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

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Showing 291 - 300 of 454 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Apaxifylline is an adenosine A1 receptor antagonist that was under investigation with Boehringer Ingelheim as a potential neuroprotective drug for the treatment of dementia. Apaxifylline was able to antagonize scopolamine-induced deficits in the rat in a memory task. A single oral application of apaxifylline 90 min before the rats received the noxious stimulus significantly attenuated the scopolamine-induced deficits observed during the retention trial of the rat in the passive avoidance paradigm. Apaxifylline treatment does not influence motility.
Chlorotheophylline (8-Chlorotheophylline) is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. Its main use is in combination with Diphenhydramine as the antiemetic drug Dimenhydrinate (marketed as Draminate, Dramamine, Detensor and Gravol among others). Dimenhydrinate is primarily used to treat nausea, vomiting, and dizziness caused by motion sickness.The stimulant properties of 8-chlorotheophylline are thought to ward off the drowsiness caused by diphenhydramine's anti-histamine activity in the central nervous system. 8-chlorotheophylline produces a number of effects including nervousness, restlessness, insomnia, headache, and nausea, which are primarily attributed to its ability to block the adenosine receptor. Because adenosine causes a decrease in neuronal firing, blockade of the adenosine receptor causes the reverse effect resulting in excitation.
Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
Status:
Possibly Marketed Outside US
Source:
PERFECT SLEEP by Lipmann, F. et al.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Coenzyme A (CoA) is a ubiquitous essential cofactor that plays a central role in the metabolism of carboxylic acids, including short- and long-chain fatty acids, as well as carbohydrate and protein. In the metabolic pathway of lipid, CoA participates in fatty acid β-oxidation, promoting triglyceride (TG) catabolism. Coenzyme A functions as an acyl group carrier and assists in transferring fatty acids from the cytoplasm to mitochondria. All genomes sequenced to date encode enzymes that use coenzyme A as a substrate, and around 4% of cellular enzymes use it (or a thioester, such as acetyl-CoA) as a substrate. Coenzyme A is the most active metabolic enzyme in the human body. It is used as a supplement for the hypothetical treatment of acne.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Bamifylline (or bamiphylline), a selective antagonist of the A1 adenosine receptor, was studied in the therapy of asthmatic syndromes.
Status:
Possibly Marketed Outside US
Source:
ETOFYLLINE by Lespagnol, A. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etofylline [7-(2-hydroxyethyl)theophylline] is a N-7-substituted derivative of theophylline, a smooth muscle relaxant. Etofylline is used to relieve bronchoconstriction. It may act as a phosphodiesterase inhibitor and adenosine receptor antagonist.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Hexobendine (Ustimon or ST7090) is a vasodilator. It inhibits uptake of adenosine and cAMP. Hexobendine was investigated in clinical trials for the treatment of cerebrovascular and coronary artery diseases.
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.

Showing 291 - 300 of 454 results