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

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Showing 10711 - 10720 of 12523 results

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

Class (Stereo):
CHEMICAL (UNKNOWN)


FLUMECINOL, a benzhydrol derivative, is a hepatic microsomal drug-metabolizing enzyme inducer. It was in clinical development for the treatment of pruritus associated with primary biliary cirrhosis.
Status:
Investigational
Source:
INN:morpheridine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Morpheridine is a pethidine analog with strong analgesic activity. Morpheridine does not cause convulsions, although it produces the standard opioid side effects such as sedation and respiratory depression. Morpheridine is not currently used in medicine and is a Schedule I drug which is controlled under United Nations drug conventions.
Status:
Investigational
Source:
INN:furethidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.
Status:
Investigational
Source:
NCT00243230: Phase 2 Interventional Completed HIV Infections
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Vicriviroc or SCH 417690 is a potent and selective antagonist of the CCR5 receptor. vicriviroc binds specifically to the CCR5 receptor and prevents infection of target cells by CCR5-tropic HIV-1 isolates. In antiviral assays, vicriviroc showed potent, broad-spectrum activity against genetically diverse and drug-resistant HIV-1 isolates and was consistently more active than SCH-C in inhibiting viral replication. This compound demonstrated synergistic anti-HIV activity in combination with drugs from all other classes of approved antiretrovirals. Competition binding assays revealed that vicriviroc binds with higher affinity to CCR5 than SCH-C. Functional assays, including inhibition of calcium flux, guanosine 5'-[35S]triphosphate exchange, and chemotaxis, confirmed that vicriviroc acts as a receptor antagonist by inhibiting signaling of CCR5 by chemokines. Finally, vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects. Vicriviroc represented a promising new candidate for the treatment of HIV-1 infection. Vicriviroc for HIV treatment was previously in Phase III studies but has since been discontinued.
Status:
Investigational
Source:
INN:levdobutamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levdobutamine is a beta-adrenoceptor agonist selective for the beta1-subtype. Levdobutamine was derived from dopamine. It is the active (S)-isomer of dobutamine. It is the cardiotonic agent.
Status:
Investigational
Source:
INN:levdobutamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levdobutamine is a beta-adrenoceptor agonist selective for the beta1-subtype. Levdobutamine was derived from dopamine. It is the active (S)-isomer of dobutamine. It is the cardiotonic agent.
Status:
Investigational
Source:
INN:levdobutamine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levdobutamine is a beta-adrenoceptor agonist selective for the beta1-subtype. Levdobutamine was derived from dopamine. It is the active (S)-isomer of dobutamine. It is the cardiotonic agent.
Status:
Investigational
Source:
NCT00832546: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
Status:
Investigational
Source:
INN:dagapamil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.
Status:
Investigational
Source:
NCT01423851: Phase 1/Phase 2 Interventional Completed Primary Myelofibrosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


NS-018 is a potent inhibitor of Janus kinase 2 (JAK2) enzyme activity and Src-family kinases. It was developed as an oral therapy for the treatment of myelofibrosis. Overall NS-018 has been used in trials studying the treatment of primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia. NS-018 is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). NS-018 also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene.

Showing 10711 - 10720 of 12523 results