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					Type 1 Glycine transporter inhibitor
ASP2535
 
 
Names
  
IUPAC name 
4-[3-(6-phenylpyridin-3-yl)-5-propan-2-yl-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole
 
Identifiers
  
 
  
 
 
ChEMBL 
 
 
 
UNII 
 
InChI=1S/C22H18N6O/c1-14(2)21-24-25-22(28(21)19-10-6-9-18-20(19)27-29-26-18)16-11-12-17(23-13-16)15-7-4-3-5-8-15/h3-14H,1-2H3
Key: FQGLDGKVKDPVLO-UHFFFAOYSA-N
 
 
CC(C)C1=NN=C(N1C2=CC=CC3=NON=C32)C4=CN=C(C=C4)C5=CC=CC=C5
 
 
Properties
  
 
C 22 H 18 N 6 O 
 
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
ASP2535  is an inhibitor of the type 1 glycine transporter .[ 1] Alzheimer's disease  and schizophrenia .
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] 
^ a b   Harada, Katsuya; Nakato, Kazuhiro; Yarimizu, Junko; Yamazaki, Mayako; Morita, Masahiko; Takahashi, Shinji; Aota, Masaki; Saita, Kyoko; Doihara, Hitoshi; Sato, Yuichiro; Yamaji, Takayuki; Ni, Keni; Matsuoka, Nobuya (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 .   
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 THAZ 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  and picrotoxinin )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