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

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Showing 801 - 810 of 2752 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.
Songorine is a diterpenoid alkaloid which can be isolated from the genus Aconitum. Songorin has demonstrated anti-inflammatory, anti-anxiolytic and the ability to promote wound healing. The Anti-anxiolytic properties appear to be linked to the agonistic activity of the Dopamine D2 receptor as shown in rat hippocampal slices. The wound healing effect is the result of songorine's ability to stimulate the development of mesenchymal progenitor cells, although the exact mechanism of action remains unclear.
Estrone glucuronide, or estrone-3-D-glucuronide is an endogenous steroid. It is formed from estrone in the liver by UDP-glucuronyltransferase via attachment of glucuronic acid and is eventually excreted in the urine by the kidneys. Early morning urine estrone-3-glucuronide assay is used in the monitoring of ovarian secretory function in precocious puberty. Estrone-3-glucuronide has also used for accurate detection of fertile period.
Bimatoprost acid is a metabolically stable analog of prostaglandin F2alpha, exhibits a relatively high affinity for the FP, EP1, and EP3 receptors and exhibits functional activity at the EP1 and FP receptors. Clinical pharmacological studies with bimatoprost reveal that it is not significantly metabolized due to the absence of free acid hydrolysis product in the systemic circulation after topical ocular administration to human volunteers. The hydrolysis of bimatoprost to a free acid occurs at very low rate.
15-Ketoprostaglandin E2 (15-keto PGE2) is a metabolite of prostaglandin E2 (PGE2) with reduced biological activity, which then by the action of prostaglandin reductase 2 (PTGR2) transforms into 13,14-dihydro-15-keto-PGE2, s a secondary metabolite without biological activity. Some experiments have shown that exists the therapeutic potential by targeting PTGR2/15-keto-PGE2 in pancreatic cancer. Besides, it is known, that 15-keto-PGE2 has higher affinity to the prostaglandin EP2 receptor than to the EP4 receptor. Some experiments also have revealed the key signaling cascade: 15-Hydroxyprostaglandin dehydrogenase (15-PGDH)/15-keto-PGE2-mediated activation of PPARγ and p21(WAF1/Cip1) in the regulation of the hepatocarcinogenesis and tumor progression.