Characterisation of 5-HT3 recognition sites in membranes of NG 108-15 neuroblastoma-glioma cells with [3H]ICS 205-930

@article{Neijt1988CharacterisationO5,
  title={Characterisation of 5-HT3 recognition sites in membranes of NG 108-15 neuroblastoma-glioma cells with [3H]ICS 205-930},
  author={Hans Ch Neijt and Angela Karpf and Philippe Schoeffter and G{\"u}nter Engel and Daniel Hoyer},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={1988},
  volume={337},
  pages={493-499}
}
  • H. NeijtA. Karpf D. Hoyer
  • Published 1 May 1988
  • Biology, Chemistry
  • Naunyn-Schmiedeberg's Archives of Pharmacology
Summary1.The binding characteristics of [3H]ICS 205-930, a potent and selective 5-hydroxytryptamine 5-HT3 receptor antagonist, were investigated in membranes prepared from murine neuroblastoma-glioma NG 108-15 cells.2.[3H]ICS 205-930 bound rapidly, reversibly and stereoselectively to a homogeneous population of high affinity recognition sites: Bmax = 58 ± 3 fmol/mg protein, pKD = 9.01 ± 0.08 (n = 11). Non linear regression and Scatchard analysis of saturation data suggested the existence of a… 

[3H]ICS 205-930 labels 5-HT3 recognition sites in membranes of cat and rabbit vagus nerve and superior cervical ganglion

It is demonstrated that [3H]ICS 205-930 identifies 5-HT3 receptors in preparations of cat and rabbit vagus nerve and superior cervical ganglion and their rank order of affinity for 5- HT3 receptors from neuroblastoma-glioma NG 108-15 cells.

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Both selective agonists and antagonists will be considered as well as a number of their radiolabeled counterparts as tools to identify 5-HT3 receptors and their properties.

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Competitive in nature, as demonstrated by saturation experiments carried out with [3H]ICS 205-930 in the presence and the absence of unlabeled compounds: apparent Bmax values were not reduced, whereas apparent KD values were increased inThe presence of competing ligands.

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  • Biology, Chemistry
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