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

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Showing 731 - 740 of 2263 results

Octopamine is an organic chemical closely related to norepinephrine. In many types of invertebrates it functions as a neurotransmitter. Octopamine is known to exert adrenergic effects in mammals although specific octopamine receptors have been cloned only in invertebrates. It has been shown that octopamine can stimulate alpha(2)-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha(2)-ARs. Octopamine stimulates lipolysis through beta(3)-rather than beta(1)-or beta(2)-AR activation in white adipocytes from different mammalian species. Octopamine activates only beta(3)-ARs and is devoid of alpha(2)-adrenergic agonism. Thus, octopamine could be considered as an endogenous selective beta(3)-AR agonist. In humans Octopamine is a trace amine found endogenously in the human brain where it interacts with signalling of catecholamines; it is structurally similar to synephrine and tyramine, being a metabolite of the latter (via dopamine β-hydroxylase) and substrate for the synthesis of the former (via phenethanolamine N-methyltransferase[3]) while being perhaps the closest in structure to noradrenaline. Octopamine is found in the bitter orange similar to many biogenic amines related to L-tyrosine that are used as dietary supplements, this includes synephrine and hordenine. p-Octopamine HCl (Norphen) was studied in the late 1960’s and 1970’s as a drug for the treatment of hypotensive regulatory and circulatory disorders. Octopamine was used as a nootropic. All optical isomers (enantiomers) of octopamine are on the World Anti-Doping Agency (WADA) 2014 list of substances prohibited in competition.
Status:
Possibly Marketed Outside US
Source:
ARPOCOX by Merck
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Arprinocid is a coccidiostat used in veterinary medicine. Effective against coccidiosis in poultry.
Status:
Possibly Marketed Outside US
Source:
Unknown by Parke Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bentazepam (also known as Thiadipone, Tiadipona) is a benzodiazepine analog, used as a short-action anxiolytic. Bentazepam a thienodiazepine with the same main mechanism of action as the classic 1,4-benzodiazepines, is a short-action anxiolytic, with an elimination-half-life of 3 to 5 hours in healthy volunteers. Bentazepam possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. A severe benzodiazepine overdose with bentazepam may result in coma and respiratory failure. Adverse effects include dry mouth, somnolence, asthenia, dyspepsia, constipation, nausea and drug-induced lymphocytic colitis has been associated with bentazepam. Severe liver damage and hepatitis has also been associated with bentazepam. Whilst liver failure from bentazepam is considered to be rare, liver function monitoring has been recommended for all patients taking bentazepam.
Status:
Possibly Marketed Outside US
Source:
Dimecarbinum by Grinev, A.N. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Mecarbinate is a chemical intermediate of arbidol hydrochloride. Dimecarbin is used in the treatment of hypertension in Russia.
Status:
Possibly Marketed Outside US
Source:
Promintic by Imperial Chemical Industries
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Metyridine has been shown to possess anthelmintic activity, particularly for the nematodes of the alimentary canal. Methyridine is able to pass freely through most of the barriers, which maintain body integrity. It produces neuromuscular block of the decamethonium type. There appears to be sufficient difference between the sensitivity of nematode and vertebrate nervous systems to this drug to allow a wide safety margin for its use in animals. Signs of toxicity, principally dullness and lassitude, may be produced by overdosage of the drug. When given subcutaneously methyridine may cause local pain, and swelling.
Status:
Possibly Marketed Outside US
Source:
Fenclozic Acid by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fenclozic acid emerged in the late 1960s as a promising carboxylic acid non-steroidal anti-inflammatory drug candidate that demonstrated potent anti-inflammatory, anti-pyretic and analgesic properties. Whole body autoradiography showed fenclozic acid distribution into all tissues except the brain, with radioactivity still detectable in blood, kidney and liver at 72 h post-dose. Fenclozic acid was compared with aspirin in a double-blind, crossover trial in patients with rheumatoid arthritis. It was concluded that fenclozic acid afforded symptomatic relief and was comparable to aspirin. Unfortunately, hepatotoxicity was observed in subsequent trials and the drug was withdrawn from the clinic.
Status:
Possibly Marketed Outside US
Source:
Madar by Sternbach, L.H.|Reeder, E.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nordazepam (INN; marketed under brand names Nordaz, Stilny, Madar, Vegesan, and Calmday) is a 1,4-benzodiazepine derivative with amnesic, anticonvulsant, anxiolytic, muscle relaxant, and sedative properties. Nordazepam is an active metabolite of diazepam, chlordiazepoxide, clorazepate, prazepam, pinazepam, and medazepam, used primarily in the treatment of anxiety disorders. Nordazepam is a partial agonist at the GABAA receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle-relaxing effects. Nordazepam’s elimination half-life is between 36 and 200 hours, with wide variation among individuals; factors such as age and gender are known to impact it. The variation of reported half-life are attributed to differences in nordazepam metabolism and that of its metabolites as nordazepam is hydroxylated to active metabolites such as oxazepam, before finally being glucuronidated and excreted in the urine. Common side effects of nordazepam include somnolence, which is more common in elderly patients and/or people on high-dose regimens. Hypotonia, which is much less common, is also associated with high doses and/or old age.
Status:
Possibly Marketed Outside US
Source:
Butalex by Wellcome Foundation
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Buparvaquone is a second-generation hydroxynaphtaquinone with novel features that make it an effective compound for the therapy and prophylaxis of all forms of theileriosis. It has shown promising activities against Leishmania spp. and Neospora caninum infection. In combination with arteether it is effective against Babesia equi. Buparvaquone directly inhibits the respiration of Theileria parasites. Due to the inhibiting effects of theileriosis on the immune system, vaccination should be delayed until the animal has recovered from theileriosis. Localised, painless, oedematous swelling may occasionally be seen at the injection site.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefalonium is a 1st generation cephalosporin with a broad spectrum of actvity against Gram-positive and Gram-negative bacterias. The drug inhibits the bacterial cell wall synthesis by binding to penicillin binding proteins. Cefalonium is approved for routine dry cow therapy to treat existing sub-clinical infections and to prevent new infections which occur during the dry period.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Diloxanide (used in the form of furoate) was developed for the treatment of intestinal amoebiasis. The effectiveness of the drug was proved in clinical trials, however, the mechanism of its action is unknown. The drug is not marketed in the United States, athough it is available in India.