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

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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NCT01092689: Phase 1 Interventional Withdrawn Pancreas Cancer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.
Status:
Designated
Source:
FDA ORPHAN DRUG:582017
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Chryseriol (Chrysoeriol) is a methoxylated flavone of great scientific interest because of its promising antioxidant, antiinflammatory, antitumor, antimicrobial, antiviral, and free radical scavenging activities. Chryseriol is a promising inhibitor of protein kinase CK2α and CK2α', the catalytic subunits of CK2, with IC50 values of 250 and 34 nM for CK2α and CK2α', respectively. Chrysoeriol produced a noncompetitive and mixed inhibition of pancreatic lipase with IC50=158uM. Chryseriol is a dual c‑Met and VEGFR2 kinase inhibitor. The results of docking experiments revealed that chrysoeriol was able to efficiently bind in the active site cavity of c‑Met and VEGFR2. The results of enzymatic assays showed relatively high binding affinities of chrysoeriol to c‑Met (Kd=12 uM) and VEGFR2 (Kd=11 uM). Chrysoeriol selectively inhibited human recombinant CYP1B1-mediated 7-ethoxyresorufin-O-deethylation (EROD) activity 5-fold more than that of CYP1A1-mediated activity in a competitive manner. Additionally, chrysoeriol inhibited E(2) hydroxylation catalyzed by CYP1B1, but not by CYP1A1. So chrysoeriol is a chemopreventive natural ingredient that can selectively inhibit CYP1B1 activity and prevent the formation of carcinogenic 4-OHE(2) from E(2.). Chrysoeriol was a selective PI3K-AKT-mTOR pathway inhibitor. It restrained the proliferation of human multiple myeloma cells, but didn't affect proliferation of PBMNCs from normal donors. It might exhibit the cell cycle regulatory effect via the inhibition of PI3K-AKT-mTOR signal pathway. The US Food and Drug Administration (FDA) recently granted orphan drug approval for Chrysoeriol, a cannabis-based drug used to treat acute myeloid leukaemia, which was developed by Jamaican scientist Dr Henry Lowe.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)