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Elinzanetant
Elinzanetant (developmental code names BAY-3427080 GSK-1144814, NT-814) is an orally active small-molecule neurokinin/tachykinin NK1 receptor and NK3 receptor antagonist which is under development by Bayer, GlaxoSmithKline, and NeRRe Therapeutics for the treatment of hot flashes and "sex hormone disorders". It has been found to relieve hot flashes in postmenopausal women and to dose-dependently suppress luteinizing hormone, estradiol, and progesterone levels in premenopausal women. As of August 2021, elinzanetant is in phase 2 clinical trials for hot flashes and "sex hormone disorders". It was also under development for the treatment of schizophrenia Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdra ... and opioid-related disorders, but development was discontinued for these uses. ...
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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.'' Androgenics Androgen receptor agonists * EC586 – oral administration, oral prodrug of testosterone (medication), testosterone (androgen/anabolic steroid) with improved pharmacokinetics Androgen receptor antagonists * Bavdegalutamide (AVR-110) – androgen receptor antagonist for prostate cancerref name="pmid33160761">
* Clascoterone (CB-03-01, Breezula, Winlevi) – androgen receptor antagonist for topical medication, topical treatment of scalp hair loss]

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NK3 Receptor
Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the ''TACR3'' gene. Function This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B. Selective ligands A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications. Agonists * Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK3 * Senktide – 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6 Antagonists * Elinzanetant (BAY-3427080 GSK-1144814, NT-814) * Fezolinetant (ESN-364) * Osanetant (SR-1 ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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Phases Of Clinical Research
The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases start with testing for safety in a few human subjects, then expand to many study participants (potentially tens of thousands) to determine if the treatment is effective. Clinical research is conducted on drug candidates, vaccine candidates, new medical devices, and new diagnostic assays. Summary Clinical trials testing potential medical products are commonly classified into four phases. The drug development process will normally proceed through all four phases over many years. If the drug successfully passes through Phases I, II, and III, it will usually be approved by the national regulatory authority for use in the general population. Phase IV trials are 'post-marketing' or 'surveillance' studies conducted to monitor safety over sever ...
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Pyrazines
Pyrazine is a heterocyclic aromatic organic compound with the chemical formula C4H4N2. It is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. It is a ''"deliquescent crystal or wax-like solid with a pungent, sweet, corn-like, nutty odour"''. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes. Synthesis Many methods exist for the organic synthesis of pyrazine and its derivatives. Some of these are among the oldest synthesis reactions still in use. In the Staedel–Rugheimer pyrazine synthesis (1876), 2-chloroacetophenone is reacted with ammonia to the amino ketone, then condensed and then oxidized to a pyrazine. A variation is the Gutknecht pyrazine synthesis (1879) also based on this selfcondensation, but differ ...
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Oxazines
Oxazines are heterocyclic compounds containing one oxygen and one nitrogen atom in a doubly unsaturated six-membered ring. Isomers exist depending on the relative position of the heteroatoms and relative position of the double bonds. By extension, the derivatives are also referred to as oxazines; examples include ifosfamide and morpholine (tetrahydro-1,4-oxazine). A commercially available dihydro-1,3-oxazine is a reagent in the Meyers synthesis of aldehydes. Fluorescent dyes such as Nile red and Nile blue are based on the aromatic benzophenoxazine. Cinnabarine and cinnabaric acid are two naturally occurring dioxazines, being derived from biodegradation of tryptophan. Dioxazines Dioxazines are pentacyclic compounds consisting of two oxazine subunits. A commercially important example is the pigment pigment violet 23. Benzoxazines Benzoxazines are bicyclic compounds formed by the ring fusion of a benzene ring with an oxazine. Polybenzoxazines are a class of polymers formed by the ...
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Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e. ...
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Opioid-related Disorder
Opioid use disorder (OUD) is a substance use disorder characterized by cravings for opioids, continued use despite physical and/or psychological deterioration, increased tolerance with use, and withdrawal symptoms after discontinuing opioids. Opioid withdrawal symptoms include nausea, muscle aches, diarrhea, trouble sleeping, agitation, and a low mood. Addiction and dependence are important components of OUD. Risk factors for OUD include a history of opioid misuse, current opioid misuse, young age, socioeconomic status, race, untreated psychiatric disorders, and environments that promote misuse (social, family, professional, etc.). Complications may include opioid overdose, suicide, HIV/AIDS, hepatitis C, and problems meeting social or professional responsibilities. Diagnosis may be based on criteria by the American Psychiatric Association in the DSM-5. If more than two of 11 criteria are present during a year, the diagnosis is said to be present. Opioids include substanc ...
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