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

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Showing 5421 - 5430 of 167129 results

Status:
Investigational
Source:
INN:resocortol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Resocortol is a synthetic corticosteroid. Information about current use of this compound is not available.
Status:
Investigational
Source:
INN:pepstatin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pepstatin is a pentapeptide of microbial origin. The peptide inhibits the acid proteases pepsin and cathepsin D and the pressor enzyme renin. Pepstatin was shown to provide long-lasting inhibition (3 to 6 days) of cathepsin D in vivo in non-tumor bearers particularly in spleen, liver, kidney, lung, and heart. Pepstatin may prove useful as "anticachexia" agent by decreasing proteolysis in muscle and other tissues. The in vivo pepstatin and IL-2 treatment decreased the T-cells and increased the natural killer-like LAK precursor cells, possibly also with an increase in its activity, which were further induced by in vitro IL-2 culture to generate an augmented LAK cell activity. This suggests the clinical potential of pepstatin in IL-2-related immunotherapy. In rats injected centrally with the specific cathepsin D inhibitor, pepstatin, the protease activity was inhibited up to 90% in most brain regions.
Status:
Investigational
Source:
INN:tipentosin
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Tipentosin is prazosin derivative. It is an angiotensin-converting enzyme inhibitor. Tipentosin was developed as an antihypertensive agent.
Status:
Investigational
Source:
INN:meglucycline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Meglucycline is an antibiotic.
Status:
Investigational
Source:
INN:tiprenolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tiprenolol (DU21445) has been shown by both in vitro and in vivo animal experiments, to possess strong beta-adrenergic blocking but a relatively less strong negative inotropic activity. The same report also demonstrated by its inhibiting influence on spontaneous mobility of rat uterus, an intrinsic beta-sympathomimetic activity. Tiprenolol reveals effects similar to propranolol. Tiprenolol was shown to have significantly less heart rate slowing effect at rest than propranolol. However, all other measurements failed to show any difference of statistical significance between the two drugs with respect to any negative inotropic or beta‐blocking activity. The administration of tiprenolol or propranolol depressed the arterial pressure and caused the deaths of some dogs in which a coronary artery had been ligated.
Status:
Investigational
Source:
NCT02376309: Not Applicable Interventional Completed Muscle Atrophy
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:trefentanil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trefentanil is a short-acting synthetic opioid of the piperidine class. The drug caused potent analgesia with the peak effect occurring 3 min after injection. There was no significant difference in analgesic potency of trefentanil and alfentanil as measured by tolerance to tibial pressure at 3 min. Trefentanil had a pharmacokinetic and pharmacodynamic profile similar to alfentanil, with a small extent of tissue distribution and a rapid blood/brain equilibration. Trefentanil caused significant respiratory depression at doses of 32 ug/kg and 64 ug/kg. It is a mu-opioid receptor agonist. Trefentanil produced naloxone reversible anti-nociception equi-efficacious to that of fentanyl.
Status:
Investigational
Source:
INN:trioxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trioxifene (LY133314) is a selective estrogen receptor modulator (SERM) with competitive binding activity against estradiol for estrogen receptor alpha (ERalpha) and antagonistic activity against ERalpha-mediated gene expression. Trioxifene has demonstrated activity in dimethyl-benzanthracene-induced mammary carcinoma in rats and human breast cancer patients. Trioxifene mesylate, an antiestrogen with a high FR affinity, was developed with the hope of improving the response rate of ER-positive patients, especially those with a borderline concentration of ER in their tumors. When used in vitro and in vivo, trioxifene has been shown to bind to the estradiol receptors with a binding affinity exceeding that of estradiol by a factor 1.7, whereas tamoxifen has a relative affinity of only 0.18 compared with trioxifene.
Status:
Investigational
Source:
NCT02249403: Phase 2 Interventional Completed Alzheimer Disease
(1999)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.
Status:
Investigational
Source:
INN:tigemonam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.

Showing 5421 - 5430 of 167129 results