Neurochemicals for the Investigation of GABAC Receptors
Neurochemicals for the Investigation of GABAC Receptors
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DOI：
10.1007/s11064-010-0271-7
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发表时间：
2010-12-01
影响因子：
4.4
通讯作者：
Mewett, Kenneth N.
中科院分区：
文献类型：
--
作者：
Johnston, Graham A. R.;Chebib, Mary;Mewett, Kenneth N.
GABA（C）受体在神经系统功能的许多方面，包括记忆，近视，疼痛和睡眠中的作用正在研究中。有证据表明在许多组织如视网膜、海马、脊髓、上级丘、垂体和肠道中存在功能性GABA（C）受体。本文综述了各种神经化学物质，已被证明是有用的，从其他受体的主要抑制性神经递质GABA的GABA（C）受体的区分。本文介绍了选择性激动剂（包括（+）-cAMP和5-甲基-IAA）、竞争性拮抗剂（如TPMPA、（+/-）-cis-3-ACPBPA和aza-THIP）、正性调节剂（别孕烯醇酮）和负性调节剂（表孕烯醇酮、洛瑞唑）。神经化学物质，可能有助于区分同型rho 1和rho 2 GABA（C）受体（2-甲基-TACA和环噻嗪）也包括在内。由于与GABA（A）和GABA（B）受体相比，GABA（C）受体的分布较不广泛、丰度较低和结构相对简单，因此GABA（C）受体是有吸引力的药物靶标。
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 rho 1 and rho 2 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.