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),
Org 24598,
Org 25935,
ALX-5407, and
sarcosine, which are selective
GlyT1
blockers, and
Org 25543 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
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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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