A mutation in the second transmembrane region of the CB1 receptor selectively disrupts G protein signaling and prevents receptor internalization.

@article{Roche1999AMI,
  title={A mutation in the second transmembrane region of the CB1 receptor selectively disrupts G protein signaling and prevents receptor internalization.},
  author={John P. Roche and S. Bounds and Stephen Brown and Kenneth Mackie},
  journal={Molecular pharmacology},
  year={1999},
  volume={56 3},
  pages={611-8}
}
We mutated a conserved aspartate in the second transmembrane domain of the cannabinoid CB(1) receptor to asparagine (D164N), stably transfected it into AtT20 cells, and examined the coupling of this mutant receptor to several intracellular effectors that are targets of wild-type CB(1) receptor activation. We found that the D164N receptor binds the CB(1) agonist WIN 55,212-2 with an affinity matching that of the wild-type CB(1) receptor and inhibits Ca(2+) currents and cAMP production with an… CONTINUE READING

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activation of the serotonin 5-HT2A receptor

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