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

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Showing 1551 - 1560 of 21518 results

Status:
Investigational
Source:
INN:etolorex
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Etolorex is an anorectic agent.
Status:
Investigational
Source:
INN:delanterone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Delanterone is an antiandrogen steroid, developed by the Dutch company Gist-Brocades N.V. for the treatment of various dermatological disorders, including hirsutism, acne, seborrhea, alopecia androgenetica, and baldness. The compound is claimed to show topical anti-androgenic activity with very weak systemic anti-androgenic activity, a lack of progesterone, anti-gonadotrophin and corticosteroid-like activity and very low toxicity.
Status:
Investigational
Source:
NCT03739125: Phase 3 Interventional Completed Type2 Diabetes
(2017)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lobeglitazone (trade name Duvie; Chong Kun Dang Pharmaceutical Corporation) was developed as effective and safe antidiabetic TZD drug. Lobeglitazone is a peroxisome proliferator-activated receptor-γ agonist. Lobeglitazone was conceptually designed by modification of the rosiglitazone structure with a substituted pyrimidine. Lobeglitazone has a p-methoxyphenoxy group at the 4-position of the pyrimidine moiety. Lobeglitazone showed more potent activity than the reference compounds (pioglitazone and rosiglitazone) with an EC50 value of 0.018 uM in a type 2 diabetes animal model, which is 16 times lower than pioglitazone (EC50 0.30 uM). Lobeglitazone exhibited similar efficacy profiles in glycemic control and lipid modulation to pioglitazone, but with a 30 times smaller dose in clinical studies. Lobeglitazone displays 12 times higher affinity to PPARγ than rosiglitazone and pioglitazone. Lobeglitazone acts as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By promoting the binding of insulin at fat cells, lobeglitazone has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles. Lobeglitazone was approved by the Ministry of Food and Drug Safety (Korea) in 2013. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.
Status:
Investigational
Source:
INN:mespirenone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mespirenone (ZK 94679, 15β,16β-methylene-spironolactone) is a steroid aldosterone antagonist. In addition, it is a quite specific inhibitor of adrenocortical mineralocorticoid synthesis. In rodents mespirenone effectively prevents aldosterone-induced hypertension. It exerts natriuretic efficacy. Although it reached phase II clinical trials, it was discontinued in 1989.
Status:
Investigational
Source:
INN:vindeburnol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Vindeburnol, a derivative of the plant alkaloid vincamine that that bears neuroprotective properties. Animal model for Alzheimer's disease has shown that vindeburnol reduced neuroinflammation and amyloid burden. In addition, the treatment with this drug can be of benefit in multiple sclerosis patients.
Status:
Investigational
Source:
INN:lorpiprazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lorpiprazole (brand name Normarex) is a marketed anxiolytic drug of the phenylpiperazine group. It has been described as a serotonin antagonist and reuptake inhibitor (SARI) in the same group as trazodone, nefazodone, and etoperidone.
Spiroxatrine is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2 adrenergic receptor. Spiroxatrine was identified as a moderately potent but non-selective agonist at the human nociceptin/orphanin FQ receptor, ORL1
Status:
Investigational
Source:
INN:droloxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Droloxifene, a derivative of the triphenylethylene drug tamoxifen, is a novel selective estrogen receptor modulator (SERM). Droloxifene also exhibits more rapid pharmacokinetics, reaching peak concentrations and being eliminated much more rapidly than tamoxifen. Its higher affinity to the estrogen receptor, higher anti-estrogenic to estrogenic ratio, more effective inhibition of cell growth and division in estrogen receptor-positive cell lines, and lower toxicity give it theoretical advantages over tamoxifen in the treatment of human breast cancer. Short-term toxicity was generally mild, and similar to that seen with other antiestrogens. Droloxifene appears active and tolerable. It may have a particular role in situations in which rapid pharmacokinetics, or an increased antiestrogenic to estrogenic ratio, are required. Droloxifene may also be a potentially useful agent for the treatment of postmenopausal osteoporosis because it can prevent estrogen deficiency-induced bone loss without causing uterine hypertrophy. Droloxifene may have an effect on bone and breast tissue because it induces apoptosis. Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.
Status:
Investigational
Source:
INN:coumazoline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Coumazoline is a vasoconstrictor developed as a nasal decongestant by a French corporation Labez. Intravenous administration of the compound to dogs lead to a marked and prolonged drop in the temperature of the gingival mucosa. In rats, coumazoline caused slowing of the dye diffusion on the surface of the skin. The compound did not influence the ciliary motility, as was measured on an isolated guinea pig trachea.
Status:
Investigational
Source:
Int Pharmacopsychiatry. 1978;13(3):138-50.: Not Applicable Human clinical trial Completed Schizophrenia/physiopathology
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Butaclamol is an antipsychotic drug, which was studied for the treatment of schizophrenia. This drug has never marketed and now is used in research, because of its action as a dopamine receptor-blocking agent. Butaclamol consists of the two forms: (-)-butaclamol, an inactive drug and (+)-butaclamol, a potent neuroleptic drug.

Showing 1551 - 1560 of 21518 results