U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 151 - 160 of 208 results

S-Adenosylmethionine (often referred to as SAMe) is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. SAM is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma (HCC), HepG2 cells and colon cancer cells. Because of structural instability, stable salt forms of SAM are required for its use as an oral drug. The commonly used salts: tosylate, butanedisulfonate, disulfate tosylate, disulfate ditosylate, and disulfate monotosylate. SAMe has been marketed in some European countries since the mid-1980s for the treatment of depression and for other medical conditions such as osteoarthritis (joint disease that causes joint pain and stiffness), fibromyalgia (widespread pain and stiffness). In addition, it is used to treat liver disease and migraine headaches. However, it is not formally approved in the UK for the treatment of depression, and in the USA, it is classified only as a dietary supplement. Some research suggests that it is more effective than placebo in treating mild-to-moderate depression and is just as effective as antidepressant medications without the side effects (headaches, sleeplessness, and sexual dysfunction). In addition, antidepressants tend to take 6 to 8 weeks to begin working, while It seems to begin more quickly. Researchers are not sure how SAMe works to relieve depression. But they speculate it might increase the amount of serotonin in the brain just as some antidepressants do. Many studies have examined injectable forms of SAMe, not oral supplements.
Status:
Possibly Marketed Outside US
Source:
NCT04597190: Phase 4 Interventional Active, not recruiting PTSD
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Serotonin (5-hydroxytryptamine, or 5-HT) is a monoamine neurotransmitter produced by serotonergic neurons in the CNS and enterochromaffin cells in the gastrointestinal tract. Pharmacologic action of serotonin is mediated by a large and diverse range of 5-HT receptors. Serotonin plays an important part in the biochemistry of depression, migraine, bipolar disorder, and anxiety. It is also believed to be influential on sexuality and appetite. Creatinine is a product of the metabolic breakdown of creatine phosphate in muscle. Creatinine is filtered by healthy kidneys. Serotonin creatinine sulfate complex was the first isolated salt form of serotonin.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Aldosterone is a hormone secreted by the adrenal cortex that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium. Recent findings have shown that the physiological functions of the hormone aldosterone go far beyond its well-known role in blood-pressure regulation and salt/water homeostasis. Aldosterone is for example involved in the regulation of inflammation, and also binds directly to mineralocorticoid receptors in specific brain regions. At the late distal tubule and collecting duct, aldosterone has two main actions: 1) aldosterone acts on mineralocorticoid receptors (MR) on principal cells in the distal tubule of the kidney nephron, increasing the permeability of their apical (luminal) membrane to potassium and sodium and activates their basolateral Na+/K+ pumps, stimulating ATP hydrolysis leading to phosphorylation of the pump and a conformational change in the pump exposes the Na+ ions to the outside. The phosphorylated form of the pump has a low affinity for Na+ ions, hence reabsorbing sodium (Na+) ions and water into the blood, and secreting potassium (K+) ions into the urine; 2) aldosterone stimulates H+ secretion by intercalated cells in the collecting duct, regulating plasma bicarbonate (HCO3−) levels and its acid/base balance; and 3) aldosterone may act on the central nervous system via the posterior pituitary gland to release vasopressin (ADH) which serves to conserve water by direct actions on renal tubular resorption.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Uracil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Uracil is a common and naturally occurring pyrimidine derivative, one of the four nucleobases in the nucleic acid of RNA In RNA, uracil binds to adenine via two hydrogen bonds. In DNA, the uracil nucleobase is replaced by it’s methylated form -- thymine. Originally discovered in 1900 by Alberto Ascoli, it was isolated by hydrolysis of yeast nuclein;[4] it was also found in bovine thymus and spleen, herring sperm, and wheat germ. It is a planar, unsaturated compound that has the ability to absorb light. Uracil readily undergoes regular reactions including oxidation, nitration, and alkylation. While in the presence of phenol (PhOH) and sodium hypochlorite (NaOCl), uracil can be visualized in ultraviolet light. Uracil also has the capability to react with elemental halogens because of the presence of more than one strongly electron donating group. Uracil readily undergoes addition to ribose sugars and phosphates to partake in synthesis and further reactions in the body. Uracil becomes uridine, uridine monophosphate (UMP), uridine diphosphate (UDP), uridine triphosphate (UTP), and uridine diphosphate glucose (UDP-glucose). Each one of these molecules is synthesized in the body and has specific functions. Uracil's use in the body is to help carry out the synthesis of many enzymes necessary for cell function through bonding with riboses and phosphates. Uracil serves as allosteric regulator and coenzyme for reactions in the human body and in plants. Uracil can be used for drug delivery and as a pharmaceutical. When elemental fluorine is reacted with uracil, 5-fluorouracil is produced. 5-Fluorouracil is an anticancer drug (antimetabolite) used to masquerade as uracil during the nucleic acid replication process. In combination with Tegafur, uracil used as a chemotherapy drug (called UFT or UFUR) used in the treatment of cancer, primarily bowel cancer. UFT is an anticancer medication composed of a fixed molar ratio (1:4) of tegafur and uracil to be administered with calcium folinate.
Status:
Possibly Marketed Outside US
Source:
Japan:Androstenedione
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Androstenedione (Δ4-Androstenedione, 4-androstene-3,17-dione or 17-ketotestosterone) is an endogenous androgen steroid hormone and intermediate in the biosynthesis of testosterone from dehydroepiandrosterone (DHEA). In turn, Androstenedione is also a precursor of dihydrotestosterone (DHT), estrogens such as estradiol and estrone, and the neurosteroid 3α-androstanediol. Androstenedione is used to increase the production of the hormone testosterone to enhance athletic performance, increase energy, keep red blood cells healthy, enhance recovery and growth from exercise, and increase sexual desire and performance. Androstenedione has been shown to increase serum testosterone levels over an eight-hour period in men when taken as a single oral dose of 300 mg per day, but a dose of 100 mg had no significant effect on serum testosterone. However, serum levels of estradiol increased following both the 100 mg and 300 mg doses. The study also reported that the serum level of estrogens and testosterone produced varied widely among individuals. Androstenedione is currently used as a nutritional supplement to grow bigger muscles and stronger bones. This implies that androstenedione may have anabolic properties. Even though it has not been convincingly demonstrated yet that androstenedione is an anabolic steroid, its anabolic properties are likely based on its proven ability to increase testosterone levels. The role of testosterone in building stronger muscles and bones is widely accepted. Thus, high doses of testosterone-boosting drugs combined with strength training have been shown to increase muscle size and strength even in normal young men. This confirms what thousands of athletes who take anabolic steroids have known for decades. Yet androstenedione is different from testosterone-boosting drugs in a number of important aspects. To begin with, androstenedione is a naturally occurring substance that is produced by the body itself. In contrast to synthetic anabolic steroids, androstenedione is right at home in the human body, and perfectly complements the complex hormonal network in the body. Information about possible side effects and risks of androstenedione is very limited. Also, recent studies show that the drug's actions don't support manufacturer's claims. While a few individuals have shown increased levels of testosterone, most failed to achieve increases in blood testosterone levels. Initial medical research has raised concerns about this supplement's safety. Doctors worry that androstenedione may increase the risk of heart disease or liver cancer. In addition, research also associates androstenedione use with increases in estradiol, a female estrogen.
mixture
Status:
US Previously Marketed
Source:
Tryptar by Armour
(1951)
Source URL:
First approved in 1951
Source:
Tryptar by Armour
Source URL:

Class:
MIXTURE

mixture
Status:
US Previously Marketed
Source:
Mixed Tocopherols N.F.
(1921)
Source URL:
First marketed in 1921
Source:
Mixed Tocopherols N.F.
Source URL:

Class:
MIXTURE



Tocopherol (alpha tocopheryl nicotinate) is an ester of tocopherol and nicotinic acid. Vitamin E (Tocopherol) is sold commercially as the esterified form (alpha tocopheryl acetate, alpha tocopheryl succinate and alpha tocopheryl nicotinate). Alpha tocopheryl nicotinate has antioxidant and vasodilatory properties. It can be used as a mild warming agent, without producing the redness typical for nicotinic acid. Tocopherol (alpha tocopheryl nicotinate) has been available in Japan since 1967. Tocopherol under the brand name Juvela N is approved in Japan for the treatment of symptoms accompanying hypertension, hyperlipidemia, peripheral circulatory disturbance resulting from arteriosclerosis obliterans. Tocopherol has being shown to inhibit platelet aggregation.
mixture
Status:
Possibly Marketed Outside US
Source:
EnaSkin Dark Spot Corrector by EnaSkin LLC
(2023)
Source URL:

Class:
MIXTURE

mixture
Status:
Possibly Marketed Outside US
Source:
NCT04445857: Phase 4 Interventional Completed Analgesia
(2020)
Source URL:

Class:
MIXTURE

Showing 151 - 160 of 208 results