ASP2535 is an inhibitor of the type 1 glycine transporter.[1] It could potentially be used in treatment of Alzheimer's disease and schizophrenia.
Potential uses
ASP2535 has been investigated for the treatment of Alzheimer's disease and schizophrenia, it is able to inhibit the memory deficit induced by scopolamine, an anticholinergic agent.[1]
References
- ↑ 1.0 1.1 Harada, Katsuya; Nakato, Kazuhiro; Yarimizu, Junko; Yamazaki, Mayako; Morita, Masahiko; Takahashi, Shinji; Aota, Masaki; Saita, Kyoko et al. (2012-06-15). "A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease". European Journal of Pharmacology 685 (1–3): 59–69. doi:10.1016/j.ejphar.2012.04.013. ISSN 1879-0712. PMID 22542656.
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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/ASP2535. Read more |
