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The antagonist properties of S 11978 on 5HT 3 receptors in N1E‐115 neuroblastoma cells
Author(s) -
Morain P.,
Abraham C.,
Lacoste JM,
Malen C.,
Laubie M.,
GiesenCrouse E.
Publication year - 1993
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/j.1472-8206.1993.tb00233.x
Subject(s) - antagonist , 5 ht receptor , radioligand , receptor , quipazine , neuroblastoma , chemistry , receptor antagonist , serotonin , pharmacology , stereochemistry , biophysics , cell culture , biology , biochemistry , genetics
Summary— The effects of the novel antagonist S 11978 (Endo‐7‐[(8‐methyl‐8‐azabicyclo[3,2,1]‐3‐octyl)oxycarbonyl] benzo[b] thiophene) on 5HT 3 receptors were examined in N1E‐115 mouse neuroblastoma x rat glioma hybrid cells, with radioligand binding and whole cell patch clamp techniques. The 5HT 3 receptor ligand [ 3 H] quipazine was displaced by ICS 205–930, GR 38032F and S 11978 with K I values of 2.25 nM, 36.5 nM and 1.75 nM respectively. Electrophysiological studies showed that S 11978 is a potent 5HT 3 antagonist: IC 50 values for inhibition of 5HT‐induced inward current by ICS 205–930, GR 38032F and S 11978 were 0.22 nM, 0.63 nM and 0.43 nM respectively at a holding potential of‐65 mV. It is concluded that S 11978 is a potent, high affinity 5HT 3 receptor antagonist.