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Restrict the search for
l-glutamine
to a specific field?
Status:
Investigational
Source:
NCT04049669: Phase 2 Interventional Recruiting Glioblastoma
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Indoximod is an orally available Indoleamine 2,3-dioxigenase inhibitor. It shows higher potency in reversing IDO-mediated T cell suppression. Indoximod improves the efficacy of multiple chemotherapeutics agents and some immunological checkpoints mediators in Phase I/II clinical studies for metastatic breast cancer, metastatic melanoma, non-small cell lung cancer, primary malignant brain tumors, metastatic pancreatic cancer, as well as metastatic prostate cancer.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fostedil (KB-944) is a phosphonic acid derivative with potent vasodilator activity. KB-944 has been demonstrated to produce long lasting coronary vasodilator and hypotensive effects in conscious and anesthetized dogs; increase coronary blood flow in isolated, blood perfused heart preparations of dogs; and reduce systemic pressure in conscious normotensive and hypertensive rats. Slow channel calcium entry blockade is thought to contribute to the vasodilator activity of KB-944. Fostedil is longer acting in hypertensive animals than either nifedipine or diltiazem suggesting a potential clinical advantage for this compound. Unexpectedly, fostedil was shown to produce atrial fibrillation in 3 of 10 hypertensive patients in a placebo controlled study. Fostedil had been in phase II clinical trials for the treatment of angina pectoris. However, this research has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Triletide is a tripeptide derivative which shows cytoprotective and antiulcerogenic activity. It is a thromboxane synthase inhibitor. Analysis of both individual and pooled data indicated that triletide was well absorbed after oral administration, with a lag time of 0.3 hours and the blood peak was reached after about 1.1 to 1.3 hours. Metabolization to desmethyl, desacetyl, desmethyl-desacetyl and hydroxylated derivatives plays a major role in the biotransformation of the drug and thus in its disappearance from blood, the distribution half-life being about 1 hour. A greater proportion of patients given the combination cimetidine and triletide was found to be endoscopically healed after treatment in comparison with those who had cimetidine alone (53% vs 40%). Intensity of symptoms decreased significantly faster and to a significantly greater extent in the same patients, as did antacid intake. Triletide appears to be equally well tolerated as, but significantly more effective than, aluminium hydroxide and magnesium hydroxide in relieving symptoms and promoting healing in patients with mild to moderate duodenal ulcer. There were no complaints of possible side-effects with either triletide treatment and no evidence of any significant changes in blood pressure, heart rate or routine haematology and haematochemistry investigations.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sampatrilat (also known as UK 81252) was developed as a dual inhibitor of both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). This drug was studied for the treatment of hypertension and congestive heart failure.
Status:
Investigational
Source:
NCT00689221: Phase 3 Interventional Completed Glioblastoma
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Cilengitide is a cyclized Arg-Gly-Glu (RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins. Its precursor was first synthesized in 1995 as c(RGDfV), and later modified by the incorporation of N-methyl Val c(RGDfMetV), generating the current form of the drug. Cilengitide displays subnanomolar antagonistic activity for αvβ3 and αvβ5, and is the first integrin antagonist evaluated in clinical phase I and II trials for treatment of glioblastoma and several other tumor types. Cilengitide-induced glioma cell death and inhibition of blood vessel formation may use different molecular mechanisms, including regulation of tumor hypoxia and activation of apoptotic pathways. Cilengitide inhibits cell signaling through FAK-Src-Akt and Erk mediated pathways in endothelial and tumor cells and attenuates the effect of VEGF stimulation on growth factor signaling. Cilengitide has shown encouraging activity in patients with glioblastoma as single agent, and in association with standard RT and temozolomide.
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.
Class (Stereo):
CHEMICAL (ACHIRAL)
Cirazoline is an agonist of alpha1A adrenergic receptor, a partial agonist of alpha1B and alpha1D receptors, and an antagonist of alpha2 adrenergic receptors. Cirazoline was used to study the biologic function of adrenergic receptors. Injection of cirazoline into to the paravenricular hypothalamic nucleus of rats suppressed food and water intake. Cirazoline caused a large renal vasopressor response in rats. Systemic administration of cirazoline impaired spatial working memory in monkeys.
Status:
Investigational
Source:
NCT03781128: Phase 2 Interventional Recruiting Cluster Headache
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Lysergide (LSD) is a semi-synthetic hallucinogen and is one of the most potent drugs known. Recreational use became popular between the 1960s to 1980s, but is now less common. LSD was first synthesized by Albert Hoffman while working for Sandoz Laboratories in Basel in 1938. Some years later, during a re-evaluation of the compound, he accidentally ingested a small amount and described the first ‘trip’. During the 1950s and 1960s, Sandoz evaluated the drug for therapeutic purposes and marketed it under the name Delysid®. It was used for research into the chemical origins of mental illness. Recreational use started in the 1960s and is associated with the ‘psychedelic period’. LSD possesses a complex pharmacological profile that includes direct activation of
serotonin, dopamine and norepinephrine receptors. In addition, one of its chief sites of
action is that of compound-specific (“allosteric”) alterations in secondary messengers
associated with 5HT2A and 5HT2C receptor activation and changes in gene expression.
The hallucinogenic effects of LSD are likely due to agonism at 5HT2A and 5HT2C
receptors. LSD is also an agonist at the majority of known
serotonin receptors, including 5HT1A, 5HT1B, 5HT1D, 5HT5A, 5HT6 and 5HT7 receptors. During the 1960s, LSD was investigated for a variety of psychiatric indications, including the following: as an aid in treatment of schizophrenia; as a means of creating a "model psychosis"; as a direct antidepressant; and as an adjunct to psychotherapy. LSD is listed in Schedule I of the United Nations 1971 Convention on Psychotropic Substances.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Enalkiren (A-64662) is a potent, dipeptide renin inhibitor, mimics the transition state of the human renin substrate, angiotensinogen. The results of clinical trials with enalkiren suggest that renin inhibitors may be safe, useful therapeutic agents in the management of hypertension. In addition, it exerts intraocular pressure lowering pressure. Enalkiren development for the treatment of glaucoma, heart failure, hypertension has been discontinued.
Status:
Investigational
Source:
NCT03231878: Phase 2/Phase 3 Interventional Completed Adrenoleukodystrophy
(2017)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Hydroxypioglitazone (M-IV) is an active metabolite of the peroxisome proliferator-activated receptor γ (PPARγ) agonist pioglitazone. Experiments in vitro have shown that hydroxypioglitazone was more efficient than the parent drug in stimulating lipid synthesis.
