Glycine receptor

Glycine

The glycine receptor (abbreviated as GlyR or GLR) is the receptor of the amino acid neurotransmitter glycine. GlyR is an ionotropic receptor that produces its effects through chloride currents. It is one of the most widely distributed inhibitory receptors in the central nervous system and has important roles in a variety of physiological processes, especially in mediating inhibitory neurotransmission in the spinal cord and brainstem.[1]

The receptor can be activated by a range of simple amino acids including glycine, β-alanine and taurine, and can be selectively blocked by the high-affinity competitive antagonist strychnine.[2] Caffeine is a competitive antagonist of GlyR.[3] Cannabinoids enhance the function.[4]

The protein Gephyrin has been shown to be necessary for GlyR clustering at inhibitory synapses.[5][6] GlyR is known to colocalize with the GABAA receptor on some hippocampal neurons.[5] Nevertheless, some exceptions can occur in the central nervous system where the GlyR α1 subunit and gephyrin, its anchoring protein, are not found in dorsal root ganglion neurons despite the presence of GABAA receptors.[7]

  1. ^ Lynch JW (October 2004). "Molecular structure and function of the glycine receptor chloride channel". Physiological Reviews. 84 (4): 1051–95. CiteSeerX 10.1.1.326.8827. doi:10.1152/physrev.00042.2003. PMID 15383648.
  2. ^ Rajendra S, Lynch JW, Schofield PR (1997). "The glycine receptor". Pharmacology & Therapeutics. 73 (2): 121–146. doi:10.1016/S0163-7258(96)00163-5. PMID 9131721.
  3. ^ Duan L, Yang J, Slaughter MM (August 2009). "Caffeine inhibition of ionotropic glycine receptors". The Journal of Physiology. 587 (Pt 16): 4063–75. doi:10.1113/jphysiol.2009.174797. PMC 2756438. PMID 19564396.
  4. ^ Xiong, Wei (2011). "Cannabinoid potentiation of glycine receptors contributes to cannabis-induced analgesia". Nature Chemical Biology. 7 (5): 296–303. doi:10.1038/nchembio.552. PMC 3388539. PMID 21460829.
  5. ^ a b Lévi S, Logan SM, Tovar KR, Craig AM (January 2004). "Gephyrin is critical for glycine receptor clustering but not for the formation of functional GABAergic synapses in hippocampal neurons". The Journal of Neuroscience. 24 (1): 207–17. doi:10.1523/JNEUROSCI.1661-03.2004. PMC 6729579. PMID 14715953.
  6. ^ Feng G, Tintrup H, Kirsch J, Nichol MC, Kuhse J, Betz H, Sanes JR (November 1998). "Dual requirement for gephyrin in glycine receptor clustering and molybdoenzyme activity". Science. 282 (5392): 1321–4. Bibcode:1998Sci...282.1321F. doi:10.1126/science.282.5392.1321. PMID 9812897.
  7. ^ Lorenzo LE, Godin AG, Wang F, St-Louis M, Carbonetto S, Wiseman PW, et al. (June 2014). "Gephyrin clusters are absent from small diameter primary afferent terminals despite the presence of GABA(A) receptors". The Journal of Neuroscience. 34 (24): 8300–17. doi:10.1523/JNEUROSCI.0159-14.2014. PMC 6608243. PMID 24920633.