LY-2365109 is a glycine reuptake inhibitor. It is able to inhibit the type 1 glycine transporter.[1] This inhibition increases extracellular levels of glycine. LY-2365109 has been shown to increase the seizure threshold in mice, meaning that this drug has potential as an anticonvulsant.[2]
References
- ↑ Zhang, Jichun; Wu, Jin; Toyohara, Jun; Fujita, Yuko; Chen, Hongxian; Hashimoto, Kenji (2011). "Pharmacological characterization of [³HCHIBA-3007 binding to glycine transporter 1 in the rat brain"]. PLOS ONE 6 (6). doi:10.1371/journal.pone.0021322. ISSN 1932-6203. PMID 21731704. Bibcode: 2011PLoSO...621322Z.
- ↑ Shen, Hai-Ying; van Vliet, Erwin A.; Bright, Kerry-Ann; Hanthorn, Marissa; Lytle, Nikki K.; Gorter, Jan; Aronica, Eleonora; Boison, Detlev (December 2015). "Glycine transporter 1 is a target for the treatment of epilepsy". Neuropharmacology 99: 554–565. doi:10.1016/j.neuropharm.2015.08.031. ISSN 1873-7064. PMID 26302655.
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Receptor
(ligands) | | GlyR |
- 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
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| NMDAR | |
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Transporter
(blockers) | |
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 | Original source: https://en.wikipedia.org/wiki/LY-2365109. Read more |
