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

@article{Neijt2004CharacterisationO5,
  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={2004},
  volume={337},
  pages={493-499}
}
  • H. Neijt, A. Karpf, +2 authors D. Hoyer
  • Published 1 May 1988
  • Chemistry, Medicine
  • 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
TLDR
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.
Common pharmacological and physico-chemical properties of 5-HT3 binding sites in the rat cerebral cortex and NG 108-15 clonal cells.
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The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons
TLDR
It is reported that this non-classical 5-HT receptor can be stimulated by 4-amino-5-chloro-2-methoxy substituted benzamide derivatives and is similar to the pharmacology of the high affinity 5- HT receptors involved in the indirect stimulation of smooth muscle in the guinea pig ileum.
Agonists and antagonists of 5-HT3 receptors
There can be little doubt that the basis of the recent remarkable advances in our understanding of the physiological and pathophysiological roles of 5-HT has been the identification and development
The effect of 5-HT3 receptor antagonists on the writhing response in mice.
  • P. Moser
  • Chemistry, Medicine
    General pharmacology
  • 1995
TLDR
Results show that 5-HT3 receptor antagonists can inhibit writhes induced by a variety of compounds and this appears to be a local action, however, the inability of 2-methyl-5-HT to induce writhing and the high doses of antagonist required indicate that further studies are required to establish a role for 5- HT3 receptors in this effect.
Organization of the mouse 5-HT3 receptor gene and functional expression of two splice variants.
TLDR
No differences in electrophysiological characteristics, such as voltage dependence, desensitization kinetics, or unitary conductance were found between homomeric 5-HT3R-AS and 5- HT3 R-AL receptors.
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