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

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Showing 491 - 500 of 619 results

Beta-erythroidine is an organic heterotetracyclic indole alkaloid isolated from the seeds and other parts of Erythrina species. A drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis. Beta-erythroidine is a neuronal nicotinic acetylcholine receptor antagonist. The beta-erythroidine and its more potent derivative (2,7-dihydro) have been used as muscular relaxants in numerous clinical applications. This activity is attributed to a antagonistic action of the dihydro-beta-erythroidine with the nicotinic receptors of acetyl choline.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dimethocaine (DMC, larocaine), a synthetic derivative of cocaine, is a widely distributed "legal high" consumed as a "new psychoactive substance" (NPS), originally was used in the 1930s as an anesthetic, primarily in dentistry, ophthalmology, and otolaryngology. This drug completely inhibits dopamine transporter and has had the potential for abuse. Dimethocaine is intended for forensic and research purposes.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


(R)-Etifoxine is an isomer, chemically isolated from Etifoxine (Stresam), an approved racemic drug (off patent) prescribed in Europe. (R)-Etifoxine was developed by Xytis Inc for treatment pain, mental disease, and central nervous system disorders. However future development has been discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pamoic acid, also called embonic acid, is a naphthoic acid derivative, used as a counter ion of a drug compound to increase the solubility of the drug in water. Pamoic acid has agonist activity for the orphan G protein-coupled receptor GPR35 by which it activates ERK and beta-arrestin2, and causes antinociceptive activity. Although (like other drug salts) it has been considered an inactive compound by the FDA.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

R-Duloxetine is an enantiomer of the antidepressant S-duloxetine. R-Duloxetine was shown was highly effective against postoperative pain, which could be potential new analgesics. R-Duloxetine could show its effect via the blocking of the neuronal Na⁺ channels.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dimethocaine (DMC, larocaine), a synthetic derivative of cocaine, is a widely distributed "legal high" consumed as a "new psychoactive substance" (NPS), originally was used in the 1930s as an anesthetic, primarily in dentistry, ophthalmology, and otolaryngology. This drug completely inhibits dopamine transporter and has had the potential for abuse. Dimethocaine is intended for forensic and research purposes.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Phenthiazamine was developed by Sekizawa et al. as a centrally acting anesthetic for fish. The time required to reduce the positive ganglionic potential in the sympathetic ganglion by phenthiazamine was prolonged in the presence of higher concentrations of Ca2+. The Ca2+-dependent action potential of guinea-pig ureter was reduced by this compound, whereas it did not affect the Na+-dependent action potential.
1-(5-isoquinolinylsulfonyl)-2-methylpiperazine (H-7) is an inhibitor of cAMP-dependent, cGMP-dependent, and Ca2+-phospholipid-dependent (protein kinase C) protein kinases at roughly equal concentrations. It is widely used to study protein kinase signaling both in vitro and in vivo.
PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Geraniol is a dietary monoterpene alcohol that is found in the essential oils of aromatic plants. To date, experimental evidence supports the therapeutic or preventive effects of geraniol on different types of cancer, such as breast, lung, colon, prostate, pancreatic, and hepatic cancer, and has revealed the mechanistic basis for its pharmacological actions. In addition, geraniol sensitizes tumor cells to commonly used chemotherapy agents. Geraniol controls a variety of signaling molecules and pathways that represent tumor hallmarks; these actions of geraniol constrain the ability of tumor cells to acquire adaptive resistance against anticancer drugs. It has been shown that geraniol inhibits HMG-CoA reductase in most types of tumor cells, which raises the possibility that the reduced prenylation of small G-proteins, such as Ras or RhoA, accounts for the antitumor effects of geraniol. In addition to its use in various commercial products, including cosmetics and fine fragrances, geraniol exerts a broad spectrum of pharmacological activities, such as anti-microbial, anti-inflammatory, anti-oxidant, anti-ulcer and neuroprotective activities. Geraniol is classified into the generally recognized-as-safe (GRAS) category by the Flavor and Extract Manufacturers Association (FEMA) and the Food and Drug Administration (FDA) of the United States.

Showing 491 - 500 of 619 results