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Erteberel
Erteberel (, ; former developmental code name LY-500307; also known as selective estrogen receptor beta agonist-1 or SERBA-1) is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and was under development by Eli Lilly for the treatment of schizophrenia. It was specifically under investigation for the treatment of negative symptoms and cognitive impairment associated with the condition. It managed to reach phase II clinical trials for this indication in the United States in 2015. As of 2021 development has been discontinued. Erteberel was also under investigation for the treatment of benign prostatic hyperplasia and reached phase II clinical studies for this use but failed to improve symptoms in men with the condition and development for this indication was discontinued. The drug has also been proposed as a potential novel treatment for glioblastoma. Erteberel has 14-fold binding selectivity for the ERβ over the ERα (Ki = 0.19 nM versus 2.68&n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective ERβ Agonists
Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) 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. Function ERβ is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene product contains an N-terminal DNA binding domain and C-terminal ligand binding domain and is localized to the nucleus, cytoplasm, and mitochondria. Upon binding to 17-β-estradiol, estriol or related ligands, the encoded protein forms homo-dimers or hetero-dimers with estrogen receptor α that interact with specific DNA sequences to activate transcription. Some isoforms dominantly inhibit the activity of other estrogen receptor family members. Several alternatively spliced transcript variants of this gene have been described, but the full-length nature of some of these variants ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Sex-hormonal Agents
This is a list of investigational sex-hormonal agents, or sex-hormonal agents that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' This list was last comprehensively updated sometime between May 2017 and September 2021. It is likely to become outdated with time. Androgenics Androgen receptor agonists * EC586 – oral prodrug of testosterone (androgen/anabolic steroid) with improved pharmacokinetics Selective androgen receptor modulators * DT-200 (G-100192, GLPG-0492) – selective androgen receptor modulator for Duchenne muscular dystrophybr>* Enobosarm (ostarine; GTx-024, MK-2866; S-22; VERU-024) – selective androgen receptor modulator for breast cancerbr>* GSK2881078, GSK-2881078 – selective androgen receptor modulator for cachexiabr>* OPK-88004 (LY-2452473; OPK-88004; TT-701) – selective androgen receptor modulator fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Functional Selectivity
Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid receptor show equivalent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diols
A diol is a chemical compound containing two hydroxyl groups ( groups). An aliphatic diol may also be called a glycol. This pairing of functional groups is pervasive, and many subcategories have been identified. They are used as protecting groups of carbonyl groups, making them essential in synthesis of organic chemistry. The most common industrial diol is ethylene glycol. Examples of diols in which the hydroxyl functional groups are more widely separated include 1,4-butanediol and propylene-1,3-diol, or beta propylene glycol, . Synthesis of classes of diols Geminal diols A geminal diol has two hydroxyl groups bonded to the same atom. These species arise by hydration of the carbonyl compounds. The hydration is usually unfavorable, but a notable exception is formaldehyde which, in water, exists in equilibrium with methanediol H2C(OH)2. Another example is (F3C)2C(OH)2, the hydrated form of hexafluoroacetone. Many gem-diols undergo further condensation to give dimer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopentanes
Cyclopentane (also called C pentane) is a highly flammable alicyclic hydrocarbon with chemical formula C5H10 and CAS number 287-92-3, consisting of a ring of five carbon atoms each bonded with two hydrogen atoms above and below the plane. It is a colorless liquid with a petrol-like odor. Its freezing point is −94 °C and its boiling point is 49 °C. Cyclopentane is in the class of cycloalkanes, being alkanes that have one or more carbon rings. It is formed by cracking cyclohexane in the presence of alumina at a high temperature and pressure. It was first prepared in 1893 by the German chemist Johannes Wislicenus. Production, occurrence and use Cycloalkanes are formed by catalytic reforming. For example, when passed over a hot platinum surface, 2-methylbutane converts into cyclopentane. Cyclopentane is principally used as a blowing agent in the manufacture of polyurethane insulating foam, replacing ozone-depleting agents such as CFC-11 and HCFC-141b. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzopyrans
4H-1-Benzopyran is an organic compound with the formula . It is one of two isomers of benzopyran, the other being 2H-1-benzopyran, which is more prevalent. It can be viewed as the fusion of a benzene ring to a heterocyclic pyran ring. Some benzopyrans have shown anticancerous activity '' in vitro''. The radical form of benzopyran is paramagnetic. The unpaired electron is delocalized over the whole benzopyran molecule, rendering it less reactive than one would expect otherwise. A similar example is the cyclopentadienyl radical. Commonly, benzopyran is encountered in the reduced state, in which it is partially saturated with one hydrogen atom, introducing a tetrahedral CH2 group in the pyran ring. Therefore, there are many structural isomers owing to the multiple possible positions of the oxygen atom and the tetrahedral carbon atom: Nomenclature According to current IUPAC The International Union of Pure and Applied Chemistry (IUPAC ) is an international federatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay, together with mood stabilizers, in the treatment of bipolar disorder. Moreover, they are also used as adjuncts in the treatment of treatment-resistant major depressive disorder. The use of antipsychotics may result in many unwanted side effects such as involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. Long-term use can produce adverse effects such as tardive dyskinesia, tardive dystonia, tardive akathisia, and brain tissue volume reduction. The long term use of antipsychotics often changes the brain both structurally and chemically in a way that can be difficult or impossible to reverse. This can lead ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Investigational Antipsychotics
This is a list of investigational antipsychotics, or antipsychotics that are currently under development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmental code names, synonyms, and brand names in parentheses.'' This list was last comprehensively updated in December 2017. It is likely to become outdated with time. Receptor modulators Monoamine receptor modulators * Brilaroxazine (RP5063; oxaripiprazole) – atypical antipsychotic (D2/3/4 and 5-HT1A partial agonist and 5-HT2A/2B/7 antagonist) * FKF-02SC (TGOF-02N) – atypical antipsychotic (D2 and 5-HT2A receptor antagonist, other actions) * Masupirdine (SUVN-502) – 5-HT6 receptor antagonist * ''N''-Methylamisulpride (LB-102) – D2,3, 5-HT7, receptor antagonist (methylated version of amisulpride) * Ralmitaront (RG-7906, RO-6889450) – TAAR1 agonist * Ulotaront (SEP-856, SEP-363856) – 5-HT1A receptor and TAAR1 agonist * Usmarapride (SUVN-D4010) – 5-HT4 rec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Testosterone
Testosterone is the primary male sex hormone and androgen in Male, males. In humans, testosterone plays a key role in the development of Male reproductive system, male reproductive tissues such as testicles and prostate, as well as promoting secondary sexual characteristics such as increased muscle and bone mass, and the growth of androgenic hair, body hair. It is associated with increased aggression, sex drive, Dominance hierarchy, dominance, courtship display, and a wide range of behavioral characteristics. In addition, testosterone in both sexes is involved in health and well-being, where it has a significant effect on overall mood, cognition, social and sexual behavior, metabolism and energy output, the cardiovascular system, and in the prevention of osteoporosis. Insufficient levels of testosterone in men may lead to abnormalities including frailty, accumulation of adipose fat tissue within the body, anxiety and depression, sexual performance issues, and bone loss. Excessiv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
