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

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Showing 21 - 30 of 97 results

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



(±)-3A,7A-di-epi-Perindopril is a mixture of two isomers (S, RR, SS) and (R, SS, RR) each of which is an isomer of the antihypertensive drug perindopril. The first of which has the same activity as the compound while the second one is almost inactive.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

(±)-2,3A-di-epi-Perindopril is a mixture of two isomers (S, SR, RR) and (R, RS, SS) which are both inactive epimers of the antihypertensive drug perindopril, although the (R, RS, SS) isomer possesses better activity.
Verticinone is a major alkaloid isolated from the bulbus of Fritillaria ussuriensis. Verticinone was rapidly absorbed, widely distributed in most tissues, and metabolized extensively before excretion. Verticinone has antitumor effects - treatment with verticinone can induce cancer cell apoptosis and autophagy via modulating the production of metabolites, which are supportive of carcinoma cell proliferation. Due to the potent antitussive activity and no addictive effect, verticinone seems to be a promising potential antitussive drug. Verticinone is expected to become a potentially novel sedative-analgesic agent without producing tolerance and dependence.
Verticine is a steroidal alkaloid compound extracted from the Fritillaria species of medicinal plants. Verticine was not only able to block the Nav1.7 ion channel but also preferably inhibited the Kv1.3 ion channel. It inhibits the production of inflammatory cytokines induced by LPS through blocking MAPKs and NF-κB signaling pathways. Verticine inhibited the hERG peak tail currents in a concentration dependent manner. Verticine exhibits anti-inflammatory, antitussive, antihypertensive and pain suppression properties.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



(3AR)-3A-epi-Perindopril is an epimer (S, RS, SS) of the drug perindopril which is commonly used to treat high blood pressure, hypertension, heart failure, or stable coronary artery disease. This epimer possesses equal activity with the parent compound, perindopril.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



(±)-7A-epi-Perindopril is a mixture of two isomers (S, SR, SS) and (R, RS, RR) each of which is an isomer of the antihypertensive drug perindopril. The first of which has the same activity as the parent compound while the second one is almost inactive.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Eugenyl glucoside is a product of eugenol glucosylation. Eugenol is the principal chemical component of clove oil, accounting for more than 90%, has been well known for its antioxidant, anti-proliferative, analgesic, local anesthetic, anti-inflammatory, antibacterial, and hair growing effects. Eugenol belongs to the class of essential oil that is generally recognized as safe (GRAS) by Food and Drug Administration. Eugenol is liable to sublimate and has a peculiar smell, its modification is needed for application as a component of hair restorers. Therefore, eugenyl glucoside is being produced by organic synthesis and commercially used as an additive in hair restorers since eugenyl glucoside is gradually degraded into eugenol by the indigeneous microorganisms of human skin and acts as a pro-drug of a hair restorer.
Quercitrin is known as a bio flavonoid antioxidant and was investigated extensively in its antioxidant potential in streptrozotocin (STZ)-induced diabetic rats. Quercitrin is also a constituent of the dye quercitron. Quercitrin can be found in Tartary buckwheat and in oaks species such as white oak or European red oak. Quercitrin has potential anti-inflammation effect that is used to treat heart and vascular conditions. Quercitrin offers protection against brain injury in mice by inhibiting oxidative stress and inflammation. Quercitrin also prevented CCl4 induced cerebral function disorders associated with its ability to inhibit the activities of monoamine oxidase (MAO), acetylcholine esterase (AChE) and the N-methyl-d-aspartate receptor 2B subunit (NR2B). Quercitrin suppressed the release of pro-inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6). Quercitrin may be a potential candidate to be developed as a neuroprotective agent. Quercitrin has been used previously as an antibacterial agent and has been shown to inhibit the oxidation of low-density lipoproteins and prevent an allergic reaction. It was demonstrated that quercitrin exerts protective effects against H2O2-induced dysfunction in lung fibroblast cells. Quercitrin has antiproliferative and apoptotic effects on lung cancer cells by modulating the immune response. There were significant increases in caspase-3 activity, loss of MMP, and increases in the apoptotic cell population in response to quercitrin in DLD-1 colon cancer cells in a time- and dose-dependent manner. These results revealed that quercitrin has antiproliferative and apoptotic effects on colon cancer cells. Quercitrin activity supported with in vivo analyses could be a biomarker candicate for early colorectal carcinoma.
Status:
US Previously Marketed
First approved in 1994

Class (Stereo):
CHEMICAL (ABSOLUTE)



Spirapril (Renormax) is an ACE inhibitor antihypertensive drug used to treat hypertension. Spiraprilat, the active metabolite of spirapril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Spiraprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.