Neurochemicals for the investigation of GABA(C) receptors.
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Johnston GA, Chebib M, Hanrahan JR, Mewett KN
Neurochemicals for the investigation of GABA(C) receptors.
Neurochem Res. 2010 Dec;35(12):1970-7. doi: 10.1007/s11064-010-0271-7. Epub 2010 Oct 21.
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- 20963487 [ View in PubMed]
- Abstract
GABA(C) 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 GABA(C) 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 GABA(C) 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 rho1 and rho2 GABA(C) receptors (2-methyl-TACA and cyclothiazide) are also covered. Given their less widespread distribution, lower abundance and relative structural simplicity compared to GABA(A) and GABA(B) receptors, GABA(C) receptors are attractive drug targets.
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