Reanalysis of constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists

@article{Romero2006ReanalysisOC,
  title={Reanalysis of constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells demonstrates lack of silent properties for reported neutral antagonists},
  author={G. Romero and M. Pujol and P. Pauwels},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2006},
  volume={374},
  pages={31-39}
}
The present study reinvestigated a series of 5-HT receptor antagonists at both constitutively active rat and human 5-HT7(a) receptors in HEK-293F cells using the cAMP signalling pathway as a functional read-out. Both rat and human 5-HT7(a) receptors were expressed in similar amounts ([3H]-LSD binding: 1.0 to 1.1 pmol/mg protein). Attenuation of basal cAMP formation by the inverse agonist SB-691673 (1 μM) was slightly larger by the human 5-HT7(a) (−73±3 %) than rat 5-HT7(a) receptor (−62±3… Expand
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