RTIOX-276

RTIOX-276
Identifiers
	IUPAC name 2-(1-(3,4-dimethoxybenzyl)-6-methoxy-7-(2,2,2-trifluoroethoxy)-3,4-dihydroisoquinolin-2(1H)-yl)-N-(pyridin-3-ylmethyl)acetamide;
Chemical and physical data
Formula	C29H32F3N3O5
Molar mass	559.586 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(NCC1=CC=CN=C1)CN2C(CC3=CC(OC)=C(OC)C=C3)C4=CC(OCC(F)(F)F)=C(OC)C=C4CC2;

RTIOX-276 is an orexin antagonist. RTIOX-276 binds selectively to the orexin 1 receptor (K_E = 8.5nM) and lacks significant affinity for the orexin 2 receptor (K_E = > 10,000nM). RTIOX-276 may have therapeutic utility for the treatment of cocaine addiction. In conditioned place preference studies, RTIOX-276 attenuated the development of place preference in mice exposed to cocaine.^[1]^[2]^[3]

References

^ Perrey DA, German NA, Gilmour BP, Li JX, Harris DL, Thomas BF, Zhang Y (September 2013). "Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Journal of Medicinal Chemistry. 56 (17): 6901–16. doi:10.1021/jm400720h. PMC 3849818. PMID 23941044.
^ Perrey DA, Decker AM, Li JX, Gilmour BP, Thomas BF, Harris DL, et al. (September 2015). "The importance of the 6- and 7-positions of tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Bioorganic & Medicinal Chemistry. 23 (17): 5709–24. doi:10.1016/j.bmc.2015.07.013. PMC 4554834. PMID 26216017.
^ Perrey DA, German NA, Decker AM, Thorn D, Li JX, Gilmour BP, et al. (April 2015). "Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor". ACS Chemical Neuroscience. 6 (4): 599–614. doi:10.1021/cn500330v. PMC 4400266. PMID 25643283.

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[1] Perrey DA, German NA, Gilmour BP, Li JX, Harris DL, Thomas BF, Zhang Y (September 2013). "Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Journal of Medicinal Chemistry. 56 (17): 6901–16. doi:10.1021/jm400720h. PMC 3849818. PMID 23941044.

[2] Perrey DA, Decker AM, Li JX, Gilmour BP, Thomas BF, Harris DL, et al. (September 2015). "The importance of the 6- and 7-positions of tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor". Bioorganic & Medicinal Chemistry. 23 (17): 5709–24. doi:10.1016/j.bmc.2015.07.013. PMC 4554834. PMID 26216017.

[3] Perrey DA, German NA, Decker AM, Thorn D, Li JX, Gilmour BP, et al. (April 2015). "Effect of 1-substitution on tetrahydroisoquinolines as selective antagonists for the orexin-1 receptor". ACS Chemical Neuroscience. 6 (4): 599–614. doi:10.1021/cn500330v. PMC 4400266. PMID 25643283.

[1]

[2]

[3]

v t e Orexin receptor modulators
OX₁	Agonists: Orexin (A, B) Antagonists: ACT-335827 ACT-462206 ACT-539313 Almorexant AZD-4041 C4X-3256 (INDV-2000) CR-5542 Daridorexant Filorexant GSK-649868 (SB-649868) JNJ-61393215 Lemborexant RTIOX-276 SB-334867 SB-408124 Suvorexant TCS-1102 Vornorexant (ORN-0829, TS-142) YZJ-1139
OX₂	Agonists: Danavorexton (TAK-925) Firazorexton Orexin (A, B) SB-668875 Suntinorexton TAK-861 TAK-994 Antagonists: ACT-335827 ACT-462206 Almorexant Daridorexant EMPA Filorexant GSK-649868 (SB-649868) JNJ-10397049 Lemborexant MK-1064 MK-3697 MK-8133 Seltorexant Suvorexant TCS-1102 TCS-OX2-29 Vornorexant (ORN-0829, TS-142) YZJ-1139

Identifiers

IUPAC name 2-(1-(3,4-dimethoxybenzyl)-6-methoxy-7-(2,2,2-trifluoroethoxy)-3,4-dihydroisoquinolin-2(1H)-yl)-N-(pyridin-3-ylmethyl)acetamide
Chemical and physical data
Formula	C₂₉H₃₂F₃N₃O₅
Molar mass	559.586 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES O=C(NCC1=CC=CN=C1)CN2C(CC3=CC(OC)=C(OC)C=C3)C4=CC(OCC(F)(F)F)=C(OC)C=C4CC2