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

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Showing 171 - 180 of 511 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


6-Thioguanosine (or thioguanosine) is a metabolite of 6-thioguanine, an immunosuppressant and anticancer prodrug, and plays a major role in the prodrug's overall photoreactivity. 6-Thioguanosine has been shown to induce DNA damage and cell death upon exposure to UVA radiation, which is correlated to the significant increase in skin cancers following prolonged treatment with thiopurine prodrug. Also existed experiments where 6-thioguanosine was used to treat idiopathic myocardial hypertrophy and where it showed clinical value in cancer chemotherapy.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



3-Deaza-adenosine (BW 91Y) is a potent inhibitor of adenosine deaminase and S-Adenosylhomocysteine (SAH) hydrolase, with potent antitumor activity against a range of leukemia cell lines. 3-Deaza-adenosine has anti-inflammatory properties, inhibiting leukocyte adhesion and chemotaxis, lymphocyte-mediated cytolysis, phagocytosis, degranulation, and NF-κB signaling. 3-Deaza-adenosine also has antiviral and antibacterial activities. 3-Deaza-adenosine has previously been shown to inhibit a variety of cellular functions, which could be critical for the development of atherosclerosis and restenosis. These include the thrombin-stimulated production of platelet-derived growth factor and the expression of endothelial leukocyte adhesion molecule-1 as well as cellular arachidonic acid and ROS production. Moreover, c3Ado prevents tumor necrosis factor (TNF)-alpha production, reduces TNF- alpha-induced macrophage adhesion to endothelial cells in vitro via the inhibition of ICAM-1 synthesis, and promotes monocyte apoptosis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Silver picrate is a poisonous explosive yellow crystalline salt (O2N)3C6H2OAg.H2O used as an antiseptic especially in vaginitis and urethritis
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control cystine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cystine is the oxidized dimer form of the amino acid cysteine. Cystine serves two biological functions, a site of redox reactions and a mechanical linkage that allows proteins to retain their 3-dimensional structure. It is common in many foods such as eggs, meat, dairy products, and whole grains as well as skin, horns and hair. Human hair and skin contain approximately 10–14% cystine by mass. Cysteine supplements are sometimes marketed as anti-aging products with claims of improved skin elasticity. Cysteine is more easily absorbed by the body than cystine, so most supplements contain cysteine rather than cystine. N-acetyl-cysteine (NAC) is better absorbed than other cysteine or cystine supplements.
Status:
US Previously Marketed

Class (Stereo):
CHEMICAL (ABSOLUTE)


N-Acetylglucosamine (N-acetyl-D-glucosamine, or GlcNAc,) is a monosaccharide and a derivative of glucose. It is part of a biopolymer in the bacterial cell wall, built from alternating units of GlcNAc and N-acetylmuramic acid (MurNAc), cross-linked with oligopeptides at the lactic acid residue of MurNAc. This layered structure is called peptidoglycan (formerly called murein). GlcNAc is the monomeric unit of the polymer chitin, which forms the outer coverings of insects and crustaceans. It is the main component of the radulas of mollusks, the beaks of cephalopods, and a major component of the cell walls of most fungi. It is lnsown, that the breakdown of glycosaminoglycans is an important consequence of inflammation at mucosal surfaces, and inhibition of metalloprotease activity may be effective in treating chronic inflammation. GlcNAc directly incorporates into glycosaminoglycans and glycoproteins, as a substrate for tissue repair mechanisms. It was shown, that GlcNAc was promising substance for treatment of chronic inflammatory bowel disease, with a mode of action which is distinct from conventional treatments. In experiments on rabbits with osteoarthritis, was found chondroprotective effects of aminomonosaccharide glucosamine, but no statistically significant difference was found between study groups. It was also investigated for the treatment of Multiple sclerosis, however, as a drug development target, GlcNAc had significant limitations. GlcNAc has poor membrane permeability, requiring high concentrations for biological effects.
Cisapride is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be expected to compromise the beneficial effects of cisapride.
Cholesterol is a sterol (a combination steroid and alcohol) and a lipid found in the cell membranes of all body tissues, and transported in the blood plasma of all animals. The high level of cholesterol in the blood is a marker of hypercholesterolemia, also called dyslipidemia. As a part of homeopathic product, it helps to support general liver and gallbladder health, and is used for temporary relief of symptoms related to adrenal glands such as fatigue and low energy. Cholesterol binds to and affects the gating of a number of ion channels such as the nicotinic acetylcholine receptor (nAChR) Inwardly-rectifying K+ channels (Kir); Transient receptor potential vanilloid 1 channels (TRPV1) and Large-conductance Ca2+-sensitive voltage-gated K+ channels (BK). It was shown the new mechanistic insights into the role of cholesterol in the regulation of nAChR, showing that cholesterol regulates the channels by two distinct mechanisms: stabilization of the channels in a resting state that depends on specific lipid-protein interactions and facilitation of the transitions between uncoupled and coupled states that depends on the hydrophobic thickness of the membrane
Status:
US Previously Marketed
First approved in 1980

Class (Stereo):
CHEMICAL (ACHIRAL)



Cinoxacin is a synthetic antibacterial agent for oral administration. Cinoxacin mode of action involves the inhibiting of DNA gyrase, a type II topoisomerase, and topoisomerase IV. Adverse effects are nausea, anorexia, vomiting, abdominal cramps/pain, perverse taste, diarrhea, headache, dizziness, rash, urticaria, pruritus, edema and other.
Status:
US Previously Marketed
Source:
Triazure by Parke-Davis
(1975)
Source URL:
First approved in 1975
Source:
Triazure by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azaribine (2′, 3′, 5′-triacetyl-6-azauridine) is the orally absorbable triacetylated derivative of the pyrimidine analog 6-azauridine. Ribonucleoside of 6-azauracil, which can be derived in the tissues by the deacetylation of azaribine, has been shown, after its intracellular conversion to 6-azauridine-5'-monophosphate, to serve as an inhibitor of the activity of a key enzyme, orotidine-5'-monophosphate (OMP) decarboxylase, critically concerned with the biosynthesis de novo of pyrimidines essential for the formation of nucleic acids. Azaribine exerts antineoplastic action. In 1975 azaribine was approved for the treatment of psoriasis. The drug was withdrawn because it may cause life-threatening or fatal blood clots in the veins and arteries.
Chloranil is an oxidant, practically useful for dehydrogenation to aromatic and alpha,beta-desaturated carbonyl compounds. Chloranil was found to inhibit human carboxylesterases: carboxylesterase 1 and 2, acetylcholinesterase and butyrylcholinesterase. In 1950s chloranil ointment was used for the treatment of psoriasis and onychomycosis.

Showing 171 - 180 of 511 results