A glycine reuptake inhibitor (GRI ) is a type of drug which inhibits the reuptake of the neurotransmitter glycine by blocking one or more of the glycine transporters (GlyTs). Examples of GRIs include bitopertin (RG1678), , Org 25935 , , and sarcosine , which are selective GlyT1 blockers , and and N-arachidonylglycine , which are selective GlyT2 blockers.[1] [2] Some weak and/or non-selective GlyT blockers include amoxapine and ethanol (alcohol ).[3]
See also [ ]
References [ ]
^ Harsing LG, Juranyi Z, Gacsalyi I, Tapolcsanyi P, Czompa A, Matyus P (2006). "Glycine transporter type-1 and its inhibitors". Curr. Med. Chem . 13 (9): 1017–44. doi :10.2174/092986706776360932 . PMID 16611082 .
^ Harvey RJ, Yee BK (November 2013). "Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain". Nat Rev Drug Discov . 12 (11): 866–85. doi :10.1038/nrd3893 . PMID 24172334 .
^ Harald Sitte; Michael Freissmuth (2 August 2006). Neurotransmitter Transporters . Springer Science & Business Media. pp. 472–. ISBN 978-3-540-29784-0 .
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Receptor (ligands )
GlyR
Positive modulators: Alcohols (e.g., , chlorobutanol (chloretone) , ethanol (alcohol) , tert -butanol (2M2P) , tribromoethanol , trichloroethanol , trifluoroethanol )
Alkylbenzene sulfonate
Anandamide
Barbiturates (e.g., pentobarbital , sodium thiopental )
Chlormethiazole
Dihydropyridines (e.g., nicardipine )
Etomidate
Ginseng constituents (e.g., ginsenosides (e.g., ))
Glutamic acid (glutamate)
Ivermectin
Ketamine
Neuroactive steroids (e.g., alfaxolone , pregnenolone (eltanolone) , pregnenolone acetate , minaxolone , ORG-20599 )
Nitrous oxide
Penicillin G
Propofol
Tamoxifen
Tetrahydrocannabinol
Triclofos
(e.g., atropine , bemesetron , cocaine , , tropisetron , zatosetron )
Volatiles /gases (e.g., chloral hydrate , chloroform , desflurane , diethyl ether (ether) , enflurane , halothane , isoflurane , methoxyflurane , sevoflurane , toluene , trichloroethane (methyl chloroform) , trichloroethylene )
Xenon
Zinc
Negative modulators: Amiloride
Benzodiazepines (e.g., bromazepam , clonazepam , diazepam , flunitrazepam , flurazepam )
Daidzein
Dihydropyridines (e.g., nicardipine , nifedipine , nitrendipine )
Furosemide
Genistein
Ginkgo constituents (e.g., bilobalide , ginkgolides (e.g., , ginkgolide B , , , ))
Imipramine
NBQX
Neuroactive steroids (e.g., , , deoxycorticosterone , DHEA sulfate , pregnenolone sulfate , progesterone )
Opioids (e.g., codeine , dextromethorphan , dextrorphan , levomethadone , levorphanol , morphine , oripavine , pethidine , thebaine )
Picrotoxin (i.e., picrotin and picrotoxinin )
Riluzole
(e.g., bemesetron , , tropisetron , zatosetron )
Verapamil
Zinc
NMDAR
Transporter (blockers )
See also
Receptor/signaling modulators
GABA receptor modulators
GABAA receptor positive modulators
Ionotropic glutamate receptor modulators