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

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Showing 121 - 130 of 537 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



AVE-0118 is a Kv1.5 blocker which was developed by Aventis Pharma for the treatment of cardiovascular diseases. The drug reached phase II of clinical trilas in patients with atrial fibrillation, however its development was terminated.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



Napelline is a diterpenoid alkaloid, from plants of the Aconitum genus, Ranunculaceae. It is a potent antiarrhythmic of class I with weak hypotensive and N-cholinoblocking effects. Napelline has analgesic and anti-inflammatory activity. Napelline has a stronger antiarrhythmic activity than Quinidine or Procaïnamide. 10(-4) - 10(-5) M block inward Na+ currents
Eupatorin is a natural flavonoid isolated from the herbs of Eupatorium semiserratum. It has the anti-inflammatory and anti-proliferative properties, which may be utilized in the development of novel anti-inflammatory and anti-tumor treatments. Eupatorin moderately inhibited human cytochrome P450 1A2 (CYP1A2). Eupatorin showed IC50 values of 0.4 ug/mL on T. cruzi epimastigotes and 61.8 ug/mL on trypomastigotes, respectively. It was demonstrated, that eupatorin exerts a vasorelaxative effect on aortic rings through the NO/sGC/cGMP and PGI2 pathways, calcium and potassium channels, muscarinic and beta-adrenergic receptors.
U-54494A is a unique and selective anticonvulsant agent acting by a Ca(2+)-related mechanism possibly through a subclass of kappa receptors. Voltage- and use-dependent block of the Na and K channels by U-54494A may be an important pharmacological basis for its anticonvulsant action. U-54494A, a racemic mixture of two enantiomers, is being developed and pre-clinically tested as an anticonvulsant drug candidate.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Columbin is a diterpenoid furanolactone, was isolated from the plant species Tinspora bakis. It displays anti-inflammatory activity, protects from azoxymethane-induced rat colon carcinogenesis and possess trypanocidal mechanism.
Isosakuranetin is a citrus fruit flavanone. It is a TRPM3 channel blocker and CYP1 enzyme isoforms inhibitor. It is a strong candidate, as chemopreventive food ingredient against CYP1B1-related carcinogenesis. Isosakuranetin may be useful in treating neuropathic pain without body temperature increase. Isosakuranetin attenuated ethanol-induced gastritis by inhibiting the infiltration of immune cells, including neutrophils, via the regulation of CXCL4 (or IL-8) secretion and the activation NF-κB.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Visnagin is furanochromone and one of the main compounds of Ammi visnaga L. (syn. Khella) that can be frequently found in ethnomedical formulations in Asia and the Middle East. Visnagin possess analgesic properties due to its calcium channel blocking properties and act in an anti-inflammatory manner by inhibiting AP-1 and NF-κB signaling.

Showing 121 - 130 of 537 results