From Wikipedia, the free encyclopedia
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), iclepertin (BI-425809), ORG-24598, ORG-25935, ALX-5407, and sarcosine, which are selective GlyT1 blockers, and ORG-25435 and N-arachidonylglycine, which are selective GlyT2 blockers.[1][2] Some weak and/or non-selective GlyT blockers include amoxapine and ethanol (alcohol).[3]
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Receptor (ligands) | GlyRTooltip Glycine receptor |
- Positive modulators: Alcohols (e.g., brometone, chlorobutanol (chloretone), ethanol (alcohol), tert-butanol (2M2P), tribromoethanol, trichloroethanol, trifluoroethanol)
- Alkylbenzene sulfonate
- Anandamide
- Barbiturates (e.g., pentobarbital, sodium thiopental)
- Chlormethiazole
- D12-116
- Dihydropyridines (e.g., nicardipine)
- Etomidate
- Ginseng constituents (e.g., ginsenosides (e.g., ginsenoside-Rf))
- 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
- Tropeines (e.g., atropine, bemesetron, cocaine, LY-278584, 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
- Antagonists: 2-Aminostrychnine
- 2-Nitrostrychnine
- 4-Phenyl-4-formyl-N-methylpiperidine
- αEMBTL
- Bicuculline
- Brucine
- Cacotheline
- Caffeine
- Colchicine
- Colubrine
- Cyanotriphenylborate
- Dendrobine
- Diaboline
- Endocannabinoids (e.g., 2-AG, anandamide (AEA))
- Gaboxadol (THIP)
- Gelsemine
- iso-THAZ
- Isobutyric acid
- Isonipecotic acid
- Isostrychnine
- Laudanosine
- N-Methylbicuculline
- N-Methylstrychnine
- N,N-Dimethylmuscimol
- Nipecotic acid
- Pitrazepin
- Pseudostrychnine
- Quinolines (e.g., 4-hydroxyquinoline, 4-hydroxyquinoline-3-carboxylic acid, 5,7-CIQA, 7-CIQ, 7-TFQ, 7-TFQA)
- RU-5135
- Sinomenine
- Strychnine
- Thiocolchicoside
- Tutin
- Negative modulators: Amiloride
- Benzodiazepines (e.g., bromazepam, clonazepam, diazepam, flunitrazepam, flurazepam)
- Corymine
- Cyanotriphenylborate
- Daidzein
- Dihydropyridines (e.g., nicardipine, nifedipine, nitrendipine)
- Furosemide
- Genistein
- Ginkgo constituents (e.g., bilobalide, ginkgolides (e.g., ginkgolide A, ginkgolide B, ginkgolide C, ginkgolide J, ginkgolide M))
- Imipramine
- NBQX
- Neuroactive steroids (e.g., 3α-androsterone sulfate, 3β-androsterone sulfate, deoxycorticosterone, DHEA sulfate, pregnenolone sulfate, progesterone)
- Opioids (e.g., codeine, dextromethorphan, dextrorphan, levomethadone, levorphanol, morphine, oripavine, pethidine, thebaine)
- Picrotoxin (i.e., picrotin and picrotoxinin)
- PMBA
- Riluzole
- Tropeines (e.g., bemesetron, LY-278584, tropisetron, zatosetron)
- Verapamil
- Zinc
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NMDARTooltip N-Methyl-D-aspartate receptor | |
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Transporter (blockers) | GlyT1Tooltip Glycine transporter 1 | |
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GlyT2Tooltip Glycine transporter 2 | |
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