Use of chimeric muscarinic receptors to investigate epitopes involved in allosteric interactions.

@article{Ellis1993UseOC,
  title={Use of chimeric muscarinic receptors to investigate epitopes involved in allosteric interactions.},
  author={John Ellis and Michael Seidenberg and Mark R. Brann},
  journal={Molecular pharmacology},
  year={1993},
  volume={44 3},
  pages={583-8}
}
All five (m1-m5) muscarinic receptors are sensitive to allosteric regulation, but gallamine is considerably more potent in slowing the dissociation of N-[3H]methylscopolamine (NMS) from the m2 subtype than from the m3 or m5 subtypes. To study the structural basis for the preference of gallamine for the m2 subtype, we evaluated [3H]NMS-gallamine interactions with chimeric receptors in which segments of the m5 receptor were systematically replaced with the corresponding m2 sequence. Substitutions… CONTINUE READING

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