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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 31 - 40 of 161 results

Cocaine is an alkaloid ester extracted from the leaves of plants including coca. Cocaine is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death. Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar which can result in additional toxicity. Following repeated doses, a person may have decreased the ability to feel pleasure and be very physically tired. Cocaine acts by inhibiting the reuptake of serotonin, norepinephrine, and dopamine. This results in greater concentrations of these three neurotransmitters in the brain. It can easily cross the blood-brain barrier and may lead to the breakdown of the barrier.
Diphenhydramine is an antihistamine which is used in the combination with naproxen sodium for the relief of occasional sleeplessness when associated with minor aches and pains. Diphenhydramine has a role nighttime sleep-aid and naproxen sodium is a pain reliever. In addition, diphenhydramine used in relieving symptoms in patients with moderate-to-severe seasonal allergic rhinitis. Diphenhydramine acts as an antagonist of histamine H1 receptor. Besides, was shown potential to repurpose diphenhydramine as an anti-melanoma therapeutic agent, it induces melanoma cell apoptosis by suppressing STAT3/MCL-1 survival signaling pathway.
Status:
Investigational
Source:
NCT04307953: Phase 2 Interventional Recruiting Fibrodysplasia Ossificans Progressiva
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Saracatinib (AZD0530) is an oral, dual inhibitor of c-Src/Abl kinases initially developed by AstraZeneca for the treatment of cancer. The drug was tested for many neoplasms and reached phase III for ovarian cancer (in combination with paclitaxel), however without demonstrating any significant effect. Sarcatinib is also tested in patients with Alzheimer's Disease (Phase II). Its effect on Alzheimer's Disease patients is explained by inhibition of another kinase, Fyn, which is highly expressed in brain.
Status:
Investigational
Source:
NCT03025308: Phase 3 Interventional Active, not recruiting Rheumatoid Arthritis
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Filgotinib (GLPG0634) is a highly selective JAK1 inhibitor. GLPG0634 is a promising drug candidate for the future treatment of autoimmune and inflammatory disorders. It is in phase III clinical trials (initiated mid-2016) for the treatment of rheumatoid arthritis, Crohn's disease and ulcerative colitis. Most common adverse events observed were infections, gastrointestinal disorders and nervous system disorders.
Status:
Investigational
Source:
NCT01038804: Phase 2 Interventional Completed Breast Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sepantronium bromide (YM155) is a selective survivin suppressant that exhibits potent antitumor activities by inducing apoptosis and autophagy in various types of cancer. Sepantronium bromide inhibited the growth of various human cancer cell lines in vitro with GI50 values in the low nM range. Sepantronium bromide blocked the growth of 119 human cancer cell lines, with the greatest inhibition in lines derived from non-Hodgkin's lymphoma, hormone-refractory prostate cancer, ovarian cancer, sarcoma, non-small-cell lung cancer, breast cancer, leukemia, and melanoma, with an average GI50 of 15 nM. Sepantronium bromide inhibited the growth of tumor cell lines regardless of their p53 status and demonstrated significant antitumor activity in 5 mice xenograft models. It also caused tumor regressions in vivo, possibly by its effects in reducing intratumoral survivin expression levels and increasing apoptosis. Sepantronium Bromide had been in phase II clinical trials by Astellas for the treatment of prostate cancer, melanoma, non-Hodgkin's lymphoma, breast cancer, diffuse large B cell lymphoma, non-small cell lung cancer (NSCLC) and other solid tumors. This compound had also been in clinical trials by National Cancer Institute (NCI) for the treatment of solid tumors (phase I) and advanced non-small cell lung cancer (NSCLC) (phase II). However, all these researches about this compound for all indications were discontinued.
Status:
US Previously Marketed
First approved in 1966

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomepromazine (also known as methotrimeprazine) is a phenothiazine neuroleptic drug. It is sold in many countries under the generic name (levomepromazine) or under brand names such as Nozinan, Detenler and many more. Levomepromazine is an antipsychotic drug is commonly used as an antiemetic to alleviate nausea and vomiting in palliative care settings particularly in terminal illness. Levomepromazine is a phenothiazine with pharmacological activity similar to that of both chlorpromazine and promethazine. It has the histamine-antagonist properties of the antihistamines together with central nervous system effects resembling those of chlorpromazine. Levomepromazine's antipsychotic effect is largely due to its antagonism of dopamine receptors in the brain. In addition, it can block 5HT2 receptors and some others, like histamine, serotonin.
Status:
US Previously Marketed
Source:
Chotbyn clihydrogen cit. by Flint
(1945)
Source URL:
First approved in 1945
Source:
Chotbyn clihydrogen cit. by Flint
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


TRICHOLINE CITRATE is indicated for the treatment and management of hepatic disorders and asthma symptoms in adults. It exerts lipotropic action in the hepatic cells. It also can lower the symptoms of asthma and reducing the pro-inflammatory and inflammatory mediators of the leukotriene pathway.
Status:
US Previously Marketed
Source:
Quinine Hypophosphite N.F.
(1921)
Source URL:
First marketed in 1921
Source:
Quinine Hypophosphite N.F.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

QUININE HYPOPHOSPHITE, a salt of quinine, was formerly used, along with the hypophosphites of sodium, potassium, calcium, and iron, in the treatment of phthisis and neurasthenic conditions.
Status:
US Previously Marketed
Source:
21 CFR 310.544(a) smoking deterrent quinine ascorbate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quinine ascorbate is a salt of antimalarial drug quinine and ascorbic acid (vitamin C). Ascorbate reduces the potency of quinolone-containing anti-malarial drugs. Quinine ascorbate was marketed as a component of over-the-counter smoking deterrent products but was not recognized as safe by the FDA regulation in 1993.
Status:
Possibly Marketed Outside US
Source:
Tai Yu Ling Antibacterial Sprays10mL by Weifang Hongyang Pharmacy Co., Ltd.
(2018)
Source URL:
First approved in 2018
Source:
Tai Yu Ling Antibacterial Sprays10mL by Weifang Hongyang Pharmacy Co., Ltd.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Matrine is an active alkaloid, extracted from a traditional Chinese herbs of the Sophora family. Matrine has been reported for its anti-inflammatory and neuroprotective effects. It was demonstrated that the antinociceptive effects of ( )-matrine was mediated by mu- and kappa-opioid receptors. It could dose-dependently restore the balance of Th17/Treg cytokines and attenuate the cognitive impairment in Alzheimer's disease rats. Sophora flavescens and its bioactive compound, matrine alleviated caffeine-induced hyperactivity and promoted non-rapid eye movement sleep by activating ventrolateral preoptic nucleus neurons and modulating serotonergic transmission. Clinical trial results indicate, that intramuscular matrine may be an economical, efficacious, safe drug for the treatment of chronic hepatitis B. Matrine injection may be used to protect the liver function for patients with primary hepatic carcinoma after trans-artery chemo-embolization (TAE), to relieve the liver cells damage, and to improve the tolerance of TAE, so as to perform the next TAE in time.