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

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Showing 481 - 490 of 1447 results

Leucine is an α-amino acid used in the biosynthesis of proteins. Leucine is an essential hydrophobic amino acid. It is used in the Leucine may be used some people as a supplement to build muscle. Leucine is also found in fish, meat, and poultry. In the pharmaceutical industry, L-leucine is used for parenteral and enteral nutrition and feeding, and is also used as a flavoring product and tablet lubricant in manufacturing. Leucine is an mTOR activator. It is a dietary amino acid with the capacity to directly stimulate muscle protein synthesis. As a dietary supplement, leucine has been found to slow the degradation of muscle tissue by increasing the synthesis of muscle proteins in aged rats. Long-term leucine supplementation does not increase muscle mass or strength in healthy elderly men. Leucine potently activates the mammalian target of rapamycin kinase that regulates cell growth. Infusion of leucine into the rat brain has been shown to decrease food intake and body weight via activation of the mTOR pathway.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control isoleucine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Isoleucine is an essential α-amino acid that is used in the biosynthesis of proteins. L-isoleucine is commonly used in parenteral and enteral nutrition. It is used in combination with the other branched chain amino acids to improve the nutritional status of patients with hepatic diseases. BCAAs serve as important fuel sources for skeletal muscle during periods of metabolic stress
Status:
US Previously Marketed
Source:
Copoietin Ferrous by Lloyd Bros. (Hoechst-Roussel)
(1963)
Source URL:
First approved in 1963
Source:
Copoietin Ferrous by Lloyd Bros. (Hoechst-Roussel)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dicobalt edetate was developed as a cyanide antidote based on the known ability of cobalt to form stable complexes with cyanide. One current cobalt-based antidote available in Europe is dicobalt-EDTA, sold as Kelocyanor. This agent chelates cyanide as the cobalticyanide. This drug provides an antidote effect more quickly than formation of methemoglobin. It can be very toxic and cause seizures, upper airway oedema, chest pain, hypotension, vomiting, rashes and dyspnoea especially in those who have not be exposed to cyanide.
Status:
US Previously Marketed
Source:
DYNACAINE W/EPINEPH PYRROCAINE by GRAHAM CHEM
(1962)
Source URL:
First approved in 1962
Source:
DYNACAINE W/EPINEPH PYRROCAINE by GRAHAM CHEM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pyrrocaine is the amide local anesthetics. It is metabolized to 2,6-xylidine. It was used mainly as an infiltration and nerve block dental anesthetic in the 1960s and favored due to its rapid onset. The potency of pyrrocaine equals that of lidocaine in both sensory and motor nerve blocking. Pyrrocaine provided to be somewhat less toxic than lidocaine. No methemoglobinemia was clinically observed. It has been classified as unsafe for use in acute porphyria. There is no evidence that it is currently used commercially.
Status:
US Previously Marketed
First approved in 1960
Source:
Dianabol by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Metandienone is an orally active synthetic anabolic-androgenic steroid. In 1970, the FDA accepted that Metandienone (Dianabol) was “Probably Effective” in treating post-menopausal osteoporosis and pituitary-deficient dwarfism. Methandrostenolone is still produced today, but typically in nations with loose prescription drug regulations and by companies that still prefer to cater to an underground athletic market. Androgenic side effects are still common with this substance. This may include bouts of oily skin, acne, and body/facial hair growth. Anabolic/androgenic steroids may also aggravate male pattern hair loss.
Status:
US Previously Marketed
Source:
NADOLOL AND BENDROFLUMETHIAZIDE by IMPAX LABS
(2007)
Source URL:
First approved in 1959
Source:
Naturetin by Squibb
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bendroflumethiazide (INN), formerly bendrofluazide (BAN) is a thiazide diuretic used to treat hypertension. CORZIDE (Nadolol and Bendroflumethiazide Tablets) for oral administration combines two antihypertensive agents: CORGARD (nadolol), a nonselective beta-adrenergic blocking agent, and NATURETIN (bendroflumethiazide), a thiazide diuretic-antihypertensive. Bendroflumethiazide works by inhibiting sodium reabsorption at the beginning of the distal convoluted tubule (DCT). Bendroflumethiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like bendroflumethiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of bendroflumethiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. Thiazides do not affect normal blood pressure. Onset of action of thiazides occurs in two hours and the peak effect at about four hours. Duration of action persists for approximately six to 12 hours. Thiazides are eliminated rapidly by the kidney.
Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin was removed from the U.S. market 20 years ago because of a high incidence of lactic acidosis. Risk factors for the development of lactic acidosis include renal deficiency, hepatic disease, cardiac disease, and drug interaction such as cimetidine. Phenformin exerts potential anti-neoplastic action.
Status:
US Previously Marketed
First approved in 1959
Source:
Laverna by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Oxyphenisatin is a stimulant laxative that has been used by mouth and as an enema. Oxyphenisatin was introduced as Lavema by Winthrop in US in 1959. Oxyphenisatin was used as a cleansing enema apart from x-ray studies and prior to urinary, gastro-intestinal and cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. May be mixed with barium for x-ray examination of the large intestine. Oxyphenisatin may cause jaundice. Oxyphenisatin-induced liver damage usually occurs when the drug has been taken for at least six months and usually two years. Oxyphenisatin was withdrawn in most countries in the early 1970s.
Status:
US Previously Marketed
Source:
CYTELLIN by LILLY
(1961)
Source URL:
First approved in 1956
Source:
Cytellin by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Beta-sitosterol is one of the main dietary phytosterols found in plants which have a similar skeleton as cholesterol. In human clinical trials, beta-sitosterol has been shown to have cholesterol-lowering effects and to relieve symptoms of benign prostatic hyperplasia. There has been a large amount of basic research conducted for potential applications of beta-sitosterol in a diverse range of conditions including cervical cancer, breast cancer, cystic fibrosis, and others. Beta-sitosterol is available over the counter as a natural health supplement and is marketed for a wide range of applications including headaches, tuberculosis, allergies, cancers, fibromyalgia, lupus, asthma, hair loss and many others.
Status:
US Previously Marketed
First approved in 1955
Source:
Vanquin by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.