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Chemical compound
Tilapertin ATC code
(4-{(R)-Phenyl[3-(trifluoromethyl)phenyl]methyl}-1-piperazinyl)acetic acid
CAS Number PubChem CID ChemSpider UNII KEGG CompTox Dashboard (EPA ) Formula C 20 H 21 F 3 N 2 O 2 Molar mass 378.395 g·mol−1 3D model (JSmol )
c1ccc(cc1)[C@H](c2cccc(c2)C(F)(F)F)N3CCN(CC3)CC(=O)O
InChI=1S/C20H21F3N2O2/c21-20(22,23)17-8-4-7-16(13-17)19(15-5-2-1-3-6-15)25-11-9-24(10-12-25)14-18(26)27/h1-8,13,19H,9-12,14H2,(H,26,27)/t19-/m1/s1
Key:MDLQJNCGZVDZFV-LJQANCHMSA-N
Tilapertin (INN ), also known as AMG-747 ,[ 1] is a investigational drug which was being evaluated as an antipsychotic .[ 2]
Mechanism of action [ edit ]
Tilapertin appears to act via the blocking of the type 1 Glycine transporter ,[ 3] making it a Glycine re-uptake inhibitor .
Two studies have been made in order to determine the safety of AMG-747 and its potential as an add-on to anti-psychotic therapy in people with schizophrenia. These studies were later halted due to a case of Stevens–Johnson syndrome in one of the participants.[ 3]
Simple piperazines(no additional rings) Phenylpiperazines
2C-B-PP
3,4-CFP
Acaprazine
Antrafenine
Aripiprazole
Batoprazine
Bifeprunox
BRL-15,572
Ciprofloxacin
CSP-2503
Dapiprazole
DCPP
DMPP
Diphenylpiperazine
Dropropizine
EGIS-12,233
Elopiprazole
Eltoprazine
Enpiprazole
Ensaculin
Etoperidone
Flesinoxan
Fluanisone
Flibanserin
Fluprazine
Itraconazole
Ketoconazole
Levodropropizine
Lorpiprazole
mCPP
Mefway
MeOPP
Mepiprazole
Naftopidil
Naluzotan
Naphthylpiperazine
Nefazodone
Niaprazine
Oxypertine
Pardoprunox
pCPP
pFPP
Posaconazole
S-14,506
S-14,671
S-15,535
SB-258,585
SB-271,046
SB-357,134
SB-399,885
Sonepiprazole
TFMPP
Tolpiprazole
Trazodone
Urapidil
Vesnarinone
Vilazodone
Vortioxetine
WAY-100,135
WAY-100,635
Benzylpiperazines Diphenylalkylpiperazines (benzhydrylalkylpiperazines) Pyrimidinylpiperazines Pyridinylpiperazines Benzo(iso)thiazolyl piperazines Tricyclics (piperazine attached via side chain) Others/Uncategorized
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 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