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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References

SHOWING 1-10 OF 19 REFERENCES
Functional characterization of the recombinant human 5-hydroxytryptamine7(a) receptor isoform coupled to adenylate cyclase stimulation.
  • 83
  • Highly Influential
  • PDF
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
  • 482
  • Highly Influential
The human 5‐HT7 serotonin receptor splice variants: constitutive activity and inverse agonist effects
  • 88
  • Highly Influential
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
  • 35
  • Highly Influential
Cloning, expression and pharmacology of a truncated splice variant of the human 5‐HT7 receptor (h5‐HT7(b))
  • 115
  • Highly Influential
Functional characterisation of the human cloned 5‐HT7 receptor (long form); antagonist profile of SB‐258719
  • 118
Differential Agonist-Mediated Internalization of the Human 5-Hydroxytryptamine 7 Receptor Isoforms
  • 41
  • PDF
Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors.
  • 45
  • Highly Influential
Functional, molecular and pharmacological advances in 5-HT7 receptor research.
  • 288
  • PDF
Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs
  • 25
  • Highly Influential
...
1
2
...