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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 51 - 60 of 297 results

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

AMPROTROPINE (Syntropan) is the phosphate salt of 3 diethylamine, 2.2 dimethylpropanol tropic acid ester. Syntropan is antispasmodic. Its main effect is parasympathetic, and its internal uses are chiefly the same as those of atropine. Syntropan produces relaxation of the tone of the stomach and inhibition of peristaltic activity. The effect of syntropan on gastric secretion excited by a meat extract meal and histamine is weak as compared with atropine. Its advantages as a mydriatic were also described: the rapid effect; the short duration; no general dangers nor discomforts; no local dangers, as damaging the corneal epithelium, or increasing the intraocular pressure; no delay in returning to work for the patient.
Status:
US Previously Marketed
First approved in 1992

Class (Stereo):
CHEMICAL (ABSOLUTE)



Teniposide is an inhibitor of topoisomerase II with anti-cancer activity. The drug was approved by FDA under the name Vumon for the treatment of children with acute lymphoblastic leukemia.
Thiabendazole (TBZ, trade names Mintezol, Tresaderm, and Arbotect) was first introduced in 1962. This drug is a fungicide and parasiticide and is indicated for the treatment of: strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, trichinosis: relief of symptoms and fever and a reduction of eosinophilia have followed the use of this drug during the invasion stage of the disease. But usage of this drug was discontinued. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminthspecific enzyme fumarate reductase. It was shown, also that thiabendazole reversibly disassembles newly established blood vessels, marking it as vascular disrupting agent (VDA) and thus as a potential complementary therapeutic for use in combination with current anti-angiogenic therapies. Was shown, that vascular disruption by TBZ results from reduced tubulin levels and hyper-active Rho signaling. In addition, was confirmed, that thiabendazole slowed tumor growth and decreased vascular density in preclinical fibrosarcoma xenografts and thus, it could lead directly to the identification of a potential new therapeutic application for an inexpensive drug that is already approved for clinical use in humans.
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:
Paveril Phosphate by Lilly
(1951)
Source URL:
First approved in 1951
Source:
Paveril Phosphate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dimoxyline is the synthetic analogue of papaverine, Acute toxicity studies show it to be less toxic than papaverine. No analgesic action and no tolerance development in experimental animals by repeated administration. But Dimoxyline does not appear to be as potent as papaverine in comparable dosage. Dimoxyline is indicated for the treatment of patients with angina pectoris. Also, significant amount of benefit was claimed in patients with acute or chronic phlebitis, arterial thrombosis or embolism, Raynaud’s phenomena and early thromboangiitis obliterans or arteriosclerosis obliterans. Detected adverse events are: nausea or abdominal cramps.
Status:
US Previously Marketed
Source:
My-B-Den by Bischoff (Dome)
(1949)
Source URL:
First approved in 1949
Source:
My-B-Den by Bischoff (Dome)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Adenosine monophosphate (AMP) is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways.
Status:
US Previously Marketed
Source:
Pentaquine Phosphate by Abbott
(1948)
Source URL:
First approved in 1948
Source:
Pentaquine Phosphate by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pentaquine is an 8-aminoquinoline that was used in the 1950s to treat malaria and trypanosomiasis. Pentaquine showed no significant sporontocidal activity against P. gallinaceum in Aedes aegypti. In the experimental animals, the antimalarial effect of pentaquine, its pharmacology and toxicology have been investigated (1, 2). Activity, 80 to 128 times that of quinine and two to eight times that of pamaquin in avian malaria. It has adverse effects very similar to those of primaquine. In mammals it is rapidly absorbed from the gastro-intestinal tract. In acute, and in short term chronic toxicity studies, pentaquine was from one-fourth to one-half as toxic as pamaquin. In the dog, pamaquin in large doses produces severe anorexia, emaciation and ocular paralysis due to central impairment of the sympathetic innervation of the eye. In high dosages pamaquin produces leukopenia, neutropenia, anemia, methemoglobinemia, emaciation, depression, and liver damage in the monkey, effects which are not produced with pentaquine in this species.
Status:
US Previously Marketed
First approved in 1948
Source:
Antistine Phosphate by Ciba
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Antazoline is an antagonist of histamine H1 receptors. It selectively bind to but does not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Antazoline in combination with naphazoline (VASOCON-A®) is indicated to relieve the symptoms of allergic conjunctivitis.
Glucose-6-phosphate belongs to the class of organic compounds known as monosaccharide phosphates. It lies at the start of two major metabolic pathways: glycolysis and the pentose phosphate pathway. It is a glucose-6-phosphatase substrate. Hexokinase is inhibited by its product, glucose 6-phosphate. The non-enzymatic glycation of myosin by glucose 6-phosphate is probably the primary cause for the observed loss of the ATPase activity of myosin.