TY - JOUR
T1 - Glycine transport inhibitors for the treatment of pain
AU - Vandenberg, Robert J.
AU - Ryan, Renae M
AU - Carland, Jane E.
AU - Imlach, Wendy L.
AU - Christie, Macdonald J
PY - 2014/8
Y1 - 2014/8
N2 - Opioids, local anesthetics, anticonvulsant drugs, antidepressants, and non-steroidal anti-inflammatory drugs (NSAIDs) are used to provide pain relief but they do not provide adequate pain relief in a large proportion of chronic pain patients and are often associated with unacceptable side effects. Inhibitory glycinergic neurotransmission is impaired in chronic pain states, and this provides a novel target for drug development. Inhibitors of the glycine transporter 2 (GlyT2) enhance inhibitory neurotransmission and show particular promise for the treatment of neuropathic pain. N-arachidonyl-glycine (NAGly) is an endogenous lipid that inhibits glycine transport by GlyT2 and also shows potential as an analgesic, which may be further exploited in drug development. In this review we discuss the role of glycine neurotransmission in chronic pain and future prospects for the use of glycine transport inhibitors in the treatment of pain.
AB - Opioids, local anesthetics, anticonvulsant drugs, antidepressants, and non-steroidal anti-inflammatory drugs (NSAIDs) are used to provide pain relief but they do not provide adequate pain relief in a large proportion of chronic pain patients and are often associated with unacceptable side effects. Inhibitory glycinergic neurotransmission is impaired in chronic pain states, and this provides a novel target for drug development. Inhibitors of the glycine transporter 2 (GlyT2) enhance inhibitory neurotransmission and show particular promise for the treatment of neuropathic pain. N-arachidonyl-glycine (NAGly) is an endogenous lipid that inhibits glycine transport by GlyT2 and also shows potential as an analgesic, which may be further exploited in drug development. In this review we discuss the role of glycine neurotransmission in chronic pain and future prospects for the use of glycine transport inhibitors in the treatment of pain.
KW - glycine transport inhibitors
KW - glycine transporter 2
KW - neuropathic pain
UR - http://www.scopus.com/inward/record.url?scp=84905489379&partnerID=8YFLogxK
U2 - 10.1016/j.tips.2014.05.006
DO - 10.1016/j.tips.2014.05.006
M3 - Review Article
C2 - 24962068
AN - SCOPUS:84905489379
SN - 0165-6147
VL - 35
SP - 423
EP - 430
JO - Trends in Pharmacological Sciences
JF - Trends in Pharmacological Sciences
IS - 8
ER -