Tilapertin

Tilapertin
Clinical data
ATC code	None;
Identifiers
	IUPAC name (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 ;
CompTox Dashboard (EPA)	DTXSID801032317 ;
Chemical and physical data
Formula	C20H21F3N2O2
Molar mass	378.395 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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]

References

^ "Tilapertin". PubChem. U.S. National Library of Medicine. Retrieved 2024-08-16.
^ World Health Organization (2013). "International Nonproprietary Names for Pharmaceutical Substances (INN): Proposed INN: List 110" (PDF). WHO Drug Information. 27 (4). World Health Organization.
^ ^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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[1] "Tilapertin". PubChem. U.S. National Library of Medicine. Retrieved 2024-08-16.

[WHO2013-2] World Health Organization (2013). "International Nonproprietary Names for Pharmaceutical Substances (INN): Proposed INN: List 110" (PDF). WHO Drug Information. 27 (4). World Health Organization.

[Dunayevich_2017-3] 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.

[1]

[2]

[3]

Tilapertin

Contents

Mechanism of action

History

See also

References

Clinical data

ATC code	None
Identifiers
IUPAC name (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^Y
CompTox Dashboard (EPA)	DTXSID801032317
Chemical and physical data
Formula	C₂₀H₂₁F₃N₂O₂
Molar mass	378.395 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES 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