YCT529
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YCT529
YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clinical trials as a potential male contraceptive. The Vitamin A signalling system plays a number of important roles in bodily systems, such as the Immune system “It seems to me inherently unlikely that a compound with such activity would be free of side effects,” says Richard Sharpe, of the University of Edinburgh. See also * Adjudin * CDD-2807 * Dimethandrolone undecanoate * JQ1 JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals. BET inhibitors structurally similar to JQ1 are being tested in ... * TDI-11861 References {{reflist Contraception for males Experimental methods of birth control Pyr ...
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Retinoic Acid Receptor Alpha
Retinoic acid receptor alpha (RAR-α), also known as NR1B1 (nuclear receptor subfamily 1, group B, member 1) is a nuclear receptor that in humans is encoded by the ''RARA'' gene. NR1B1 is a gene with a protein product and has a chromosomal location of 17q21.2. RARA codes for the nuclear hormone receptor Retinoic Acid Receptor, Alpha subtype, and are themselves transcription factors. There are another 2 subtypes of RARs, Beta subtype, and Gamma subtype. Function Retinoid signaling is transduced by 2 families of nuclear receptors, retinoic acid receptor ( RAR) and retinoid X receptor ( RXR), which form RXR/RAR heterodimers. In the absence of ligand, DNA-bound RXR/RARA represses transcription by recruiting the corepressors NCOR1, SMRT ( NCOR2), and histone deacetylase. When ligand binds to the complex, it induces a conformational change allowing the recruitment of coactivators, histone acetyltransferases, and the basic transcription machinery. Retinoic Acid Receptor Alpha, th ...
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Male Contraceptive
Male contraceptives, also known as male birth control, are methods of preventing pregnancy that solely involve the male physiology. The most common kinds of male contraception include condoms, outercourse, and vasectomy. In domestic animals, castration is commonly used for contraception. Other forms of male contraception are in various stages of research and development. These include methods like RISUG/VasalGel (which has completed a small phase II clinical trial in humans in India) and ultrasound (with results so far obtained in experimental animals). Methods Surgery Vasectomy is a surgical procedure for male sterilization or permanent birth control. During the procedure, the vasa deferentia of a man are severed, and then tied or sealed to prevent sperm from entering into the seminal stream (ejaculate). Vasectomies are usually performed in a physician's office or medical clinic. CDC research has estimated there is a probability of 11 failures per 1,000 procedures over 2 years ...
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CDD-2807
CDD-2807 is a chemical compound which acts as a potent and selective inhibitor of serine/threonine-protein kinase 33 ( STK33), with a IC50 of 9.2 nM. In animal studies it causes production of abnormal sperm with reduced motility, and it has been investigated as a potential male contraceptive drug. See also * JQ1 * TDI-11861 * YCT529 YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clini ... References {{pharm-stub Indazoles Biphenyls Carboxamides Azetidines Piperidines Spiro compounds Ethynyl compounds Nitrogen heterocycles ...
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TDI-11861
TDI-11861 is a chemical compound which acts as a potent and selective inhibitor of soluble adenylyl cyclase (sAC). In animal studies it reversibly inhibits sperm motility, producing temporary infertility without hormonal side effects. While TDI-11861 is at an early developmental stage and is unlikely to be developed for medical uses in humans itself, it represents an important proof of concept which may potentially lead to the development of future male contraceptive drugs. See also * CDD-2807 * JQ1 * YCT529 YCT529 is a drug which acts as a potent and selective antagonist of the Vitamin A receptor retinoic acid receptor alpha (RAR-α). In studies on mice it produced a 99% reduction in sperm production, and it has proceeded to early stage human clini ... References {{pharm-stub Chloroarenes Pyrimidines Morpholines Pyrazoles Difluoromethyl compounds ...
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Vitamin A
Vitamin A is a fat-soluble vitamin and an essential nutrient for humans. It is a group of organic compounds that includes retinol, retinal (also known as retinaldehyde), retinoic acid, and several provitamin A carotenoids (most notably beta-carotene -carotene. Vitamin A has multiple functions: it is essential for embryo development and growth, for maintenance of the immune system, and for vision, where it combines with the protein opsin to form rhodopsin the light-absorbing molecule necessary for both low-light (scotopic vision) and color vision. Vitamin A occurs as two principal forms in foods: A) retinol, found in animal-sourced foods, either as retinol or bound to a fatty acid to become a retinyl ester, and B) the carotenoids alpha-carotene, β-carotene, gamma-carotene, and the xanthophyll beta-cryptoxanthin (all of which contain β-ionone rings) that function as provitamin A in herbivore and omnivore animals which possess the enzymes that cleave and convert provi ...
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Sperm Production
Spermatogenesis is the process by which haploid spermatozoa develop from germ cells in the seminiferous tubules of the testis. This process starts with the mitotic division of the stem cells located close to the basement membrane of the tubules. These cells are called spermatogonial stem cells. The mitotic division of these produces two types of cells. Type A cells replenish the stem cells, and type B cells differentiate into primary spermatocytes. The primary spermatocyte divides meiotically (Meiosis I) into two secondary spermatocytes; each secondary spermatocyte divides into two equal haploid spermatids by Meiosis II. The spermatids are transformed into spermatozoa (sperm) by the process of spermiogenesis. These develop into mature spermatozoa, also known as sperm cells. Thus, the primary spermatocyte gives rise to two cells, the secondary spermatocytes, and the two secondary spermatocytes by their subdivision produce four spermatozoa and four haploid cells. Spermatozoa are t ...
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Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ...
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Immune System
The immune system is a network of biological processes that protects an organism from diseases. It detects and responds to a wide variety of pathogens, from viruses to parasitic worms, as well as cancer cells and objects such as wood splinters, distinguishing them from the organism's own healthy tissue. Many species have two major subsystems of the immune system. The innate immune system provides a preconfigured response to broad groups of situations and stimuli. The adaptive immune system provides a tailored response to each stimulus by learning to recognize molecules it has previously encountered. Both use molecules and cells to perform their functions. Nearly all organisms have some kind of immune system. Bacteria have a rudimentary immune system in the form of enzymes that protect against virus infections. Other basic immune mechanisms evolved in ancient plants and animals and remain in their modern descendants. These mechanisms include phagocytosis, antimicrobial pe ...
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Adjudin
Adjudin (AF-2364) is a drug which is under development as a potential non-hormonal male contraceptive drug, which acts by blocking the production of sperm in the testes, but without affecting testosterone production. It is an analogue of the chemotherapy drug lonidamine, an indazole-carboxylic acid, and further studies continue to be conducted into this family of drugs as possible contraceptives. , adjudin was in phase II human trials. As shown in mature male rats, the agent induces reversible germ cell loss from the seminiferous epithelium by disrupting cell adhesion function between Sertoli and germ cells. It weakens the adhesion between the Sertoli cell and maturing sperm leading to a sloughing and loss of the latter. As it does not affect spermatogonia themselves the loss of fertility is reversible. In experiments hormonal levels ( FSH, LH, testosterone) were undisturbed during administration, and normal spermatogenesis returned in 95% of the tubules of rats at 210 days ...
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Dimethandrolone Undecanoate
Dimethandrolone undecanoate (DMAU), also known by its developmental code name CDB-4521, is an experimental androgen/anabolic steroid (AAS) and progestogen medication which is under development as a potential birth control pill for men. It is taken by mouth, but can also be given by injection into muscle. Side effects of DMAU include mild weight gain and mild decreases in levels of HDL cholesterol. It may also cause low estrogen levels and associated symptoms such as reduced sexual function and decreased bone mineral density. DMAU is an AAS, and hence is an agonist of the androgen receptor, the biological target of androgens like testosterone. It is also a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. Due to its androgenic and progestogenic activity, DMAU has antigonadotropic effects. These effects result in reversible suppression of sperm production and are respon ...
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Contraception For Males
Birth control, also known as contraception, anticonception, and fertility control, is the use of methods or devices to prevent unwanted pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth control only became available in the 20th century. Planning, making available, and using birth control is called family planning. Some cultures limit or discourage access to birth control because they consider it to be morally, religiously, or politically undesirable. The World Health Organization and United States Centers for Disease Control and Prevention provide guidance on the safety of birth control methods among women with specific medical conditions. The most effective methods of birth control are sterilization by means of vasectomy in males and tubal ligation in females, intrauterine devices (IUDs), and implantable birth control. This is followed by a number of hormone-based methods including oral pills, patches, vaginal rings, a ...
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Experimental Methods Of Birth Control
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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