Key result
The biphenylimidazole derivative L-162,313 acts as a high-affinity partial agonist on the AT1 receptor, stimulating phosphoinositide hydrolysis with an EC50 of 33 ± 11 nM.
Population
COS-7 cells transfected with rat AT1 receptor, stably transfected Chinese hamster ovary cells, Xenopus…
Comparison
L-162,313 (a biphenylimidazole derivative) vs Angiotensin II, untransfected cells, and…
Design
Preclinical
Authors
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May serve as preclinical AT1 partial agonist probe; leaves open whether non-peptide agonists can be translated clinically.
Effect estimate: EC50 33 ± 11 nM
A subset of biphenylimidazole compounds, such as L-162,313, can act as high affinity partial agonists on the AT1 receptor with distinct molecular interactions compared to peptide agonists and non-peptide antagonists.
Perlman et al. (1995) studied this question. L-162,313 vs. Angiotensin II was evaluated on Phosphoinositide hydrolysis stimulation (EC50 33 ± 11 nM). The biphenylimidazole derivative L-162,313 acts as a high-affinity partial agonist on the AT1 receptor, stimulating phosphoinositide hydrolysis with an EC50 of 33 ± 11 nM.
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