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Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Amfonelic acid (AFA) is a dopamine reuptake inhibitor. Experiments on rats have shown that AFA treatment completely prevented the effects of methamphetamine on the dopaminergic system, both morphologically and biochemically.
Class (Stereo):
CHEMICAL (RACEMIC)
Nifurimide, a 5-nitrofuran derivative, is an antibacterial agent. It was used for controlling Salmonella choleraesuis in swine. The mode of action of 5-nitrofuran analogues is based on red-ox biotransformation.
Status:
Investigational
Source:
INN:clodanolene [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Clodanolene is a skeletal muscle contraction antagonist, closely related to dantrolene sodium. The drug has no measurable direct effect on the peripheral or central nervous systems. In a mouse of muscle spasticity (Straub-tail mouse), clodanolene induced skeletal muscle relaxation more effectively than neuromuscular blocking agents, local anesthetics, or centrally-acting muscle relaxants. Indirect evidence indicates clodanolene acts on caffeine-sensitive calcium stores in the muscle cells.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Midaflur, an imidazoline derivative, was developed as an anesthetic agent. This drug acted as a central skeletal muscle relaxant and showed sedative properties. Preclinical experiments have shown that midaflur had minimal effects at high doses in cardiovascular studies. In addition, it was inactive in anti-inflammatory, diuretic, and plasma glucose studies. Information about the current use of this compound is not available.
Status:
Investigational
Source:
USAN:METOPRINE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Metoprine is a diaminopyrimidine folate antagonist with potential antineoplastic activity. Metoprine inhibits dihydrofolate reductase, resulting in decreased cellular folate metabolism and cell growth. Metoprine shows potent in vitro antitumor activity against several experimental tumors including methotrexate-resistant tumors. Metoprine inhibits the enzyme dihydrofolate reductase, much less effectively than methotrexate but it also inhibits histamine-N-methyltransferase, resulting in decreased histamine catabolism. S phase cells are most sensitive, whilst cells in G2 and M are least sensitive to the lethal effects of Metoprine, and a prolonged exposure to a high Metoprine concentration produces maximum cytotoxic effects. After oral administration, Metoprine has a widespread distribution and concentration in all tissues examined with the highest tissue/plasma ratios found in brain, lung, pancreas, and skin. Phase I and early Phase II clinical trials in various centers have shown activity in hypernephroma, epidermoid carcinoma arising in bronchus or head and neck, central nervous system leukemia, malignant melanoma, and mycosis fungicides. Metoprine had been in some phase II clinical trials but further studies were discontinued due to CNS and hematological toxicity.
Class (Stereo):
CHEMICAL (MIXED)
Fenestrel (ORF-3858) is a nonsteroidal antizygotic compound. It antagonizes progesterone. Fenestrel is a post-coital contraceptive.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Trimoprostil is a synthetic prostaglandin E2 derivative and prostanoid receptor agonist, with potential gastric secretion inhibitor and antiulcerogenic activity. It has been shown to reduce hydrogen ion secretion, to enhance gastric bicarbonate secretion and to reduce aspirin-induced gastric mucosal injury. In contrast to many E prostaglandins, it does not lower the tone of the lower oesophageal sphincter. Trimoprostil was well tolerated and more effective than placebo in the treatment of mild to moderate symptomatic reflux oesophagitis. It may be protective to human squamous oesophageal mucosa. Trimoprostil was not as effective as cimetidine in the treatment of duodenal ulcer.
Class (Stereo):
CHEMICAL (ACHIRAL)
It is known that the terbucromil possessed uricosuric effects in man. However, information about the current development and use of this compound is not available.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Menoctone is a potent liver-stage antimalarial with corresponding erythrocytic stage efficacy. This drug is an effective treatment against Theileria parva, a parasitic protozoan that causes East Coast fever in cattle. Menoctone most likely targets the mitochondrial respiration chain of Plasmodium.
Class (Stereo):
CHEMICAL (ACHIRAL)
Clioxanide is a derivative of diiodobenzanilide, developed by Parke, Davis & Co in the 1960s. It was used as an antihelmintic against Fasciola hepatica and Haemonchus contortus. In sheep, the compound was demonstrated high efficiency (greater than 90%) when administered at 20-40 mg/kg. Later it was found that clioxanide is an inhibitor of Type III Secretion in Yersinia bacteria.