RO5256390

RO-5256390
Identifiers

IUPAC name (S)-4-((S)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine
CAS Number	1043495-96-0
PubChem CID	24963286
ChemSpider	34959936
ChEMBL	ChEMBL3684869
Chemical and physical data
Formula	C₁₃H₁₈N₂O
Molar mass	218.300 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES NC1=N[C@@H](C[C@@H](C2=CC=CC=C2)CC)CO1
InChI InChI=1S/C13H18N2O/c1-2-10(11-6-4-3-5-7-11)8-12-9-16-13(14)15-12/h3-7,10,12H,2,8-9H2,1H3,(H2,14,15)/t10-,12-/m0/s1 Key:IXDKFUBXESWHSL-JQWIXIFHSA-N

RO5256390 or RO-5256390 is a drug developed by Hoffmann-La Roche which acts as an agonist for the trace amine associated receptor 1 (TAAR1), which has been shown to block compulsive and binge-like eating behavior in rats. For this reason, it is being investigated as a potential drug to treat binge eating disorder.^[1] The drug shows robust aversive and locomotor-suppressing effects in rodents that are dependent on TAAR1 activation.^[2] Similar aversive effects have also been observed with other TAAR1 agonists like RO5263397 and RO5166017.^[2]^[3]

Reference section

^ Ferragud A, Howell AD, Moore CF, Ta TL, Hoener MC, Sabino V, Cottone P (June 2017). "The Trace Amine-Associated Receptor 1 Agonist RO5256390 Blocks Compulsive, Binge-like Eating in Rats". Neuropsychopharmacology. 42 (7): 1458–1470. doi:10.1038/npp.2016.233. PMC 5436108. PMID 27711047.
^ ^a ^b Shabani S, Houlton S, Ghimire B, Tonello D, Reed C, Baba H, Aldrich S, Phillips TJ (September 2023). "Robust aversive effects of trace amine-associated receptor 1 activation in mice". Neuropsychopharmacology. 48 (10): 1446–1454. doi:10.1038/s41386-023-01578-4. PMC 10425385. PMID 37055488.
^ Liu J, Wu R, Johnson B, Zhang Y, Zhu Q, Li JX (October 2022). "Selective TAAR1 agonists induce conditioned taste aversion". Psychopharmacology (Berl). 239 (10): 3345–3353. doi:10.1007/s00213-022-06222-5. PMID 36056214.

Human trace amine-associated receptor ligands

TAAR1

Agonists

Endogenous^†

Synthetic and natural^‡

Neutral antagonists

RTI-7470-44

Inverse agonists

EPPTB (RO-5212773)

TAAR2

Agonists^‡
Neutral antagonists

TAAR5

Agonists^‡	N,N-Dimethylethylamine Trimethylamine
Neutral antagonists
Inverse agonists^‡	3-Iodothyronamine

^† References for all endogenous human TAAR1 ligands are provided at List of trace amines

^‡ References for synthetic TAAR1 agonists can be found at TAAR1 or in the associated compound articles. For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references.

See also: Receptor/signaling modulators

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