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

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Showing 91 - 100 of 7029 results

Status:
Investigational
Source:
INN:cloticasone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cloticasone is a synthetic glucocorticoid corticosteroid, an analog of fluticasone. Cloticasone was discovered by Glaxo in the 1980s and claimed to be useful as an antiinflammation agent.
Status:
Investigational
Source:
INN:silicristin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Silicristin is a flavonolignan isolated from Silybum marianum and has been shown to exhibit inhibitory activities against lipoxygenase and prostaglandin synthetase. It has a role as a radical scavenger, a lipoxygenase inhibitor, a prostaglandin antagonist and a metabolite. It is a flavonolignan, a member of 1-benzofurans, a polyphenol, an aromatic ether and a secondary alpha-hydroxy ketone. Silicristin is a potent inhibitor of the thyroid hormone transporter MCT8. Silicristin is a sodium pump inhibitor, it inhibited Na(+)/K(+)-ATPase (NKA) with IC50 of 110 uM. Silicristin exhibits relatively good antioxidant effectiveness against phenylglyoxylic ketyl radicals and DPPH. Silicristin protects cardiomyocytes against doxorubicin-induced oxidative stress is due mainly to their cell membrane stabilization effect, radical scavenging and iron chelating potency.
Status:
Investigational
Source:
INN:sumacetamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Sumacetamol is a acetylaminothioalkanoate derivative patented by Sterwin A.-G. as an analgesic and antipyretic agent. Sumacetamol is used in combination with free paracetamol. In clinical trials, Sumacetamol failed to demonstrate superior efficacy in pain and swelling management compare to paracetamol but shows a longer duration of analgesia. The rates of reported adverse events were similar in paracetamol and Sumacetamol, although reports of mild to moderate drowsiness were more common after the Sumacetamol combination.
Status:
Investigational
Source:
INN:carbofenotion
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carbophenothion is a highly toxic organophosphate insecticide used as a citrus pesticide called Trithion. Carbophenothion is a potent inhibitor of acetylcholinesterase, a neuromuscular enzyme that is widely needed for the normal function of insects, as well as people and many other animals. The Environmental Protection Agency (EPA) classifies it as a Restricted Pesticide (RUP). Carbophenothion is used in various brands, such as Trithion. This pesticide contains 80% Carbophenothion as its only active ingredient. Due to the widespread use of these organophosphates in the United States in the nineties, this was the most common cause of agricultural poisoning. Carbophenothion is used as an insecticide and acaricide, the main purpose of which is to protect citrus fruits, but also to protect the cotton from aphids (lice) and spider mites. In addition, it is used in combination with oil, and also as a pesticide against many other pests on fruits, nuts, vegetables, sorghum, corn, and others. In addition, it is used to combat animal parasites.
Status:
Investigational
Source:
INN:dimiracetam
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Dimiracetam is a nootropic drug of the racetam family. Dimiracetam inhibited the NMDA-induced increase of [3H]D-Asp release from hippocampal synaptosomes. The increased potency and longer duration of action of dimiracetam, together with the potential cognition enhancing property makes it a very promising and safe for the treatment of neuropathic pain conditions for which there are very limited therapeutic options. Dimiracetam is in Phase II clinical trials for the treatment of HIV-associated pain and in phase I clinical trials for the treatment of osteoarthritis pain.
Status:
Investigational
Source:
INN:diproleandomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Diproleandomycin is a semisynthetic antibacterial agent. This antibiotic produced by Streptomyces antibiotocus.
Status:
Investigational
Source:
INN:sardomozide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sardomozide (previously known as SAM486A or CGP-48664) was developed as an inhibitor of S-adenosyl-methionine-decarboxylase, a key enzyme for polyamine biosynthesis. Sardomozide possessed the broad-spectrum antiproliferative and antitumor activity. The drug participated in a phase II clinical trial as a monotherapy in patients with refractory or relapsed non-Hodgkin's lymphoma. In Phase II clinical trial in patients with metastatic melanoma, the drug didn’t have significant therapeutic potential. The further development of this drug was discontinued.
Status:
Investigational
Source:
INN:burapitant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Burapitant (SSR-240,600) is a drug developed by Sanofi-Aventis which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor. Burapitant inhibited the binding of radioactive substance P to tachykinin NK1 receptors in human lymphoblastic IM9 cells, human astrocytoma U373MG cells, and human brain cortex. It also showed a subnanomolar affinity for guinea pig NK1 receptors but was less potent on rat and gerbil NK1 receptors. Burapitant inhibited [Sar(9),Met(O2)(11)]substance P-induced inositol monophosphate formation in human astrocytoma U373MG cells. Burapitant (0.1-10 mg/kg i.p. or p.o.) antagonized the excitatory effect of i.c.v. infusion of [Sar(9),Met(O2)(11)]substance P (SP) on the release of acetylcholine in the striatum of anesthetized and awake guinea pigs. This antagonistic action was still observed after repeated administration of Burapitant (5 days, 10 mg/kg p.o., once a day). Burapitant (10 mg/kg i.p.) inhibited the phosphorylation of the cAMP response element-binding protein in various brain regions induced by i.c.v. administration of [Sar9,Met(O2)(11)]SP. While burapitant itself did not proceed beyond early clinical trials and was never developed for clinical use in humans, promising animal results from this and related compounds have led to a number of novel drugs from this class that has now been introduced into medical use.
Status:
Investigational
Source:
INN:codoxime [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Codoxime is a synthetic derivative of an opiate dihydrocodeinone. It differs from dihydrocodeinone by the substitution of a carboxymethyl oxime for the ketonic oxygen at carbon 6 of the dihydrocodeinone molecule. Codoxime has been proposed as an antitussive with prolonged duration of action. In a clinical trial conducted on prisoner volunteers in 1966, it was found that codoxime has a capacity to produce physical dependence of the morphine type.
Status:
Investigational
Source:
INN:chloroserpidine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Chloroserpidine is deserpidine derivative with hypotensive and sedative action