Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor.

@article{Schwartz2003TherapeuticIO,
  title={Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor.},
  author={J. C. Schwartz and S{\'e}verine Morisset and Agn{\`e}s Rouleau and Xavier Ligneau and Florence Gbahou and Jo{\"e}l Tardivel-Lacombe and Holger Stark and Walter Schunack and C. Robin Ganellin and J. M. Arrang},
  journal={Journal of neural transmission. Supplementum},
  year={2003},
  volume={64},
  pages={1-16}
}
Some G-protein-coupled receptors display constitutive activity, that is spontaneous activity in the absence of agonist: a proportion of the receptor population adopts a conformation that can bind and activate G proteins. Whereas this was mainly shown to occur with recombinant or pathologically mutated receptors, the physiological relevance of the process has remained debated. We have adressed this question in the case of the histamine H3 receptor, a presynaptic inhibitory receptor regulating… CONTINUE READING

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