Tilapertin

Chemical compound

  • None
Legal statusLegal status
  • Investigational
Identifiers
  • (4-{(R)-Phenyl[3-(trifluoromethyl)phenyl]methyl}-1-piperazinyl)acetic acid
CAS Number
  • 1000690-85-6
PubChem CID
  • 25063875
ChemSpider
  • 32699053
UNII
  • A2SV488G98
KEGG
  • D10672 checkY
CompTox Dashboard (EPA)
  • DTXSID801032317 Edit this at Wikidata
Chemical and physical dataFormulaC20H21F3N2O2Molar mass378.395 g·mol−13D model (JSmol)
  • Interactive image
  • c1ccc(cc1)[C@H](c2cccc(c2)C(F)(F)F)N3CCN(CC3)CC(=O)O
InChI
  • 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

Tilapertin appears to act via the blocking of the type 1 glycine transporter,[3] making it a glycine re-uptake inhibitor.

History

Two studies have been made in order to determine the safety of tilapertin 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]

See also

  • Bitopertin

References

  1. ^ "Tilapertin". PubChem. U.S. National Library of Medicine. Retrieved 2024-08-16.
  2. ^ World Health Organization (2013). "International Nonproprietary Names for Pharmaceutical Substances (INN): Proposed INN: List 110" (PDF). WHO Drug Information. 27 (4). World Health Organization.
  3. ^ a b Dunayevich E, Buchanan RW, Chen CY, Yang J, Nilsen J, Dietrich JM, et al. (April 2017). "Efficacy and safety of the glycine transporter type-1 inhibitor AMG 747 for the treatment of negative symptoms associated with schizophrenia". Schizophrenia Research. 182: 90–97. doi:10.1016/j.schres.2016.10.027. PMID 27789188.
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Typical
DisputedAtypicalOthers
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Simple piperazines
(no additional rings)
Phenylpiperazines
Benzylpiperazines
Diphenylalkylpiperazines
(benzhydrylalkylpiperazines)
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclics
(piperazine attached via side chain)
Others/Uncategorized
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Receptor
(ligands)
GlyRTooltip Glycine receptor
NMDARTooltip N-Methyl-D-aspartate receptor
  • See here instead.
Transporter
(blockers)
GlyT1Tooltip Glycine transporter 1
GlyT2Tooltip Glycine transporter 2
See also
Receptor/signaling modulators
GABA receptor modulators
GABAA receptor positive modulators
Ionotropic glutamate receptor modulators
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