ALX-1393 is a glycine reuptake inhibitor.
Pharmacodynamics
ALX-1393 works by inhibiting the action of GLYT2.[1] This causes elevated levels of glycine, an inhibitory neurotransmitter.
Potential uses
ALX-1393 has been shown to have potential as an analgesic. This is thought to be due to the elevated glycine levels reducing the transmission of the pain signals.[2]
Tests have shown that it was able to help reduce cancer pain in a potent way.[3]
References
- ↑ Eckle, V.-S.; Antkowiak, B. (2013-12-03). "ALX 1393 inhibits spontaneous network activity by inducing glycinergic tonic currents in the spinal ventral horn". Neuroscience 253: 165–171. doi:10.1016/j.neuroscience.2013.08.042. ISSN 1873-7544. PMID 23994185.
- ↑ Benito-Muñoz, Cristina; Perona, Almudena; Felipe, Raquel; Pérez-Siles, Gonzalo; Núñez, Enrique; Aragón, Carmen; López-Corcuera, Beatriz (2021-06-02). "Structural Determinants of the Neuronal Glycine Transporter 2 for the Selective Inhibitors ALX1393 and ORG25543". ACS Chemical Neuroscience 12 (11): 1860–1872. doi:10.1021/acschemneuro.0c00602. ISSN 1948-7193. PMID 34003005.
- ↑ Motoyama, Naoyo; Morita, Katsuya; Shiraishi, Seiji; Kitayama, Tomoya; Kanematsu, Takashi; Uezono, Yasuhito; Dohi, Toshihiro (October 2014). "Relief of cancer pain by glycine transporter inhibitors". Anesthesia and Analgesia 119 (4): 988–995. doi:10.1213/ANE.0000000000000388. ISSN 1526-7598. PMID 25076101.
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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/ALX-1393. Read more |
