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

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Showing 471 - 480 of 1447 results

Nickel (II) oxide is an olive gray powder, insoluble in water and soluble in acids. It is produced industrially and used mainly as an intermediate in the production of nickel alloys and as a hydrogenation catalyst. Long-term inhalation of NiO is damaging to the lungs, causing lesions and in some cases cancer.
Status:
US Approved Allergenic Extract (1994)

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bronopol is used as a preservative in various cosmetic, pharmaceutical, toiletry and household preparations at concentrations of up to 0.1% (wt/vol) particularly because of its high activity against Gram-negative bacteria, especially Pseudomonas aeruginosa and other pseudomonad. Bronopol hydrolyzes within 3 h at 60 °C and pH 8, producing formaldehyde, nitrosamines, and other molecules. Although the parent compound (bronopol) is rather short-lived in the environment, its degradation products are toxic and more persistent. The protection against the bactericidal activity of bronopol afforded by catalase or superoxide dismutase suggests that the activity stems from the aerobic interaction and the generation of active oxygen species from oxygen diffusing into the suspensions during bronopol treatment. The acute oral LD50 was 307 mg/kg for rat males and 342 mg/kg for females. Bronopol is moderately toxic by the oral route. Results from an acute dermal toxicity study while inadequate, suggest bronopol is highly toxic by the dermal route.
Clove oil is a natural product, derived from the Eugenia caryophyllata tree. Clove oil is 85 to 95% eugenol. Isoeugenol and methyleugenol make up 5 to 15% of the remaining ingredients. Isoeugenol is manufactured from eugenol by a process of isomerization. Isoeugenol have been used in foods and eugenol has been used in animal feeds. Isoeugenol is used as a fish anesthetic. The mechanism of action of isoeugenol in fish has not been determined. It is hypothesised that its effects are mediated via receptors controlling cellular ion channels in a similar way to that described for local anaesthetics. Reports of adverse reactions involving the use of isoeugenol in humans are primarily confined to incidents of contact sensitization or allergy following dermal exposure.
Imidurea (Imidazolidinyl urea) is used as an antimicrobial agent and preservative in cosmetics and toiletries. It is very active against gram and gram- bacteria as a synergist in combination with parabens. Imidazolidinyl urea is more active against bacteria than fungi and is often combined with parabens to provide a broad spectrum preservative system. This preservative is one of the most widely used preservative systems in the world. The Food and Drug Administration (FDA) considers imidazolidinyl urea as one of the most common antimicrobial agents used in cosmetics. Due to its high water solubility, imidazolidinyl urea can be incorporated into almost all water-based cosmetics, toiletries, and cold mix formulations. It is present in a wide range of liquid and powder products such as baby lotion, skin cream, sunscreens, shampoos, eyeliners, blush, perfumes, deodorants, hair dyes, shaving cream, and face masks. Imidazolidinyl urea is permitted for use in personal care products in the European Union at a maximum concentration of 0.6%. In Japan, imidazolidinyl urea is allowed in rinse-off cosmetics such as shampoo, body wash, and facial cleanser at a maximum concentration of 0.3%. Imidurea is an ingredient of FDA-approved NIZORAL® (ketoconazole) 2% Shampoo, indicated for the treatment of tinea (pityriasis) versicolor caused by or presumed to be caused by Pityrosporum orbiculare (also known as Malassezia furfur or M. orbiculare).
Status:
US Previously Marketed
First approved in 2019

Class (Stereo):
CHEMICAL (ACHIRAL)



Diphencyprone (DPCP) is a potent topical sensitizing agent that has been used since the late 1970s by physicians for the treatment of alopecia areata (AA), viral warts (human papillomavirus) and cutaneous metastases of melanoma. Although to date the compound is not approved as a drug by the FDA or EMA, physicians have continued to use DPCP because of its proven effects in these dermatological conditions. Diphenylcyclopropenone acts as a local irritant, triggering a local sensitization. It triggers an immune response that opposes the action of the autoreactive cells that otherwise cause hair loss. The efficacy of DPCP has generally been ascribed to immunological reactions by the host. Inducing inflammation with a contact sensitizer is counterintuitive to treating AA, an autoimmune disorder. Studies using microarray and miRNA profiling may provide information about how DPCP induces inflammation in human skin at different times. Gene targets and microRNAs identified through these data may be modulated by an RNA interference approach to enhance DPCP efficacy and response rates
Status:
US Previously Marketed
Source:
INGENOL MEBUTATE by PADAGIS ISRAEL
(2019)
Source URL:
First approved in 2012

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ingenol is an extremely weak PKC (protein kinase C) activator, with potent anticancer activity. Ingenol derivatives have received constant and multidisciplinary attention on account of their pleiotropic pattern of biological activity. This includes activation of PKC (protein kinase C), tumor-promotion, anticancer, and anti-HIV properties, and the possibility of dissecting co-cancerogenic and clinically useful activities has been demonstrated. Certain ingenol esters show powerful anticancer activity, and a structure-activity relationship model to discriminate between their apoptotic and non-apoptotic properties has been developed.
Status:
US Previously Marketed
First approved in 2011

Class (Stereo):
CHEMICAL (ACHIRAL)



Ezogabine (U.S. adopted name) or retigabine (international nonproprietary name) is one of a family of aminopyrroles with anticonvulsant activity. It is used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. The drug was approved by the European Medicines Agency under the trade name Trobalt and by the United States Food and Drug Administration (FDA), under the trade name Potiga. The mechanism by which ezogabine exerts its therapeutic effects has not been fully elucidated. In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability. This mechanism of action is unique among antiepileptic drugs, and may hold promise for the treatment of other neurologic conditions, including migraine, tinnitus and neuropathic pain. In vitro studies suggest that ezogabine may also exert therapeutic effects through augmentation of GABA-mediated currents.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(24)(i) menstrual/diuretic ethyl nitrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ethyl nitrate is an inhaled organic nitrate that affects pulmonary vascular tone and may be used as a possible treatment for persistent pulmonary hypertension of the newborn. Ethyl nitrate acts by generating NO, which activates soluble guanylate cyclase to increase intracellular cyclic GMP. This, in turn, leads to a decrease in intracellular calcium and relaxation of the vascular smooth muscle.
Cholesterol is a sterol (a combination steroid and alcohol) and a lipid found in the cell membranes of all body tissues, and transported in the blood plasma of all animals. The high level of cholesterol in the blood is a marker of hypercholesterolemia, also called dyslipidemia. As a part of homeopathic product, it helps to support general liver and gallbladder health, and is used for temporary relief of symptoms related to adrenal glands such as fatigue and low energy. Cholesterol binds to and affects the gating of a number of ion channels such as the nicotinic acetylcholine receptor (nAChR) Inwardly-rectifying K+ channels (Kir); Transient receptor potential vanilloid 1 channels (TRPV1) and Large-conductance Ca2+-sensitive voltage-gated K+ channels (BK). It was shown the new mechanistic insights into the role of cholesterol in the regulation of nAChR, showing that cholesterol regulates the channels by two distinct mechanisms: stabilization of the channels in a resting state that depends on specific lipid-protein interactions and facilitation of the transitions between uncoupled and coupled states that depends on the hydrophobic thickness of the membrane
Status:
US Previously Marketed
First approved in 1976

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Prazepam is a benzodiazepine derivative and is indicated to treat symptoms of anxiety. Benzodiazepines are used to treat severe incapacitating symptoms or symptoms leading to an extreme suffering for the patient. Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation. Prazepam is a prodrug for N-desmethyl-diazepam, which is responsible for the therapeutic effects of prazepam. Prazepam was discontinued in USA.