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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
CC(C)(C)C1=C(C=CC(=C1)C2=CC3=C(C=C2)OCO3)OCCN(C)CC(=O)O
Properties
C 22 H 27 N O 5
Molar mass
−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
LY-2365109 is aglycine reuptake inhibitor .It is able to inhibit thetype 1 glycine transporter .[ 1] [ 2]
^ 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 .
Receptor (ligands )
GlyR Tooltip 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 andpicrotoxinin )PMBA Riluzole Tropeines (e.g.,bemesetron ,LY-278584 ,tropisetron ,zatosetron )Verapamil Zinc NMDAR Tooltip N-Methyl-D-aspartate receptor
Transporter (blockers )
GlyT1 Tooltip Glycine transporter 1 GlyT2 Tooltip Glycine transporter 2
