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EIDD-1723
EIDD-1723, also known as EPRX-01723 or as progesterone 20''E''-[''O''-[(phosphonooxy)methyl]oxime] sodium salt, is a synthetic compound, synthetic, water-soluble structural analog, analogue of progesterone (medication), progesterone and a neurosteroid which was developed for the potential treatment of traumatic brain injury.Guthrie, D. B., Lockwood, M. A., Natchus, M. G., Liotta, D. C., Stein, D. G., & Sayeed, I. (2017). U.S. Patent No. 9,802,978. Washington, DC: U.S. Patent and Trademark Office. https://patents.google.com/patent/US9802978B2/en It is a rapidly converted prodrug of EIDD-036 (EPRX-036; progesterone 20-oxime), which is considered to be the active form of the agent. Previous C3 and C20 oxime derivatives of progesterone, such as P1-185 (progesterone 3-''O''-(-valine)-''E''-oxime), were also developed and studied prior to EIDD-1723. See also * List of neurosteroids#Pregnanes 2, List of neurosteroids § Inhibitory > Synthetic > Pregnanes * List of progestogen esters#Oxim ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Neurosteroids
This is a list of neurosteroids, or natural and synthetic steroids that are active on the mammalian nervous system through receptors other than steroid hormone receptors. It includes inhibitory, excitatory, and neurotrophic neurosteroids as well as pheromones and vomeropherines. In contrast to steroid hormones, neurosteroids have rapid, non- genomic effects through interactions with membrane steroid receptors and can quickly influence central nervous system function. Inhibitory Natural Cholestanes * 25-Hydroxycholesterol: cholest-5-en-3β,25-diol – NMDA receptor negative allosteric modulator Androstanes * 3α,5α-Androstanediol (3α-androstanediol): 5α-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator * 3α,5β-Androstanediol (etiocholanediol): 5β-androstane-3α,17β-diol – GABAA receptor positive allosteric modulator * 3α-Androstenol: 5α-androst-16-en-3α-ol – GABAA receptor positive allosteric modulator * Androsterone: 5α-androsta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Progestogen Esters
This is a list of progestogen esters, or esters of progestogens.http://www.micromedexsolutions.com Unlike the case of testosterone and estradiol, progesterone cannot be esterified as it lacks hydroxyl groups, so all progestogen esters, with the exception of esters of 17α-hydroxyprogesterone like hydroxyprogesterone caproate, are esters of progestins ( synthetic progestogens) and are non-bioidentical. In addition, whereas all androgen and estrogen esters are prodrugs of the parent compound, only some and not all progestogen esters act as prodrugs. Esters of 17α-hydroxyprogesterone and 19-norprogesterone derivatives like hydroxyprogesterone caproate, medroxyprogesterone acetate, and nomegestrol acetate are active themselves and ''are not'' prodrugs, whereas esters of 19-nortestosterone derivatives like norethisterone acetate and norethisterone enanthate are not active themselves and ''are'' prodrugs. Esters of progesterone derivatives Esters of 17α-hydroxyprogesterone deri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progesterone (medication)
Progesterone (P4) is a medication and naturally occurring steroid hormone. It is a progestogen and is used in combination with estrogens mainly in hormone therapy for menopausal symptoms and low sex hormone levels in women. It is also used in women to support pregnancy and fertility and to treat gynecological disorders. Progesterone can be taken by mouth, in through the vagina, and by injection into muscle or fat, among other routes. A progesterone vaginal ring and progesterone intrauterine device used for birth control also exist in some areas of the world. Progesterone is well tolerated and often produces few or no side effects. However, a number of side effects are possible, for instance mood changes. If progesterone is taken by mouth or at high doses, certain central side effects including sedation, sleepiness, and cognitive impairment can also occur. The medication is a naturally occurring progestogen and hence is an agonist of the progesterone receptor (PR), t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EIDD-036
EIDD-036, also known as EPRX-036, as well as progesterone 20-oxime (P4-20-O) or 20-(hydroxyimino)pregn-4-en-3-one, is a synthetic, water-soluble analogue of progesterone, a neurosteroid, and the active metabolite An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body ... of EIDD-1723 (EPRX-01723), a medication developed for the potential treatment of traumatic brain injury.Guthrie, D. B., Lockwood, M. A., Natchus, M. G., Liotta, D. C., Stein, D. G., & Sayeed, I. (2017). U.S. Patent No. 9,802,978. Washington, DC: U.S. Patent and Trademark Office. https://patents.google.com/patent/US9802978B2/en See also * List of neurosteroids § Inhibitory > Synthetic > Pregnanes * List of progestogen esters § Oximes of progesterone derivatives References Experimental drugs Human drug metaboli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
P1-185
P1-185, also known as progesterone 3-''O''-(L-valine)-''E''-oxime or as pregn-4-ene-3,20-dione 3-''O''-(L-valine)-''E''-oxime, is a synthetic progestogen and neurosteroid and an oxime ester analogue and prodrug of progesterone (and by extension of allopregnanolone). It was developed as an improved water-soluble version of progesterone such that it could be formulated as an aqueous preparation and easily and rapidly administered intravenously as a potential therapy for traumatic brain injury. However, the chemical synthesis of P1-185 was described as somewhat challenging, so oxime conjugates of progesterone of the C20 instead of C3 position, such as EIDD-1723 EIDD-1723, also known as EPRX-01723 or as progesterone 20''E''- phosphonooxy)methyl.html"_;"title="'O''- 'O''-[(phosphonooxy)methylximesodium_salt,_is_a_synthetic_compound.html"__"title="phosphonooxy)methylxime.html"_;"title_..._and_ 'O''-[(phosphonooxy)methylximesodium_salt,_is_a_synthetic_compound.html"__"title="p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pregnanes
Pregnane, also known as 17β-ethylandrostane or as 10β,13β-dimethyl-17β-ethylgonane, is a C21 steroid and, indirectly, a parent of progesterone. It is a parent hydrocarbon for two series of steroids stemming from 5α-pregnane (originally allopregnane) and 5β-pregnane (17β-ethyletiocholane). It has a gonane core. 5β-Pregnane is the parent of pregnanediones, pregnanolones, and pregnanediols, and is found largely in urine as a metabolic product of 5β-pregnane compounds. Pregnanes Pregnanes are steroid derivatives with carbons present at positions 1 through 21. Most biologically significant pregnane derivatives fall into one of two groups: pregnenes and pregnadienes. Another class is pregnatrienes. Pregnenes Pregnenes have a double bond. Examples include: * Cortisone * Hydrocortisone * Progesterone Pregnadienes Pregnadienes have two double bonds. Examples include: * Cyproterone acetate * Danazol * Fluocinonide See also * 5β-Pregnane * Pregnanedione * Pregna ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phosphate Esters
In chemistry, a phosphate is an anion, salt, functional group or ester derived from a phosphoric acid. It most commonly means orthophosphate, a derivative of orthophosphoric acid . The phosphate or orthophosphate ion is derived from phosphoric acid by the removal of three protons . Removal of one or two protons gives the dihydrogen phosphate ion and the hydrogen phosphate ion ion, respectively. These names are also used for salts of those anions, such as ammonium dihydrogen phosphate and trisodium phosphate. File:3-phosphoric-acid-3D-balls.png, Phosphoricacid File:2-dihydrogenphosphate-3D-balls.png, Dihydrogenphosphate File:1-hydrogenphosphate-3D-balls.png, Hydrogenphosphate File:0-phosphate-3D-balls.png, Phosphate In organic chemistry, phosphate or orthophosphate is an organophosphate, an ester of orthophosphoric acid of the form where one or more hydrogen atoms are replaced by organic groups. An example is trimethyl phosphate, . The term also refers to the trival ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organic Sodium Salts
Organic may refer to: * Organic, of or relating to an organism, a living entity * Organic, of or relating to an anatomical organ Chemistry * Organic matter, matter that has come from a once-living organism, is capable of decay or is the product of decay, or is composed of organic compounds * Organic compound, a compound that contains carbon ** Organic chemistry, chemistry involving organic compounds Farming, certification and products * Organic farming, agriculture conducted according to certain standards, especially the use of stated methods of fertilization and pest control * Organic certification, accreditation process for producers of organically-farmed products * Organic horticulture, the science and art of growing fruits, vegetables, flowers, or ornamental plants by following the essential principles of organic agriculture * Organic products, "organics": ** Organic food, food produced from organic farming methods and often certified organic according to organic farming stan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurosteroids
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was coined by the French physiologist Étienne-Émile Baulieu and refers to steroids synthesized in the brain. The term, ''neuroactive steroid'' refers to steroids that can be synthesized in the brain, or are synthesized by an endocrine gland, that then reach the brain through the bloodstream and have effects on brain function. The term neuroactive steroids was first coined in 1992 by Steven Paul and Robert Purdy. In addition to their actions on neuronal membrane receptors, some of these steroids may also exert effects on gene expression via nuclear steroid hormone receptors. Neurosteroids have a wide range of potential clinical applications from sedation to treatment of epilepsy and traumatic brain injury. Ganaxolone, a synthetic analog of the end ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuroprotective Agents
Neuroprotection refers to the relative preservation of neuronal structure and/or function. In the case of an ongoing insult (a neurodegenerative insult) the relative preservation of neuronal integrity implies a reduction in the rate of neuronal loss over time, which can be expressed as a differential equation. It is a widely explored treatment option for many central nervous system (CNS) disorders including neurodegenerative diseases, stroke, traumatic brain injury, spinal cord injury, and acute management of neurotoxin consumption (i.e. methamphetamine overdoses). Neuroprotection aims to prevent or slow disease progression and secondary injuries by halting or at least slowing the loss of neurons. Despite differences in symptoms or injuries associated with CNS disorders, many of the mechanisms behind neurodegeneration are the same. Common mechanisms of neuronal injury include decreased delivery of oxygen and glucose to the brain, energy failure, increased levels in oxidative stre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neurosteroid
Neurosteroids, also known as neuroactive steroids, are endogenous or exogenous steroids that rapidly alter neuronal excitability through interaction with ligand-gated ion channels and other cell surface receptors. The term ''neurosteroid'' was coined by the French physiologist Étienne-Émile Baulieu and refers to steroids synthesized in the brain. The term, ''neuroactive steroid'' refers to steroids that can be synthesized in the brain, or are synthesized by an endocrine gland, that then reach the brain through the bloodstream and have effects on brain function. The term neuroactive steroids was first coined in 1992 by Steven Paul and Robert Purdy. In addition to their actions on neuronal membrane receptors, some of these steroids may also exert effects on gene expression via nuclear steroid hormone receptors. Neurosteroids have a wide range of potential clinical applications from sedation to treatment of epilepsy and traumatic brain injury. Ganaxolone, a synthetic analog of the end ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
