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

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Showing 51 - 60 of 1509 results

Status:
Investigational
Source:
USAN:STIROFOS [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

(E)-Tetrachlorovinphos is an (E)- isomer of Tetrachlorovinphos. Tetrachlorovinphos is an organophosphate cholinesterase inhibitor that is used as an insecticide. Tetrachlorvinphos was introduced and first used commercially in 1966 in the USA. Tetrachlorvinphos was originally registered for use on various food crops, livestock, pet animals. Tetrachlorvinphos is applied dermally to livestock to control flies and mites. It is used as an oral larvicide in cattle, hog, goats and horses; in cattle ear tags to control flies; in cattle feedlots; in poultry dust boxes to control poultry mites; and in poultry houses. Tetrachlorvinphos also is used in pet sleeping areas and pet flea collars and to control flies around refuse sites, recreational areas, and for general outdoor treatment. Tetrachlorvinphos can cause cholinesterase inhibition in humans; that is, it can overstimulate the nervous system causing nausea, dizziness, confusion, and at very high exposures (e.g., accidents or major spills), respiratory paralysis and death. In 2014, the Natural Resources Defense Council (NRDC) filed a lawsuit against the United States Environmental Protection Agency (EPA) seeking EPA to respond to NRDC’s 2009 petition to ban tetrachlorvinphos in common pet flea treatment products. Tetrachlorvinphos is reportedly registered for use in Canada, South Africa, and Australia.
Status:
Investigational
Source:
INN:ilmofosine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ilmofosine (1-hexadecylthio; 2-methoxyethyl-racglycero-3-phosphocholine) is a synthetic 1-S-thioether alkyl lysophospholipid derivative with potential antineoplastic activity. In extensive preclinical evaluation against tumor cell lines and in the human tumor colony-forming assay, Ilmofosine was cytotoxic against both leukemias and solid tumors. Ilmofosine was effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma. Ilmofosine exhibited competitive inhibition of protein kinase C activity with respect to phosphatidyl-serine and inhibited the enzyme activated by diolein.
Status:
Investigational
Source:
J Antimicrob Chemother. Nov 2023;78(11):2702-2714.: Not Applicable Human clinical trial Completed Leishmaniasis, Visceral
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phosphorylcholine (ChoP) is a small zwitterionic amino alcohol, which is composed of a negatively charged phosphate bonded to a small, positively charged choline group. Phosphorylcholine is the precursor metabolite of choline in the glycine, serine, and threonine metabolism pathways and in intermediate between choline and cytidine-diphosphate choline in the glycerophospholipid metabolism pathway. Phosphorylcholine is an interesting compound from an immunologic point of view, being an immunodominant determinant of pneumococcal teichoic acids and also a major prerequisite for proinflammatory effects of PAF and PAF-like lipids where PC is a common denominator. PC is also a component of some bacteria, apoptotic cells, and OxLDL, which, if exposed, is immunogenic. PC has several properties that could in principle both promote and protect against disease, depending on the pathogen and type of inflammatory reaction. In the field of interventional cardiology, phosphorylcholine is used as a synthetic polymer-based coating, applied to drug-eluting stents, to prevent the occurrence of coronary artery restenosis. To date, more than 120,000 Phosphorylcholine-coated stents have been implanted in patients with no apparent deleterious effect in the long term compared to bare metal stent technologies
Status:
Investigational
Source:
INN:vincofos
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Vincofos is a broad-spectrum canine anthelmintic. All or nearly all of the ascarids, hookworms, whipworms, and the tapeworm, Taenia pisiformis, were expelled following therapy with vincofos. The tapeworm, Dipylidium caninum, was also effectively removed by the vincofos treatment, but it appeared that a slightly greater dosage would be required to obtain maximum anthelmintic effect.
Status:
Investigational
Source:
INN:sodium picofosfate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Picofosforic acid is the laxative.
Status:
Investigational
Source:
INN:norcodeine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Norcodeine is the N-demethylated derivative of codeine. It has relatively little opioid activity in its own right, but is formed as a metabolite of codeine following ingestion. Codeine and its other major metabolites codeine-6-glucuronide and norcodeine have weak affinity to opioid μ-receptors.
Status:
Investigational
Source:
INN:fosfosal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fosfosal (2-phosphonoxybenzoic acid) is a O-phosphorylated derivative of salicylic acid used in analgesic and anti-inflammatory therapy. Fosfosal showed analgesic effect in the acetic acid-induced writhing and in the hot plate tests in mice, and showed antiinflammatory effect in the xylene induced mice ears swelling and in acetic acid induced increased vascular permeability tests in mice. Both the effects had no significant differences between fosfosal and aspirin, but the former had less stomach irritation.
Dexfosfoserine (Phosphoserine, L-Serine-O-Phosphate, O-Phosphoserine), the most abundant phosphoamino acid in the eukaryotic phosphoproteome, is not encoded in the genetic code but synthesized posttranslationally. Dexfosfoserine is an agonist of the group III metabotropic glutamate receptors. This endogenous compound inhibits neural stem cells proliferation and promotes survival of nascent neurons thus it has potential therapeutic value in addition to its basic utility as a probe for dissecting molecular mechanisms underlying neurogenesis.
Status:
Investigational
Source:
INN:tafluposide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tafluposide (also known as F 11782) is an epipodophyllotoxin derivative patented by Pierre Fabre Medicament as an antitumor agent. Tafluposide acts as a catalytic inhibitor of topoisomerases I and II, that capable of completely inhibiting the DNA-binding activity of topoisomerase. In preclinical models single or multiple i.p. doses of Tafluposide proves highly active against the s.c. grafted B16 melanoma, significantly increasing survival and inhibiting tumor growth. Tafluposide inhibits the number of pulmonary metastatic foci of the melanoma by 99%. In human tumor xenograft studies, multiple i.p. doses of Tafluposide results in major inhibitory activity against breast) tumors, as well as causing definite tumor regression. Significant activity was also recorded Tafluposide against the refractory lung xenografts.
Status:
Investigational
Source:
INN:flufosal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLUFOSAL is an antithrombotic agent.