VARUBI is a selective and competitive antagonist
of human substance P/neurokinin 1 (NK-1) receptors, with a plasma half-life of approximately seven days.
Exendin (9-39) is a well-characterized, competitive antagonist
of glucagon-like peptide-1 (GLP-1) at its receptor.
Like zafirlukast, montelukast is a competitive antagonist
for the cysteinyl leukotrienes.
Together, these findings give indirect evidence for the idea that PA could be a potent competitive antagonist
of P2Y12 receptor, and open the possibility to consider it as new member of the non-nucleotide generation of antiplatelet drugs.
The authors conclude that GCA represents a more accurate definition of additivity for mixtures that include partial agonists or competitive antagonist
Flumazenil is a competitive antagonist
at the benzodiazepine receptor with duration of action varying from 140 to 250 minutes.
NK4 is an elastase-generated fragment of hepatocyte growth factor (HGF) containing four kringle domains, initially discovered as a competitive antagonist
Sodium sulfacetamide acts as a competitive antagonist
to para aminobenzoic acid (PABA), a component of bacterial growth which can lead to the development of rosacea "pimples," while sulfur reportedly inhibits the growth of Propionbacterium acnes and the formation of free fatty acids.
DIM had little AhR-related activity in the HlGl assay (approximately 8% of the maximal effect of TCDD), making it a nearly complete competitive antagonist
This effect appears to be mediated exclusively by GR, because the GR-specific competitive antagonist
, RU-486, completely blocked the hormone responsiveness of this construct (Figure 3A).
PHARMA & BIOTECH LICENSING OPPORTUNITIES IN PSYCHIATRIC DRUG DISCOVERY AND DEVELOPMENT Moderator: John Reid, PhD Director, Global Alliance Management CNS Research & Development AstraZeneca Pharmaceuticals LP PRE 703: A Novel mGluR Competitive Antagonist
as Potential Anti-Anxiety Agent Ken Curry, Ph.
A sampling of topics: neurochemical and developmental aspects of glutamate receptors in the retina, insights from structure-function studies of AMPA receptor agonists and competitive antagonists
, NMDA receptor-mediated activation of arachidonic acid and nitric oxide signaling pathways in the spinal processing of pain, AMPA receptor-mediated neuronal death in motor neuron disease, excitotoxicity and white matter damage, and chemoreception of umami in caterpillars.