Add time:08/21/2019         Source:sciencedirect.com

In radioligand binding experiments, MDL 73147EF and MDL 74156 (cas 127951-99-9) inhibited the binding of [3H]GR65630 to 5-hydroxytryptamine3 (5-HT3) binding sites on membranes prepared from NG108-15 neuroblastoma × glioma cells. The calculated dissociation constants (KI) were 20.03 ± 6.58 and 0.44 ± 0.18 nM, respectively (means ± S.E.M., n = 6 and 9, respectively). Application of 5-HT (10–50 μM) to voltage-clamped NG108-15 cells elicited a rapidly desensitizing inward membrane current, characteristic for the activation of 5-HT3 receptors. The 5-HT-induced membrane current was suppressed in a reversible, concentration-dependent manner by MDL 73147EF and MDL 74156EF. The concentrations required to block half the 5-HT response (IC50) were 3.8 and 0.1 nM, respectively. It is concluded that both compounds are potent and reversible antagonists at 5-HT3 receptors in this neuroblastoma cell line.

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