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

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Showing 61 - 70 of 1990 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Quinpirole (LY 171,555) is a psychoactive drug and research chemical which acts as a selective D2 and D3 receptor agonist. Quinpirole is the most widely used D2 agonist in in vivo and in vitro studies. Specific quinpirole binding in rat brain was saturable, and dependent on temperature, membrane concentration, sodium concentration and guanine nucleotides. Saturation analysis revealed high affinity binding characteristics (KD = 2.3 nM) which were confirmed by association-dissociation kinetics. The regional distribution of [3H]quinpirole binding sites roughly paralleled the distribution of [3H]spiperone binding sites, with greatest densities present in the striatum, nucleus accumbens and olfactory tubercles. A variety of drugs, most notably monoamine oxidase inhibitors (MAOls), inhibit the binding of [3H]quinpirole, but not [3H]spiperone or [3H](-)N-n-Propylnorapomorphine, in rat striatal membranes by a mechanism that does not appear to involve the enzymatic activity of MAO. Clinically antidepressant MAOIs exhibited selectivity between sites labeled by [3H]quinpirole and [3H]spiperone as did a number of structurally related propargylamines and N-acylethylenediamine derivatives and other drugs such as debrisoquin and phenylbiguanide. Quinpirole has been shown to increase locomotion and sniffing behavior in mice and induces compulsive behavior symptomatic of obsessive compulsive disorder in rats.
Status:
Investigational
Source:
INN:iprocrolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

IPROCROLOL is a beta-adrenoceptor antagonist with antiarrhythmic properties.
Status:
Investigational
Source:
INN:teloxantrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Teloxantrone (also known as DuP 937) was developed as an anthrapyrazole intercalator that inhibits DNA synthesis. Teloxantrone interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis. The drug participated in phase II clinical trials in colorectal carcinoma, in non-small cell lung cancer, in metastatic malignant melanoma. However, these studied apparently were discontinued.
Status:
Investigational
Source:
USAN:Amikhelline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Amikhellin (AK), an antimitotic drug, is a synthetic water-soluble derivative of khellin, an alkaloid extracted from seeds of Ammi Visnaga. Amikhellin has been used so far mostly as a vasodiator. Amikhellin binds to double-stranded DNA by an intercalation process. It inhibits the DNA-polymerase from murine sarcoma leukemia virus.
Status:
Investigational
Source:
INN:ciclosidomine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ciclosidomine is morpholine derivative and nitric oxide donors developed for vascular diseases treatment.
Status:
Investigational
Source:
INN:pazelliptine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pazelliptine (previously known as BD 40 or SR 95225A) was developed as an antitumor drug that binds to the DNA sequence, preferable to G-C rich region and thus produces cellular DNA lesions. This drug was undergoing phase II trials in France for the treatment of cancer. However, this study was discontinued.
Status:
Investigational
Source:
INN:fenbenicillin
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Fenbenicillin (phenoxybenzylpenicillin) is an acid-stable, orally active penicillin. Fenbenicillin demonstrated antibacterial activity in patients suffering from streptococcal, pneumococcal, and penicillin-sensitive staphylococcal infections.
Status:
Investigational
Source:
Ann Thorac Surg. Oct 2022;114(4):1468-1474.: Not Applicable Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


S-nitrosoglutathione (GSNO) is an endogenous S-nitrosothiol that acts as a NO pool. The level of GSNO is tightly regulated by S-nitrosoglutathione reductase (GSNOR), an enzyme that degrades GSNO. GSNOR inhibitors offer a potentially promising option for the management of pre-eclampsia, a cause of maternal death and of perinatal morbidity. The GSNO treatment of traumatic brain injury improved neurobehavioral functions. GSNO can increase the expression of certain proteins at concentrations present in the normal human airway. GSNO has an important role in regulating respiratory function (breathing) and preventing inflammation in the respiratory tract, that is why this compound participated in phase I clinical trials for patients with asthma. In addition, GSNO was studied in the cystic fibrosis airway. The obtained results have shown that GSNO replacement therapy could be an effective treatment. In addition, GSNO was investigated for patients with chronic obstructive pulmonary disease.
Status:
Investigational
Source:
INN:miloxacin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Miloxacin, an antibacterial agent that was used in veterinary. This drug was also studied for the treatment of acute intestinitis. Experiments in vitro have shown that this compound exhibited significant activities against Escherichia coli, Klebsiella pneumonia, Proteus mirabilis, Proteus vulgaris, and less active against a Pseudomonas aeruginosa infection and inactive at the maximum test doses against a Streptococcus pyogenes infection. Information about the current use of miloxacin is not available.
Status:
Investigational
Source:
INN:valdipromide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Valdipromide is an antidepressant.