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

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Showing 361 - 370 of 13268 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fasobegron is an agonist of β3-adrenoreceptor.
Status:
Investigational
Source:
INN:inakalant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Inakalant is diazabicyclo[3.3.1]nonane derivative patented by pharmaceutical company AstraZeneca AB as antiarrhythmic agent.
Status:
Investigational
Source:
INN:clodacaine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Clodacaine is a local anesthetic drug, invented by Cilag AG in the late 1950s.
Status:
Investigational
Source:
INN:nafazatrom [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nafazatrom [BAY G 6575] is a leukotriene synthesis inhibitor that was being developed by Bayer in Germany. It is a pyrazolinone derivative with potential antimetastatic activities. Nafazatrom, originally developed as an antithrombotic agent, inhibits the key prostaglandin catabolic enzyme, 15-hydroxyprostaglandin dehydrogenase, which prolongs the biological half-life of prostacyclin (prostaglandin I2; PGI2) and prevents intravascular coagulation. Nafazatrom, in the micromolar range, inhibits the metabolism of PGs (prostaglandins) by 15-OH PGDH in a dose-dependent manner. The IC50 for inhibition of 15-OH PGDH was estimated to be 18.5 uM when [3H]PGF2 alpha was used as substrate. This agent also serves as a reducing cofactor with the hydroperoxidase moiety of cyclooxygenase and accelerates the conversion of arachidonic acid into precursors of PGI2. An elevated level of PGI2 prevents aggregation of platelets; subsequently it decreases the formation of tumor cell-platelet aggregates as well as their sequestration in blood vessels, which is an important initiating step in the development of metastasis. Nafazatrom may have had potential as an antithrombotic, anti-ischaemic and antiasthmatic agent. However, the development of nafazatrom was discontinued.
Status:
Investigational
Source:
INN:minepentate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Minepentate was developed as an antiparkinsonian drug. However, it has never been marketed.
Pamicogrel is a cyclooxygenase inhibitor with platelet anti-aggregatory properties which is under development by Kanebo for chronic arterial occlusion. It also has potential in both prophylaxis and treatment of ischemic brain injury. An NDA was submitted in Japan in April 1997. The effects of the drug on platelet aggregation were originally disclosed in EP-00159677, while the later European patent, EP-00560136, claims its use in brain dysfunction induced by hypoxia arising from disturbance of cerebral circulation, such as cerebral hemorrhage or cerebral infarction.
Status:
Investigational
Source:
INN:itrocinonide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ITROCINONIDE is a synthetic corticosteroid which showed no signs of systemic activity (cortisol depression).
Status:
Investigational
Source:
INN:pinolcaine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.
Status:
Investigational
Source:
INN:mivobulin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity
Status:
Investigational
Source:
INN:lorapride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lorapride is a centrally acting sulfonamide. It has pharmacodynamic properties that are mainly related to ulcer treatment. On the basis of its psychopharmacologic profile, it has no neuroleptic potential, but it does exhibit some psychostimulating components. After oral administration, absorption of lorapride was rapid. The rate of absorption was first order for solution and zero order for capsule.