Lesogaberan is a potent and selective agonist of the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant GABAB receptors. This compound shows high affinity for rat GABAB receptors with a Ki value of 5.1 nM, while demonstrating a lower affinity for GABAA receptors at 1.4 μM. Lesogaberan is primarily utilized in research to investigate its effects on transient lower esophageal sphincter relaxation through its peripheral action, making it a valuable tool in studies related to gastrointestinal function and pharmacology.
Lesogaberan is a potent and selective agonist of the GABAB receptor, exhibiting an EC50 of 8.6 nM for human recombinant GABAB receptors. This compound shows high affinity for rat GABAB receptors with a Ki value of 5.1 nM, while demonstrating a lower affinity for GABAA receptors at 1.4 μM. Lesogaberan is primarily utilized in research to investigate its effects on transient lower esophageal sphincter relaxation through its peripheral action, making it a valuable tool in studies related to gastrointestinal function and pharmacology.
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