Picrotoxin-like channel blockers of GABAA receptors

doi:10.1073/pnas.0601121103

Comment

. 2006 Apr 18;103(16):6081-2.

doi: 10.1073/pnas.0601121103. Epub 2006 Apr 10.

Picrotoxin-like channel blockers of GABAA receptors

Richard W Olsen¹

Affiliations

Affiliation

¹ Department of Molecular and Medical Pharmacology, Geffen School of Medicine, University of California, Los Angeles, CA 90095-1735, USA. rolsen@mednet.ucla.edu

PMID: 16606858
PMCID: PMC1458832
DOI: 10.1073/pnas.0601121103

Comment

Picrotoxin-like channel blockers of GABAA receptors

Richard W Olsen. Proc Natl Acad Sci U S A. 2006.

. 2006 Apr 18;103(16):6081-2.

doi: 10.1073/pnas.0601121103. Epub 2006 Apr 10.

Author

Richard W Olsen¹

Affiliation

¹ Department of Molecular and Medical Pharmacology, Geffen School of Medicine, University of California, Los Angeles, CA 90095-1735, USA. rolsen@mednet.ucla.edu

PMID: 16606858
PMCID: PMC1458832
DOI: 10.1073/pnas.0601121103

No abstract available

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Conflict of interest statement

Conflict of interest statement: No conflicts declared.

Figures

**Fig. 1.**
Schematic view of the GABA_A receptor–chloride channel and its blocker picrotoxinin. (A) Chemical structure of picrotoxinin. (B) Structure of a cys-loop ligand-gated ion channel receptor. Schematic view of a native GABAR heteropentamer, with the channel in the center, formed of two copies of an α subunit (α1–α6), two copies of a β subunit (β1, β2, or β3), and one additional type, like γ2 or δ. (C) Cytoplasmic end of the TM2/channel α-helix for two β3 subunits (black dots in B; the other three subunits are not shown) in GABAR, showing the PTX site residues near 2′–9′ (residues are numbered 1′–23′ from the N-terminal bottom of the helix to the C-terminal extracellular end of the helix).

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Comment on

Structural model for gamma-aminobutyric acid receptor noncompetitive antagonist binding: widely diverse structures fit the same site.
Chen L, Durkin KA, Casida JE. Chen L, et al. Proc Natl Acad Sci U S A. 2006 Mar 28;103(13):5185-90. doi: 10.1073/pnas.0600370103. Epub 2006 Mar 10. Proc Natl Acad Sci U S A. 2006. PMID: 16537435 Free PMC article.

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References

1. Martin D. L., Olsen R. W., editors. GABA in the Nervous System. Philadelphia: Lippincott Williams & Wilkins; 2000.
1. Chen L., Durkin K. A., Casida J. E. Proc. Natl. Acad. Sci. USA. 2006;103:5185–5190. - PMC - PubMed
1. Porter L. A. Chem. Rev. Washington, DC: 1967. pp. 441–464. - PubMed
1. Olsen R. W., Gordey M. In: Handbook of Experimental Pharmacology, Pharmacology of Ionic Channel Function: Activators and Inhibitors. Endo M., Kurachi Y., Mishina M., editors. Vol. 147. Heidelberg: Springer; 2000. pp. 497–515.
1. Windholz M., Budavari S., Stroumtsos L. Y., Fertig M. N., editors. The Merck Index. 9th Ed. Rahway, NJ: Merck; 1976.

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[1] Martin D. L., Olsen R. W., editors. GABA in the Nervous System. Philadelphia: Lippincott Williams & Wilkins; 2000.

[2] Martin D. L., Olsen R. W., editors. GABA in the Nervous System. Philadelphia: Lippincott Williams & Wilkins; 2000.

[3] Chen L., Durkin K. A., Casida J. E. Proc. Natl. Acad. Sci. USA. 2006;103:5185–5190. - PMC - PubMed

[4] Chen L., Durkin K. A., Casida J. E. Proc. Natl. Acad. Sci. USA. 2006;103:5185–5190. - PMC - PubMed

[5] Porter L. A. Chem. Rev. Washington, DC: 1967. pp. 441–464. - PubMed

[6] Porter L. A. Chem. Rev. Washington, DC: 1967. pp. 441–464. - PubMed

[7] Olsen R. W., Gordey M. In: Handbook of Experimental Pharmacology, Pharmacology of Ionic Channel Function: Activators and Inhibitors. Endo M., Kurachi Y., Mishina M., editors. Vol. 147. Heidelberg: Springer; 2000. pp. 497–515.

[8] Olsen R. W., Gordey M. In: Handbook of Experimental Pharmacology, Pharmacology of Ionic Channel Function: Activators and Inhibitors. Endo M., Kurachi Y., Mishina M., editors. Vol. 147. Heidelberg: Springer; 2000. pp. 497–515.

[9] Windholz M., Budavari S., Stroumtsos L. Y., Fertig M. N., editors. The Merck Index. 9th Ed. Rahway, NJ: Merck; 1976.

[10] Windholz M., Budavari S., Stroumtsos L. Y., Fertig M. N., editors. The Merck Index. 9th Ed. Rahway, NJ: Merck; 1976.

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Picrotoxin-like channel blockers of GABAA receptors

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