| Identification | Back Directory | [Name]
(S)-5-(3-(tert-butyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-7-yl)-3-(4-fluorophenyl)-1,2,4-oxadiazole | [CAS]
1313498-17-7 | [Synonyms]
(S)-5-(3-(tert-butyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridin-7-yl)-3-(4-fluorophenyl)-1,2,4-oxadiazole
1,2,4-Triazolo[4,3-a]pyridine, 3-(1,1-dimethylethyl)-7-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-5,6,7,8-tetrahydro-, (7S)- | [Molecular Formula]
C18H20FN5O | [MDL Number]
MFCD21609262 | [MOL File]
1313498-17-7.mol | [Molecular Weight]
341.38 |
| Hazard Information | Back Directory | [Uses]
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research[1]. | [in vivo]
LSN2814617 (0.3-60 mg/kg, Orally, once) displays significant unbound brain exposure and dose-dependent occupancy of the mGlu5 receptor[1].
LSN2814617 (0-10 mg/kg, Orally, once) significantly modulates amphetamine-induced locomotor hyperactivity[1].
LSN2814617 (0-3 mg/kg, Orally, once) markedly increase wakefulness[1]. | Animal Model: | Male Lister Hooded rats (180-250 g, four to eight per cage)[1] | | Dosage: | 0, 2.5, 5, and 10 mg/kg | | Administration: | Orally, once, 60 min before amphetamine | | Result: | Significantly modulated amphetamine hyperactivity, although a trend level decrease in hyperactivity was observed for the highest dose. At the end of the test session, from 75 to 120 min, the 10 mg/kg dose of LSN2814617 significantly increased amphetamine-induced hyperactivity. |
| Animal Model: | Adult male Wistar rats (approximately 270 g)[1] | | Dosage: | 0, 0.3, 1, and 3 mg/kg
| | Administration: | Orally, once | | Result: | Displayed dose-dependently increase in wakefulness immediately following oral administration; Produced 234 ± 16 min of increased wake for over 7 h in the case of 3 mg/kg. Produced dose-dependent reductions in both NREM and REM sleep. |
| [IC 50]
rat mGluR5: 42 ± 9 nM (IC50); human mGluR5: 52 ± 21 nM (IC50) | [References]
[1] Gilmour G, et al. In vitro characterisation of the novel positive allosteric modulators of the mGlu? receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. DOI:10.1016/j.neuropharm.2012.07.030 |
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