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

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Showing 1381 - 1390 of 1447 results

Status:
Possibly Marketed Outside US
Source:
Japan:Bucladesine Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Bucladesine is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. The compound is used in a wide variety of research applications because it mimics cAMP and can induce normal physiological responses when added to cells in experimental conditions. cAMP is only able to elicit minimal responses in these situations. The neurite outgrowth instigated by bucladesine in cell cultures has been shown to be enhanced by nardosinone. Recently, the effect of bucladesine as a cAMP analog has been studied on the pentylenetetrazol-induced seizure in the wild-type mice. The data showed that bucladesine (300nM/mouse) reduced the seizure latency and threshold. In addition they found that combination of bucladesine and pentoxyfillin has additive effect on seizure latency and threshold. Bucladesine is more lipophilic than cAMP and in contrast to cAMP capable of penetrating cell membranes. Bucladesine interferes with different protein kinases which are normally activated by cAMP. Bucladesine has undergone in the past clinical developments as systemic treatment for cardioprotection and as topical treatment to improve wound healing. In Japan, a bucladesine ointment (Actosin® ointment; Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan) was marketed to treat skin ulcers. Clinical studies have shown favourable effects on diabetic foot ulcers or decubitus, but the compound was later withdrawn despite good tolerability. One possible reason for the withdrawal may be the odour of the cream formulation which can be related to the hydrolytic cleavage in aqueous solutions resulting in release of butyric acid.
Status:
Possibly Marketed Outside US
Source:
Adehl by Nippon Kayaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Colforsin daropate (a derivative of Colforsin) is cardiotonic, adenylate cyclase activator. It is reported as an ingredient of Adehl in Japan. Colforsin daropate hydrochloride is used for the treatment of acute heart failure. Colforsin daropate is capable of directly stimulating adenylate cyclase, which in turn causes vasorelaxation via elevated intracellular concentrations of cyclic adenosine monophosphate, making it a useful therapeutic tool in treating cerebral vasospasm.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Orazamide, which is composed of one molecule of 5-aminoimidazole-4-carboxamide (AICA), one molecule of orotic acid and two molecules of water, is used clinically for the treatment of hepatitis and cirrhosis The nucleoside of AICA (AICAR) is internalized and becomes phosphorylated by adenosine kinase to form AICAR mono-phosphate (AICA ribotide, ZMP), an intermediate in the late steps of de novo purine biosynthesis. In hepatocytes, AICA can inhibit the fatty acid synthesis, sterol synthesis, and gluconeogenesis.
Status:
Possibly Marketed Outside US
Source:
Japan:Androstenediol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



This compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans. The value of Δ5-diol as a radiation countermeasure is based mainly on its stimulation of production of white blood cells and platelets. Androstenediol used by the body to make testosterone and estrogen. There is some concern that androstenediol might increase the risk of coronary heart disease. There is also developing evidence that androstenediol might help prostate cancer cells grow. Taking androstenediol along with estrogen and testosterone pills might cause too much estrogen or testosterone in the body.
Status:
Possibly Marketed Outside US
Source:
Japan:Methylmethionine Sulfonium Chloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



METHYLMETHIONINE (S-Methionine methyl sulfonium, SMMS) chloride is a derivative of methionine metabolism in some plants. Methylmethionine has therapeutic effects on gastrointestinal ulceration potentially via its ability to promote dermal fibroblast migration and growth. The natural derivative Methylmethionine is biosynthesized from L-methionine which is first converted to S-adenosylmethionine. The subsequent conversion, involving replacement of the adenosyl group by a methyl group is catalyzed by the enzyme methionine S-methyltransferase. Methylmethionine is particularly abundant in plants, being more abundant than methionine. S-Methylmethionine is sometimes referred to as vitamin U, but it is not considered a true vitamin. The term was coined in 1950 by Garnett Cheney for uncharacterized anti-ulcerogenic factors in raw cabbage juice that may help speed healing of peptic ulcers.
Vincamine is the major alkaloid of Vinca minor. Although vincamine has been used therapeutically for almost three decades, the exact mechanisms of action and its effects are still unknown. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Vincamine is beneficial to the nervous system's cells feeding and protecting processes and is utilized as an adjuvant in case of cerebrovascular insufficiency, age-related psycho-behavioral disorders, post concussion syndrome in head trauma, in case of post-stroke sequels. Vincamine may be used as a dietary nootropic supplement.
Vincamine is the major alkaloid of Vinca minor. Although vincamine has been used therapeutically for almost three decades, the exact mechanisms of action and its effects are still unknown. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Vincamine is beneficial to the nervous system's cells feeding and protecting processes and is utilized as an adjuvant in case of cerebrovascular insufficiency, age-related psycho-behavioral disorders, post concussion syndrome in head trauma, in case of post-stroke sequels. Vincamine may be used as a dietary nootropic supplement.
Status:
Possibly Marketed Outside US
Source:
Japan:Nizofenone Fumarate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nizofenone (Ekonal, Midafenone) is a neuroprotective drug which protects neurons from death following cerebral anoxia (interruption of oxygen supply to the brain). It might thus be useful in the treatment of acute neurological conditions such as stroke. Nizofenone ameliorates various pathophysiologic events during ischemia, such as ATP depletion, lactate accumulation, glutamate release, free fatty acid liberation, edema, and neuronal degeneration; in particular, ischemia-induced excessive glutamate release has been completely blocked by this drug. This drug has also radical-scavenging action, comparable to vitamin E, and inhibits oxygen radical-induced lipid peroxidation. The potent cerebroprotective effect of nizofenone has been demonstrated in various experimental models of cerebral hypoxia, ischemia (focal and global), ischemia-reperfusion, and infarction. The clinical efficacy of nizofenone has been proved by pioneering double-blind studies in acute subarachnoid hemorrhage patients. Nizofenone is clinically used for preventing the delayed ischemic neurologic deficits due to late vasospasm following subarachnoid hemorrhage.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Prosultiamine (Alinamin®), a well-known thiamine derivative, was first developed by Takeda Pharmaceutical Company in Japan in the 1950s. The drug is a homolog of allithiamine produced by thiol-type vitamin B1 and allicin. Prosultiamine is converted to vitamin B1 after absorption from the gut. The drug thus enables a long-lasting high blood concentration of vitamin B1, resulting in efficient access of vitamin B1 to nervous tissue. Prosultiamine has cured many patients with vitamin B1 deficiency resulting in beriberi neuropathy and Wernicke’s encephalopathy. Prosultiamine is also a potential treatment for HTLV, since it has been shown to reduce viral load and symptoms.
Manganese gluconate is a manganese salt of gluconic acid. Manganese gluconate is sometimes used as a food additive for its texture and light pink coloring. As a food additive, manganese gluconate increases satiety, and the texture of processed foods related to mouth feel. However, in recent years, manganese gluconate has been used less and less as a food additive due to its high toxicity. Many food manufacturers have abandoned using manganese gluconate in favor of other chemical compounds that provide similar effects with a lower toxicity. According to the Food and Drug Administration, manganese gluconate is generally recognized as safe, or GRAS. However, high amounts of manganese gluconate intake, upwards of 15 mg per day, may cause potentially serious health risks. Manganese gluconate toxicity may cause a chemical imbalance in the brain, increasing your risk of developing anxiety, depression, nervousness, psychosis, and mania. Manganese gluconate is used for prevention of deficiency and osteoporosis (off-label).

Showing 1381 - 1390 of 1447 results