bone resorption is resorption of bone tissue, that is, the process by which osteoclasts break down the tissue in bones and release the minerals, resulting in a transfer of calcium from bone tissue to the blood.More
9 Bone density
Bone density, or bone mineral density (BMD), is the amount of bone mineral in bone tissue. The concept is of mass of mineral per volume of bone, although clinically it is measured by proxy according to optical density per square centimetre of bone surface upon imaging. Bone density measurement is used in clinical medicine as an indirect indicator of osteoporosis and fracture risk. It is measured by a procedure called densitometry, often performed in the radiology or nuclear medicine departments of hospitals or clinics. The measurement is painless and non-invasive and involves low radiation exposure. Measurements are most commonly made over the lumbar spine and over the upper part of the hip. The forearm may be scanned if the hip and lumbar spine are not accessible.More

See also

References

  1. ^ I Shaw (31 March 2009). Endocrine-Disrupting Chemicals in Food. Elsevier. pp. 550–. ISBN 978-1-84569-574-3.
  2. ^ a b c d Hegele-Hartung C, Siebel P, Peters O, Kosemund D, Müller G, Hillisch A, Walter A, Kraetzschmar J, Fritzemeier KH (2004). "Impact of isotype-selective estrogen receptor agonists on ovarian function". Proc. Natl. Acad. Sci. U.S.A. 101 (14): 5129–34. doi:10.1073/pnas.0306720101. PMC 387385. PMID 15037755.
  3. ^ Tony M. Plant; Anthony J. Zeleznik (15 November 2014). Knobil and Neill's Physiology of Reproduction. Academic Press. pp. 1150–. ISBN 978-0-12-397769-4.
  4. ^ Hertrampf T, Schleipen B, Velders M, Laudenbach U, Fritzemeier KH, Diel P (2008). "Estrogen receptor subtype-specific effects on markers of bone homeostasis". Mol. Cell. Endocrinol. 291 (1–2): 104–8. doi:10.1016/j.mce.2008.03.003. PMID 18433985. S2CID 1774519.


  • Share this