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

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Showing 821 - 830 of 2340 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



A-844606 is a selective α7 nicotinic acetylcholine receptor (nAChR) partial agonist (EC50 values are 1.4 and 2.2 μM at human and rat receptors respectively). Displays no measurable effect on α4β2 nAChRs. Stimulates α7 nAChR-induced ERK1/2 phosphorylation in PC12 cells. A-844606 is being investigated as the drug potentially usefull in the treatment of cognition disorders.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1). A-784168 has a good CNS penetration. Significant CNS penetration is necessary for a TRPV1 antagonist to produce broad-spectrum analgesia that was shown on animal models after oral administration of this compound.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

A-796260 is a compound that acts as a potent and selective cannabinoid CB2 receptor agonist. The analgesic effects of A-796260 on activity-induced pain behavior were evaluated in a rat model, the results demonstrated that A-796260 may be a useful new pharmacological compound for further studying CB2 receptor pharmacology and for evaluating its role in the modulation of pain.
A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 uM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 uM, 1.9 uM, or 1.1 uM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 uM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 uM. A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells. A recent research shows A-769662 inhibited cell proliferation and DNA synthesis.