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

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Showing 71 - 80 of 209 results

Vanillin (4-hydroxy-3-methoxybenzaldehyde), a pleasant smelling organic aromatic compound, is widely used as a flavoring additive in food, beverage, cosmetic and drug industries. It is reported to cross the blood brain barrier and also displayed antioxidant and neuroprotective activities. Vanillin is a natural substance widely found in many plant species and often used in beverages, foods, cosmetics, and pharmaceutical products. Antioxidant and anticancer potential have been described for this compound. Vanillin has been classified as a bioantimutagen and is able to inhibit mutagenesis induced by chemical and physical mutagens in various cell systems. Vanillin, a selective agonist of TRPV1, has been shown to attenuate i.c.v. STZ and AlCl3+d-galactose induced experimental Alzheime's disease (AD).
Status:
US Previously Marketed
Source:
Physostigmine Salicylate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Physostigmine Salicylate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Physostigmine (Phy) is one of the oldest drug isolated from Calabar beans and successfully used for the treatment of glaucoma in 1864. Since then, it has been widely employed for various therapeutic purposes. Recently, it has gained prominence because of its clinical trials in the treatment of Alzheimer's disease. Physostigmine was used to treat glaucoma. It can be applied topically to the conjunctiva. Phy is also considered to be a potent prophylactic antidote for organophosphate poisoning. It is a reversible cholinesterase (ChE) inhibitor and has a short duration of action. For the last 50 years, numerous authors have shown that pretreatment with Phy would rapidly improve the incapacitating effects of organophosphate intoxication in various animal species. Phy carbamylates to a portion of ChE enzyme and thus protects the enzyme from binding with organophosphate, which are irreversible ChE inhibitors. The carbamylated ChE enzyme decarbamylates to free the enzyme for normal functioning. The rates of decarbamylation of butyrylcholinesterase (BuChE) in plasma and ChE in brain and muscle are different and are related to the half-life of Phy in these tissues. In addition to ChE inhibition, Phy has a direct action on acetylcholine (ACh) receptor ionophore complex by interacting with the ACh-gated cation channels. A cholinesterase inhibitor that is rapidly absorbed through membranes. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.
Vasicinone is a quinazoline alkaloid. Hepatoprotective activity of vasicinone has being shown in mice. Pre-treatment with vasicinone and silymarin (25 mg/kg/day for 7 days) significantly decreased CCl4-induced increase in SGOT, SGPT, ALP levels. Vasicinone has shown cytotoxic and antiproliferative activity in several tumor cell lines. Vasicinone, an oxidation product of vascinine is a potent bronchodialator. Vasicinone could be utilised in alternate anti asthmatic therapy, since it plays a vital role in scavenging Nitric oxide which could prevent the bronchial inflammation in asthmatic patients.
Status:
Possibly Marketed Outside US
First approved in 2017

Class (Stereo):
CHEMICAL (RACEMIC)


Fenamiphos is an organophosphate insecticide and nematicide used for the control of nematodes and sucking insects (including aphids and thrips) on food and non-food crops, and for the control of nematodes in the turf. Fenamiphos blocks the enzyme acetylcholinesterase in the target pests. Fenamiphos is a highly toxic poison that acts by inhibiting cholinesterase (ChE) enzymes in the blood and central and peripheral nervous systems. Inhibition of plasma cholinesterase activity is the most sensitive toxicological endpoint in acute and short-term studies on experimental animals. Fenamiphos is applied on a variety of plants such as tobacco, turf, bananas, pineapples, citrus, and other fruit vines, some vegetables, and grains. In Brazil, this pesticide has been extensively used in tomato crop at planting and also in melon.
Alpha-terpineol is a monoterpene found in the essential oils of several aromatic plant species. It has an anti-inflammatory and antioxidant effects. alpha-Terpineol is a fragrance ingredient used in decorative cosmetics, fine fragrances, shampoos, toilet soaps, and other toiletries as well as in non-cosmetic products such as household cleaners and detergents. alpha-Terpineol was approved by the FDA as a flavor.
Palmatine is a protoberberine alkaloid. Palmatine is major component of herbal preparations mainly used in traditional medicine Chinese, Korean and Indian. Palmatine can be found in various medicinal plants such as Coptis chinensis, Rhizoma coptidis, Corydalis yanhusuo, Radix tinosporae, among others. It exerts diverse pharmacological and biological properties. Palmatine has been proposed as a promising DNA phototherapy drug, notably due to its ability to produce in situ singlet oxygen only when interacting with DNA.
Imidocarb is a carbanilide derivative with antiprotozoal activity. It is usually administered as the dipropionate salt. Imidocarb is a drug sold under the brand name Imizol and is used to treat canine ehrlichiosis. wo mechanisms of action have been proposed: As the effect of imidocarb on Trypanosoma brucei is antagonized by excess polyamines, it is has been suggested that imidocarb interferes with their production and/or use. Imidocarb blocks the entry of inositol into erythrocytes containing Babesia, resulting in starvation of the parasite. It is generally accepted in that imidocarb has anticholinesterase activity.
Status:
Possibly Marketed Outside US
Source:
Carylderm by Union Carbide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Carbaryl (1-naphthyl methylcarbamate) is a chemical in the carbamate family used chiefly as an insecticide. It is a white crystalline solid commonly sold under the brand name Sevin, a trademark of the Bayer Company.Union Carbide discovered carbaryl and introduced it commercially in 1958. Bayer purchased Aventis CropScience in 2002, a company that included Union Carbide pesticide operations. It remains the third-most-used insecticide in the United States for home gardens, commercial agriculture, and forestry and rangeland protection. As a veterinary drug, it is known as carbaril. Carbaryl is an anticholinesterase inhibitor. It is indicated for the treatment of head and pubic lice. It is available as a lotion (Carylderm) and a shampoo (Carylderm; New Suleo; Derbac). Carbaryl was developed because lice began to show resistance to organochlorine insecticides such as DDT and gamma benzene hexachloride (Quellada; Lorexane). It was introduced in the late 1960s particularly for the control of head lice; it is less effective against mites, and not recommended for scabies.
Status:
Possibly Marketed Outside US
Source:
GENESERINE by Eber
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Eseridine (Geneserine) has been known for many years as an anticholinergic agent and used in therapy as a gastrointestinal antispastic. Eseridine salicylate is an inhibitor of cholinesterase activity that has been given by mouth in preparations for dyspepsia and other gastric disorders. It has also been studied for the treatment of Alzheimer’s disease.
Dichlorvos is a synthetic organic chemical used as an insecticide. Dichlorvos does not occur naturally in the environment, but is manufactured by industry. Dichlorvos is sold under many trade names including Vapona®, Atgard®, Nuvan®, and Task®. It is also used as an insecticide for slow release on pest-strips for pest control in homes.  Dichlorvos is used as an anthelmintic (worming agent) for dogs, swine, and horses, as a botacide (agent that kills fly larvae) for horses, and in flea collars for dogs. In 1995, EPA proposed cancellation of dichlorvos for all home uses, and for many commercial and industrial uses.