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

  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},
  • 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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Brain serotonin subsystem complexity and receptor heterogeneity: therapeutic potential of selective serotonin agonists and antagonists.

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  • J. Fozard
  • Biology
    Naunyn-Schmiedeberg's Archives of Pharmacology
  • 2004
MDL 72222 is the first reported selective and potent antagonist of responses mediated through the 5-HT receptors present on the terminal sympathetic neurones of the rabbit heart and on the neurones subserving the afferent limb of the Bezold-Jarisch reflex.

Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine

Neuronal 5-HT receptors in the periphery

  • J. Fozard
  • Biology, Chemistry
  • 1984

The depolarizing action of 5‐hydroxytryptamine on rabbit vagal afferent and sympathetic neurones in vitro and its selective blockade by ICS 205–930

This study provides quantitative evidence on the blocking action of ICS 205–930 at neuronal 5‐HT receptors using a technique that allows the depolarizing responses evoked by the amine to be directly recorded.