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

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Showing 351 - 360 of 1076 results

Status:
US Previously Marketed
Source:
Reneal by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Reneal by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phytic acid is a major phosphorus storage compound of most seeds and cereal grains. It has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron. Phytic acid is also considered to be a natural antioxidant and is suggested to have potential functions of reducing lipid peroxidation and as a preservative in foods. Clathrin-associated adaprot complex AP-2 has it been suggested may act as one of the receptor sites for Phytic acid. Both in vivo and in vitro experiments have demonstrated striking anticancer (preventive as well as therapeutic) effects of Phytic acid.
Status:
US Previously Marketed
Source:
Syntetrin by Bristol
(1959)
Source URL:
First approved in 1959
Source:
Syntetrin by Bristol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Rolitetracycline, launched in the late 1950s, was the first of the semi -synthetic tetracyclines. Rolitetracycline is formed by a Mannich condensation of formaldehyde and pyrrolidine with tetracycline. Rolitetracycline is a pro -drug of tetracycline, in which the pyrrolidine moiety improves bioavailability compared with tetracycline. Rolitetracycline has broad spectrum Gram positive activity in vivo, but pH instability limits use to parenteral administration. Rolitetracycline passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
Status:
US Previously Marketed
Source:
Daricon by Pfizer
(1958)
Source URL:
First approved in 1958
Source:
Daricon by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Oxyphencyclimine is an anticholinergic drug (trade name Daricon) used in treating peptic ulcers. Daricon was discontinued in USA, but still used worldwide.
Triamcinolone is a long-acting synthetic corticosteroid primarily used for their anti-inflammatory effects in disorders of many organ systems. Triamcinolone diacetate injectable suspension is indicated for intramuscular use as follows: Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, serum sickness, transfusion reactions. Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, severe erythema multiform (Stevens-Johnson syndrome). Endocrine Disorders Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsuppurative thyroiditis. To tide the patient over a critical period of the disease in regional enteritis and ulcerative colitis. Hematologic Disorders Acquired (autoimmune) hemolytic anemia, Diamond-Blackfan anemia, pure red cell aplasia, selected cases of secondary thrombocytopenia. Trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate ant tuberculous chemotherapy. For palliative management of leukemia’s and lymphomas. Nervous System Acute exacerbations of multiple sclerosis; cerebral edema associated with primary or metastatic brain tumor, or craniotomy. Sympathetic ophthalmia, uveitis and ocular inflammatory conditions unresponsive to topical corticosteroids. To induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus. Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate ant tuberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis. As adjunctive therapy for short-term administration in acute gouty arthritis; acute rheumatic carditis. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins that, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Firstly, however, these glucocorticoids bind to the glucocorticoid receptors, which translocate into the nucleus, bind DNA (GRE), and change genetic expression both positively and negatively. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Status:
US Previously Marketed
Source:
Blutene Chloride by Abbott
(1953)
Source URL:
First approved in 1953
Source:
Blutene Chloride by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Tolonium chloride (INN, also known as toluidine blue or TBO) is a phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery. Toluidine blue has high affinity for acidic tissue components, thereby staining tissues rich in DNA and RNA. It has found wide applications both as vital staining in living tissues and as a special stain owing to its metachromatic property. Toluidine blue has been used in vivo to identify dysplasia and carcinoma of the oral cavity.
Status:
US Previously Marketed
Source:
Gemonil by Abbott
(1952)
Source URL:
First approved in 1952
Source:
Gemonil by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Methbarbital is a barbiturate anticonvulsant, discovered by Merck in 1905. It was introduced to market for treatment of epolepsy by Abbott in 1952, and discontinued in 1990.
Status:
US Previously Marketed
Source:
Evans Blue by Parke Davis
(1951)
Source URL:
First approved in 1951
Source:
Evans Blue by Parke Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Evans Blue (EBD) is an azo dye which has a very high affinity for serum albumin. It can be useful in physiology in estimating the proportion of body water contained in blood plasma. Evans Blue Dye is widely used to study blood vessel and cellular membrane permeability as it is non-toxic, it can be administered as an intravital dye and it binds to serum albumin – using this as its transporter molecule. The EBD–albumin conjugate (EBA) can be: (i) identified macroscopically by the striking blue colour within tissue; (ii) observed by red auto-fluorescence in tissue sections examined by fluorescence microscopy; and (iii) assessed and quantified by spectrophotometry for serum samples, or homogenised tissue. has recently been utilised in mdx mice to identify permeable skeletal myofibres that have become damaged as a result of muscular dystrophy. EBD has the potential to be a useful vital stain of myofibre permeability in other models of skeletal muscle injury and membrane-associated fragility. Evans Blue is a potent inhibitor of L-glutamate uptake into synaptic vesicles. It also inhibits AMPA and kainate receptor-mediated currents (IC50 values are 220 and 150 nM respectively). P2X-selective purinoceptor antagonist.
Status:
US Previously Marketed
First approved in 1951
Source:
Kwell by Reed & Carnrick
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lindane is an isomer of hexachlorocyclohexane that has been used both as an agricultural insecticide and as a pharmaceutical. As a shampoo, lindane is used for treamtment lice infestation. Lindane lotion is used for treatment of scabies. Due to toxicities, associated with lindane, it is used only in patients who cannot tolerate or have failed first-line treatment with safer medication. Lindane exerts its parasiticidal action by being directly absorbed into the parasites and their ova, where it interferes with GABA neurotransmitter function by interacting with the GABAA channel complex at the picrotoxin binding site.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(7) dandruff chloroxylenol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlorothymol is a derivate of thymol. Thymol is a known antifungal agent, which was applied as a dusting powder for superficial infections now only found as a general antimicrobial agent used in mouthwashes. Chlorothymol more potent germicide, but severely irritating to the mucous membranes. It is used in cosmetic biocides, denaturants, deodorant agents, oral care agents, and preservatives. Chlorothymol was not considered an ocular irritant. Chlorothymol was nonmutagenic compound in the paper-disk method using E. coli. No adverse reactions were noted during the course of the study of AMA Laboratories in 1996 performed to assess the skin irritation and sensitization of an OTC topical cream. OTC topical cream containing 0.032% Chlorothymol under semiocclusion was considered a nonprimary irritant and a nonprimary sensitizer.
Status:
US Previously Marketed
Source:
KECTIL DIHYDROSTREPTOMYCIN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1948
Source:
Dihydrostreptomycin Sulfate by Merck
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dihydrostreptomycin is an antibiotic compound derived from streptomycin by reduction with hydrogen. The primary mechanism of action of the antibiotic dihydrostreptomycin is binding to and modifying the function of the bacterial ribosome, thus leading to decreased and aberrant translation of proteins, in addition it binds mechanosensitive channel of large conductance (MscL) and modifies its conformation, thus allowing the passage of K+ and glutamate out of, and dihydrostreptomycin into, the cell. It has about the same degree of antibacterial activity as streptomycin, but it is less effective against some gram-negative microorganisms. Because it has a higher risk of irreversible deafness, and its effectiveness is no greater that that of streptomycin, dihydrostreptomycin is no longer used clinically. To date dihydrostreptomycin is approved for veterinary use to treat bacterial infections.