Martin Davies¹, Alan N. Bateson^1,2 and Susan M. J. Dunn^1,2

¹ Department of Pharmacology

²Division of Neuroscience, Faculty of Medicine, University of Alberta, Edmonton, Alberta, Canada T6G 2H7

Received 07/16/96; Accepted 07/22/96; On-line 09/01/96

1. Abstract

2. Introduction

3. Mutational analysis of ligand-gated ion channels: General considerations

4. Mutational analysis of ligand binding domains in the GABA_A receptor

4.1.The nicotinic acetylcholine receptor: A receptor prototype

4.2.GABA recognition site(s)

4.2.1. Residues implicated in GABA binding

4.2.2. Investigation of a role for a conserved disulfide loop

4.2.3. A role for aromatic and hydroxylated amino acid residues

4.2.4. Other GABA binding proteins

4.3. Benzodiazepine recognition site(s)

4.3.1. Importance of the alpha subunit(s)

4.3.2. Importance of the gamma subunit(s)

4.4. Identification of a single residue conferring high affinity loreclezole binding

5. Mutational analysis of the channel forming region of the GABA_A receptor

6. Mutational analysis of post-translational modifications of the GABA_A receptor

6.1. Phosphorylation sites

6.2. Glycosylation sites

7. Recent models of GABA_A receptor structure and function

8. Conclusions

9. Acknowledgments

10. References

11. Entire manuscript

Keywords: molecular pharmacology; brain; ligand-gated ion channels; GABA_A receptor; mutagenesis