MK-801 (a use-dependent channel blocker or uncompetitive antagonist) and CGP 37849 (a competitive antagonist
) have shown antidepressant properties in preclinical studies, either alone or combined with traditional antidepressants.[12,13]
Ginger is a competitive antagonist
for H3 receptors and it has clinical effect a few days after treatment for approximately 80% of women.
It acts as a competitive antagonist
of growth hormone releasing hormone at its receptor in pituitary and immune cells12.
Neostigmine acts as a competitive antagonist
at the neuromuscular junction by increasing the level of acetocholine available for binding to nicotinic receptors.
Like zafirlukast, montelukast is a competitive antagonist
for the cysteinyl leukotrienes.
Icatibant is a selective competitive antagonist
of the bradykinin [[beta].sub.2], receptor.
Pregnenolone has also been demonstrated to partially protect against memory deficits, induced by the administration of an N-Methyl-D-aspartale (NMDA) receptor competitive antagonist
. (12) These receptors play key roles in learning and memory, (13),(14),(15) in excitatory synaptic transmission, (16) as well as in the central regulation of bodily functions.
Exposure to 10 [micro]M SB-710411 causes a significant shift in the agonist concentration-response curve with no suppression of the [E.sub.max], suggesting that it acts as a competitive antagonist
. In contrast, SB-710411 did not alter the contractile efficacy of angiotensin-II, phenylephrine, or KCl, although it potentiated the contractile response to endothelin-1 in the isolated rat aorta.
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.
Flumazenil is a competitive antagonist
at the benzodiazepine receptor with duration of action varying from 140 to 250 minutes.
The IL-1 family (8) comprises 3 members: IL-1A and IL-1B, which act as proinflammatory agonists, and their competitive antagonist
, the IL-1 receptor antagonist (IL-1RA).
NK4 is an elastase-generated fragment of hepatocyte growth factor (HGF) containing four kringle domains, initially discovered as a competitive antagonist