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LY-2365109

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Inhibitor of the type 1 glycine transporter (GlyT1)

LY-2365109
Names

IUPAC name 2-[2-[4-(1,3-Benzodioxol-5-yl)-2-tert-butylphenoxy]ethyl-methylamino]acetic acid
Identifiers
CAS Number	hydrochoride: 868265-28-5
3D model (JSmol)	Interactive image
ChEMBL	ChEMBL1628564
ChemSpider	9727535
PubChem CID	11552757
InChI InChI=1S/C22H27NO5/c1-22(2,3)17-11-15(16-6-8-19-20(12-16)28-14-27-19)5-7-18(17)26-10-9-23(4)13-21(24)25/h5-8,11-12H,9-10,13-14H2,1-4H3,(H,24,25) Key: FKPLJWGRBCQLTL-UHFFFAOYSA-N
SMILES CC(C)(C)C1=C(C=CC(=C1)C2=CC3=C(C=C2)OCO3)OCCN(C)CC(=O)O
Properties
Chemical formula	C₂₂H₂₇NO₅
Molar mass	385.460 g·mol⁻¹
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). Infobox references

Chemical compound

LY-2365109 is aglycine reuptake inhibitor. It is able to inhibit thetype 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

[edit]

^Zhang, Jichun; Wu, Jin; Toyohara, Jun; Fujita, Yuko; Chen, Hongxian; Hashimoto, Kenji (2011)."Pharmacological characterization of [³H]CHIBA-3007 binding to glycine transporter 1 in the rat brain".PLOS ONE.6 (6) e21322.Bibcode:2011PLoSO...621322Z.doi:10.1371/journal.pone.0021322.ISSN 1932-6203.PMC 3121759.PMID 21731704.
^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.PMC 4655139.PMID 26302655.

Glycine receptor modulators

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

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 andpicrotoxinin)
PMBA
Riluzole
Tropeines (e.g.,bemesetron,LY-278584,tropisetron,zatosetron)
Verapamil
Zinc

NMDARTooltip N-Methyl-D-aspartate receptor

Seehere instead.

Transporter
(blockers)

GlyT1Tooltip Glycine transporter 1	ACPPB ALX-5407 (NFPS) ASP2535 Bitopertin (RG1678/RO4917838) CP-802079 Ethanol (alcohol) Glycyldodecylamide GSK1018921 Iclepertin LY-2365109 Mardepodect ORG-24598 ORG-25935 (SCH-900435) Pesampator (BIIB-104, PF-04958242) PF-03463275 Sarcosine SNG-12 (Synapsinae) SSR-103,800 SSR-504,734 Tilapertin
GlyT2Tooltip Glycine transporter 2	ALX-1393 Amoxapine Ethanol (alcohol) NAGly Opiranserin (VVZ-149) ORG-25543 VVZ-368

See also: Receptor/signaling modulators; GABA receptor modulators; GABA_A receptor positive modulators; Ionotropic glutamate receptor modulators

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