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

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Showing 301 - 310 of 1040 results

Status:
US Previously Marketed
Source:
GUANIDINE HYDROCHLORIDE by MERCK SHARP DOHME
(1939)
Source URL:
First approved in 1939
Source:
GUANIDINE HYDROCHLORIDE by MERCK SHARP DOHME
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Guanidine is a small basic compound. Guanidine stimulates the neuromuscular junction presynaptically by inhibiting voltage-gated potassium (Kv) channels, leading to the enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases. The hydrochloride salt of guanidine was approved by FDA for the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert.
Oleic acid is an unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. Oleic acid occurs naturally in various animal and vegetable fats and oils. It is a component of the normal human diet as a part of animal fats and vegetable oils. Oleic acid may be responsible for the hypotensive (blood pressure reducing) effects of olive oil. Oleic acid has being shown to have a potential anticancer activity.
Status:
US Previously Marketed
Source:
RUTIN RUTIN by ABBOTT
(1961)
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rutin, also called rutoside, is the glycoside flavonoid found in a certain fruits and vegetables. Most rutine-rich foods are capers, olives, buckwheat (whole grain flour), asparagus, raspberry.In a clinical trial, rutin was found to aid control of intraocular pressure in patients with primary open angle glaucoma. As a component of dietary supplement Phlogenzym, rutin is used for treatment of osteoarthritis. Rutin is also used for treatment of post-surgical swelling of the arm after breast cancer surgery. Traditionally, rutin is used to prevent mucositis due to cancer treatment, to treat blood vessel disease such as varicose veins, bleeding, hemorrhoids.
Status:
US Previously Marketed
Source:
Strontium Bromide U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Strontium Bromide U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Strontium ranelate is composed of an organic moiety (ranelic acid) and of two atoms of stable nonradioactive strontium. In vitro, strontium ranelate increases collagen and noncollagenic proteins synthesis by mature osteoblast enriched cells. The effects of strontium ranelate on bone formation were confirmed as strontium ranelate enhanced pre-osteoblastic cell replication. The stimulation by strontium ranelate of the replication of osteoprogenitor cell and collagen, as well as noncollagenic protein synthesis in osteoblasts, provides substantial evidence to categorize strontium ranelate as a bone-forming agent. In the isolated rat osteoclast assay, a pre-incubation of bone slices with strontium ranelate induced a dose- dependent inhibition of the bone resorbing activity of treated rat osteoclast. Strontium ranelate also dose-dependently inhibited, in a chicken bone marrow culture, the expression of both carbonic anhydrase II and the alpha-subunit of the vitronectin receptor. These effects showing that strontium ranelate significantly affects bone resorption due to a direct and/or matrix-mediated inhibition of osteoclast activity and also inhibits osteoclasts differentiation, are compatible with the profile of an anti-resorptive drug. Pharmacological and clinical studies suggest that strontium ranelate optimizes bone resorption and bone formation, resulting in increased bone mass, which may be of great value in the treatment of osteoporosis. Strontium ranelate is approved by EMA for the treatment of severe osteoporosis in postmenopausal women and in adult men.
Status:
US Previously Marketed
Source:
Solution of Formaldehyde U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Solution of Formaldehyde U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Formaldehyde is a naturally occurring organic compound, and an important industrial precursor to many other materials and organic compounds. Formaldehyde solution (formalin) is used as a disinfectant. Formaldehyde vapors are toxic, upon entry formaldehyde reacts readily with macromolecules, including DNA to form DNA-protein and DNA-DNA cross-links.
Status:
US Previously Marketed
Source:
Sugar U.S.P.
(1921)
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Sucrose is a disaccharide composed of glucose and fructose, and found in many plants and plant parts. Sucrose is often extracted and refined from either sugarcane or beet sugar for human consumption. Upon ingestion, sucrose is hydrolyzed in the small intestine by by sucrase to glucose and fructose. Sucrose is used as inactive ingredients in numerous drugs. In medicine, sucrose is used for pain relief in infants.
Status:
US Previously Marketed
Source:
Quinine Salicylate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Quinine Salicylate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Quinine soluble salts possess an extremely bitter taste, that may have a perplexing problem especially to children. That is why one of the most common combinations for oral administration is a slightly soluble quinine salicylate salt. It is known that now quinine is used in the absence of artemisin combination therapies (ARTs) to treat CQ resistant (CQR) P. falciparum malaria. Although the precise mechanism of the antimalarial activity of quinine is not completely understood, it can act via the inhibition on nucleic acid synthesis, on protein synthesis, and on glycolysis in Plasmodium falciparum, and also drug can affect via the binding with hemazoin in parasitized erythrocytes.
Phenylmercuric ammonium acetate is a fungicide and bactericide. It is used for the seed treatment.
Status:
US Previously Marketed
Source:
Eumydrin by Bayer
(1911)
Source URL:
First marketed in 1911
Source:
Eumydrin by Bayer
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Methylatropine (methylatroponium) is a belladonna derivative. In 1902 the Bayer Company introduced atropine methonitrate, a quaternary ammonium salt of atropine (Eumydrin), as a mydriatic for dilation of the pupil during ophthalmic examination. Due to its highly polar nature it penetrates less readily into the central nervous system than atropine and was therefore introduced for relieving pyloric spasms in infants. Atropine methyl nitrate is a muscarinic acetylcholine receptor antagonist that does not cross the blood-brain barrier. Atropine methyl nitrate has been used for its peripheral muscarinic effects (targeting the bladder, respiratory tract, and to block parasympathetic signaling to the heart, among others) and to separate central from peripheral nervous system effects, or to protect against peripheral side effects when using muscarinics that do cross the blood brain barrier.
Leonurine (LN) is a natural alkaloid extracted from Herba leonuri which is used in Chinese traditional medicine and possesses anti-inflammatory properties. Leonurine has potential as a therapeutic agent for rheumatoid arthritis and might be a promising therapeutic compound to treat osteoclast-related diseases, such as osteoporosis. These effects are achieved through the inhibition of NF-κB and mitogen-activated protein kinase pathways. In addition, it was found that leonurine protects BBB integrity by regulating the HDAC4/NOX4/MMP-9 tight junction pathway and could therfeore represent a new class of potential drugs against the acute onset of ischemic stroke. In experiments on mice with adenomyosis leonurine attenuated generalized hyperalgesia, however, the mechanism responsible for alleviating pain was not readily apparent.