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

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Showing 49871 - 49880 of 55039 results

Status:
Investigational
Source:
NCT00502710: Phase 2 Interventional Completed Diabetes Mellitus Type 2
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carmegliptin is a potent, long-acting, selective, orally bioavailable, pyrrolidinone-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. ). DPP-IV is a proline-specific serine protease enzyme that is known to rapidly inactivate two incretin hormones released during food ingestion, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Incretins are essential for regulating both fasting and postprandial plasma glucose by stimulating insulin secretion, supporting β-cell mass, and inhibiting glucagon production by the α-cells to reduce glucose production by the liver. By selectively inhibiting DPP-IV, carmegliptin prolongs the activity of circulating GLP-1 and GIP and improves their potential to prolong the antidiabetic actions. Carmegliptin is indicated for use as monotherapy or in combination with other oral antihyperglycemic agents for the treatment of Type 2 diabetes.
Status:
Investigational
Source:
INN:ciprefadol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ciprefadol is an opioid analgesic drug. It binds with a high affinity to mu (Ki 4.2 nM) and kappa (Ki 2.5 nM) opioid receptors. In vivo, ciprefadol displays mixed antagonist/agonist activity in the mouse writhing and the rat tail heat tests: in low doses, the compound inhibits the analgesic effect of morphine, while at higher doses it displays analgesic effect. Chronic administration of ciprefadol to rhesus monkeys produced a marked physical dependence more severe than that of morphine, and its effect was consistent with what would be expected of a potent, long-lasting morphine-like agonist.
Status:
Investigational
Source:
INN:cefmepidium chloride
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Cefmepidium is a semisynthetic cephalosporin with broad antibacterial activity against penicillin-resistant strains.
Status:
Investigational
Source:
INN:bromadoline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Bromadoline is a selective agonist of a μ-opioid receptor with potent analgesic activity developed by the Upjohn company in the 1970s for pain management.
Status:
Investigational
Source:
NCT01188967: Phase 2 Interventional Completed Nicotine Dependence
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Talaglumetad (also known as LY-544344) is a bicyclohexane derivative patented by Eli Lilly and Company as modulators of metabotropic glutamate receptor. Talaglumetad acts as a prodrug of Eglumegad, a selective agonist of metabotropic glutamate receptors (mGluR2/3) and metabolized to release active compound by both human jejunal homogenates and rat liver homogenates. In experiments on mice, Talaglumetad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment.
Status:
Investigational
Source:
INN:estrazinol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Estrazinol is a synthetic estrogen.
Status:
Investigational
Source:
INN:benzopyrronium bromide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT00003359: Phase 1 Interventional Completed Unspecified Adult Solid Tumor, Protocol Specific
(1998)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Batabulin or T138067 (2-fluoro-1-methoxy-4-pentafluorophenylsulfonamidobenzene) covalently and selectively modifies the beta1, beta2, and beta4 isotypes of beta-tubulin at a conserved cysteine residue, thereby disrupting microtubule polymerization. Cells exposed to batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy. Batabulin is equally efficacious in inhibiting the growth of sensitive and multidrug-resistant human tumor xenografts in athymic nude mice. Batabulin has been in clinical trials for the treatment of cancers (breast cancer, colorectal cancer, glioma, hepatocellular carcinoma, non-small cell lung cancer). It does not have clinical activity in the treatment of colorectal cancer and glioma. Batabulin development was discontinued.
Status:
Investigational
Source:
INN:hexasonium iodide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Hexasonium, an anticholinergic agent, was studied as a spasmolytic. Information about the current use of this drug is not available.

Showing 49871 - 49880 of 55039 results