Neurochemical Research

, Volume 35, Issue 12, pp 1970–1977

Neurochemicals for the Investigation of GABAC Receptors

  • Graham A. R. Johnston
  • Mary Chebib
  • Jane R. Hanrahan
  • Kenneth N. Mewett
ORIGINAL PAPER

DOI: 10.1007/s11064-010-0271-7

Cite this article as:
Johnston, G.A.R., Chebib, M., Hanrahan, J.R. et al. Neurochem Res (2010) 35: 1970. doi:10.1007/s11064-010-0271-7

Abstract

GABAC receptors are being investigated for their role in many aspects of nervous system function including memory, myopia, pain and sleep. There is evidence for functional GABAC receptors in many tissues such as retina, hippocampus, spinal cord, superior colliculus, pituitary and the gut. This review describes a variety of neurochemicals that have been shown to be useful in distinguishing GABAC receptors from other receptors for the major inhibitory neurotransmitter GABA. Some selective agonists (including (+)-CAMP and 5-methyl-IAA), competitive antagonists (such as TPMPA, (±)-cis-3-ACPBPA and aza-THIP), positive (allopregnanolone) and negative modulators (epipregnanolone, loreclezole) are described. Neurochemicals that may assist in distinguishing between homomeric ρ1 and ρ2 GABAC receptors (2-methyl-TACA and cyclothiazide) are also covered. Given their less widespread distribution, lower abundance and relative structural simplicity compared to GABAA and GABAB receptors, GABAC receptors are attractive drug targets.

Keywords

GABA GABAC TPMPA Allopregnanolone Loreclezole Cyclothiazide 

Abbreviations

Aza-THIP

4,5,6,7-tetrahydropyrazolo[3,4-c]pyridin-3-ol

CACA

cis-4-aminocrotonic acid

(+)-CAMP

(1S,2R)-2-aminomethylcyclopropanecarboxylic acid

(±)-cis-3-ACPBPA

(±)-cis-(3-aminocyclopentanyl)butylphosphinic acid

5-Me-IAA

5-methyl-1H-imidazole-4-acetic acid

2-Methyl-TACA

trans-4-amino-2-methylbut-2-enoic acid

P4MPA

(piperidin-4-yl)methylphosphinic acid

SGS742

(3-aminopropyl)-n-butylphosphinic acid

THIP

4,5,6,7-tetrahydroisolazolo[5,4-c]pyridin-3-ol

TPMPA

(1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid

Copyright information

© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  • Graham A. R. Johnston
    • 1
  • Mary Chebib
    • 2
  • Jane R. Hanrahan
    • 2
  • Kenneth N. Mewett
    • 1
  1. 1.Adrien Albert Laboratory of Medicinal Chemistry, Department of Pharmacology D06The University of SydneySydneyAustralia
  2. 2.Faculty of Pharmacy A15The University of SydneySydneyAustralia