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

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Showing 261 - 270 of 296 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Piperidine is a normal constituent in mammalian brain. It was shown to affect synaptic mechanism in the CNS, and influence neural mechanisms governing regulation of emotional behavior, sleeping, and extrapyramidal function. In addition, there are enzyme systems within the brain that synthesize and metabolize piperidine, and uptake and storage mechanisms for piperidine are found in the nerve endings. Piperidine, which proved to be a highly effective “antipsychotomimetic” agent in rats, has been reported to bring about substantial improvement in a variety of schizophrenic patients.
Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of jistamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. In addition, histamine is being studied for treatment of multiple sclerosis. It was approved, that histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The H3R is an auto receptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.
Status:
US Previously Marketed
First approved in 1957

Class (Stereo):
CHEMICAL (ACHIRAL)


P-32 is a radioactive isotope of phosphorus with a half-life of 14.29 days. Radioactive decay of P-32 produces beta-particles (electrons) which are able to penetrate tissue at a range of 3-8 mm. Phosphate ion P-32 has many applications in medicine and biology. P32 sodium phosphate was approved by the FDA for the treatment of polycythemia vera, chronic myelocytic leukemia, and chronic lymphocytic leukemia. P32-phosphate may also be used in the palliative treatment of selected patients with multiple areas of skeletal metastases. As metabolic uptake of phosphorus is selectively increased in malignant tissues, P-32 was also used for cancer diagnostics.
Status:
US Previously Marketed
First approved in 1957

Class (Stereo):
CHEMICAL (ACHIRAL)


P-32 is a radioactive isotope of phosphorus with a half-life of 14.29 days. Radioactive decay of P-32 produces beta-particles (electrons) which are able to penetrate tissue at a range of 3-8 mm. Phosphate ion P-32 has many applications in medicine and biology. P32 sodium phosphate was approved by the FDA for the treatment of polycythemia vera, chronic myelocytic leukemia, and chronic lymphocytic leukemia. P32-phosphate may also be used in the palliative treatment of selected patients with multiple areas of skeletal metastases. As metabolic uptake of phosphorus is selectively increased in malignant tissues, P-32 was also used for cancer diagnostics.
Status:
US Previously Marketed
First approved in 1957

Class (Stereo):
CHEMICAL (ACHIRAL)


P-32 is a radioactive isotope of phosphorus with a half-life of 14.29 days. Radioactive decay of P-32 produces beta-particles (electrons) which are able to penetrate tissue at a range of 3-8 mm. Phosphate ion P-32 has many applications in medicine and biology. P32 sodium phosphate was approved by the FDA for the treatment of polycythemia vera, chronic myelocytic leukemia, and chronic lymphocytic leukemia. P32-phosphate may also be used in the palliative treatment of selected patients with multiple areas of skeletal metastases. As metabolic uptake of phosphorus is selectively increased in malignant tissues, P-32 was also used for cancer diagnostics.
Status:
US Previously Marketed
Source:
OLEANDOMYCIN 200MG OLEANDOMYCIN PHOSPHATE by ROERIG
(1961)
Source URL:
First approved in 1956
Source:
Matromycin by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oleandomycin is a macrolide antibiotic, which was first described under the designation P.A.105 by Sobin, English, and Celmer (1954-5). Later it appeared on the market under three names and in two forms: as pure oleandomycin ("matromycin," Pfizer; "romicil," Hoffmann-La Roche) and as a mixture with twice its weight of tetracycline ("sigmamycin," Pfizer). Oleandomycin can be employed to inhibit the activities of bacteria responsible for causing infections in the upper respiratory tract much like Erythromycin can. Both can affect staphylococcus and enterococcus genera. Oleoandomycin is reported to inhibit most gram-positive bacteria, but has only a slight inhibiting effect on gram-negative bacteria, rickettsiae, and larger viruses. The spectrum of activity on micro-organisms is therefore wider than that of penicillin and streptomycin, but narrower than that of chloramphenicol and the tetracyclines. Oleandomycin is approved as a veterinary antibiotic in some countries. It has been approved as a swine and poultry antibiotic in the United States. However, it is currently only approved in the United States for production uses. Oleandomycin is a bacteriostatic agent. Like erythromycin, oleandomycin binds to the 50s subunit of bacterial ribosomes, inhibiting the completion of proteins vital to survival and replication. It interferes with translational activity but also with 50s subunit formation. However, unlike erythromycin and its effective synthetic derivatives, it lacks a 12-hydroxyl group and a 3-methoxy group. This change in structure may adversely affect its interactions with 50S structures and explain why it is a less powerful antibiotic.
Status:
US Previously Marketed
Source:
Sodium Albamycin by Upjohn
(1956)
Source URL:
First approved in 1956
Source:
Sodium Albamycin by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Novobiocin (also known as streptonivicin) is an aminocoumarin antibiotic, active against Staphylococcus epidermidis. Novobiocin and other aminocoumarin antibiotics act as a potent competitive inhibitor of DNA gyrase B. The oral form of the drug was withdrawn from the market in 1999 due to safety or effectiveness reasons. Later it was discovered that novobiocin inhibited Hsp90 and topoisomerase II, and novobiocin was investigated in clinical trials against metastatic breast cancer and non-small cell lung cancer. Topical form of novobiocin was investigated in combination with nalidixic acid for treatment of psoriasis.

Showing 261 - 270 of 296 results