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

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Showing 431 - 440 of 4343 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:odalprofen
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Odalprofen was used as an analgesic. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT02764385: Not Applicable Interventional Completed Smoking
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01051635: Phase 1 Interventional Completed Neoplasms
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Indimitecan, also known as LMP776, is a novel topoisomerase I inhibitor. A substance being studied in the treatment of cancer. It blocks certain enzymes that break and rejoin DNA strands. These enzymes are needed for cells to divide and grow. Blocking them may cause cancer cells to die. Indimitecan (LMP776) also helps anticancer drugs kill cancers that are resistant to some other drugs. LMP776 is a type of indenoisoquinoline and a type of topoisomerase inhibitor. In vitro, LMP776 induces TOP 1 cleavage at unique genomic positions and causes cell cycle arrest in both S and G (2)-M phases. Protein linked DNA breaks were observed in cells treated with nanomolar concentrations of LMP776.
Status:
Investigational
Source:
INN:clonitazene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Clonitazene is a synthetic opioid analgesic, structurally related to etonitazene. In the USA clonitazene is a schedule I narcotic controlled substance.
Status:
Investigational
Source:
INN:piclozotan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Piclozotan (SUN N4057) is a 1,4-benzoxazepine derivative that exhibits sub-nanomolar affinity at serotonin 1A receptor with good selectivity over dopamine D2 and α1-adrenoceptors. Piclozotan reduced levodopa-induced forelimb hyperkinesia by 55% and 69%, respectively, at 1h relative to the control. Piclozotan significantly lengthened the duration of rotational behavior by 26% versus the control and attenuated the increase in striatal levodopa-derived extracellular dopamine levels. Piclozotan, a serotonin 1A agonist, can improve motor complications in patients with advanced Parkinson's disease. Piclozotan has been shown to be neuroprotective against ischemic neuronal damage in animal models. Piclozotan had been in phase II for the treatment of stroke. However, this research has been discontinued.
Status:
Investigational
Source:
INN:hydroxypethidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Hydroxypethidine, an opioid analgesic is an opioid receptor agonist. Hydroxypethidine is under the control of narcotic drugs according to US Single Convention 1961.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.
Status:
Investigational
Source:
INN:froxiprost
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Froxiprost (ONO-995), a synthetic analog of dinoprost, is a prostanoid receptor agonist. Froxiprost is active in contracting the uterine smooth muscle and is used as a pharmacological tool.
Status:
Investigational
Source:
NCT03194620: Not Applicable Interventional Completed Healthy
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

(-)-Epigallocatechin is a polyphenol, which occurs naturally in various plants, including green tea leaves. The compound was shown to have anti-cancer activity in vitro, with breast cancer, lung cancer, and colon cancer cells. The commercial preparation of Polyphenon E contains about 3% (-)-epigallocatechin as an impurity.