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

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Status:
Investigational
Source:
INN:mecrilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mecrylate (metyl 2-cyanoacrylate) ) is a clear, colorless liquid with a strong, acrid odor. In contact with hydroxide ions (liquids like blood or water, air humidity), the cyanoacrylates form long, strong and waterproof chains in an exothermic reaction. The resulting polymer leads to a stable adhesive bond. It may be used as tissue adhesive in surgery. Mecrylate is the first generation short-chain cyanoacrylate, it turned out to be histotoxic and caused distinct foreign-body reactions.
Status:
Investigational
Source:
NCT03298373: Phase 1 Interventional Unknown status Healthy Men
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04084860: Phase 2 Interventional Recruiting Alcohol Use Disorder
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02097706: Phase 2 Interventional Recruiting Borderline Personality Disorder
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


N-Methyl-D-aspartic acid is an amino acid derivative acting as a specific agonist at the NMDA receptor, and therefore mimics the action of the neurotransmitter glutamate on that receptor. Unlike glutamate, NMDA only binds to and regulates the NMDA receptor and has no effect on other glutamate receptors (such as those for AMPA and kainate). NMDA receptors are particularly important when they become overactive during withdrawal from alcohol as this causes symptoms such as agitation and, sometimes, epileptiform seizures. NMDA is a water-soluble synthetic substance that is not normally found in biological tissue.
Status:
Investigational
Source:
NCT03506945: Not Applicable Interventional Recruiting Depressive Symptoms
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



MPEP (2-methyl-6-(phenylethynyl)pyridine) was one of the first compounds found to act a selective antagonist for the metabotropic glutamate receptor subtype mGluR5. It was under development by Novartis in the late 1990's. MPEP was found to produce neuroprotective effects following acute brain injury in animals. MPEP was also found to have positive effects on animal models of depression, anxiety and morphine withdrawl.
Status:
Investigational
Source:
NCT04182126: Not Applicable Interventional Recruiting LLIN, PBO LLIN, IRS, Larviciding
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01092689: Phase 1 Interventional Withdrawn Pancreas Cancer
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) is a mutagenic and carcinogenic heterocyclic amine formed during ordinary cooking, and is subsequently metabolically activated by cytochrome P4501A2 (CYP1A2) and N-acetyltransferase 2 (NAT2). PhIP has been used in trials studying the basic science of Pancreas Cancer.
Bardoxolone methyl, the C-28 methyl ester of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid (CDDO) known as CDDO-Me or RTA 402, is one of the derivatives of synthetic triterpenoids. Bardoxolone methyl directly blocks IKKbeta activity and thereby the NF-kappaB pathway by interacting with Cys-179 in the IKKbeta activation loop. Binding of bardoxolone methyl to Kelch-like erythroid cell-derived protein with CNC homology-associated protein 1 (Keap1) disrupts its critical cysteine residues, leading to the release of the nuclear factor erythroid 2-related factor 2 (Nrf2), which hinders its ubiquitination and finally leads to its stabilization and nuclear translocation. In the nucleus, Nrf2 activates the transcription of phase 2 response genes, leading to a coordinated antioxidant and anti-inflammatory response. In addition, it acts as an antagonist of the peroxisome proliferator-activated receptor gamma. Through Keap1/Nrf2 and nuclear factor-κB pathways, this agent can modulate the activities of a number of important proteins that regulate inflammation, redox balance, cell proliferation and programmed cell death. This agent is generally well tolerated, but it may increase adverse cardiovascular events. Presently, it is being further tested for the treatment of patients with chronic kidney disease, cancer, and pulmonary arterial hypertension.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)