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LSN2814617

Catalog No. T27855 CAS 1313498-17-7

Synonyms: LSN-2814617, LSN 2814617

LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties but little in the way of rebound hypersomnolence. LSN2814617 can be used for schizophrenia research [1].

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LSN2814617, CAS 1313498-17-7

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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Description	LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu 5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC 50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). In vivo EEG studies demonstrated that LSN2463359 has marked wake-promoting properties but little in the way of rebound hypersomnolence. LSN2814617 can be used for schizophrenia research [1].
In vitro	LSN2814617 (1nM-10 μM) fails to elicit responses alone in rat cortical neurons, and causes a concentration-dependent increase in the [Ca2+]i response in AV12 cells [1].
In vivo	Administered orally in doses ranging from 0.3 to 60 mg/kg, LSN2814617 demonstrates significant unbound brain exposure and dose-dependent mGlu5 receptor occupancy, as well as markedly modulating amphetamine-induced locomotor hyperactivity in doses up to 10 mg/kg. In doses up to 3 mg/kg, it notably increases wakefulness. In the study involving male Lister Hooded rats (180-250 g, housed four to eight per cage), doses of 0, 2.5, 5, and 10 mg/kg of LSN2814617, given orally 60 minutes before amphetamine exposure, significantly modulated amphetamine hyperactivity. Notably, the highest dose displayed a trend towards reduced hyperactivity. However, from 75 to 120 minutes into the test session, the 10 mg/kg dose significantly increased amphetamine-induced hyperactivity. In adult male Wistar rats (approximately 270 g), doses of 0, 0.3, 1, and 3 mg/kg resulted in a dose-dependent increase in wakefulness immediately after administration, with the 3 mg/kg dose yielding 234 ± 16 minutes of increased wakefulness over 7 hours and also reducing both non-rapid eye movement (NREM) and rapid eye movement (REM) sleep.

Synonyms	LSN-2814617, LSN 2814617
Molecular Weight	341.38
Formula	C18H20FN5O
CAS No.	1313498-17-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Loomis S, McCarthy A, Baxter C, Kellett DO, Edgar DM, Tricklebank M, Gilmour G. Distinct pro-vigilant profile induced in rats by the mGluR5 potentiator LSN2814617. Psychopharmacology (Berl). 2015 Nov;232(21-22):3977-89. doi: 10.1007/s00213-015-3936-8. PubMed PMID: 25902875; PubMed Central PMCID: PMC4600478. 2. Ahnaou A, Langlois X, Steckler T, Bartolome-Nebreda JM, Drinkenburg WH. Negative versus positive allosteric modulation of metabotropic glutamate receptors (mGluR5): indices for potential pro-cognitive drug properties based on EEG network oscillations and sleep-wake organization in rats. Psychopharmacology (Berl). 2015 Mar;232(6):1107-22. doi: 10.1007/s00213-014-3746-4. PubMed PMID: 25323624. 3. Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD. In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ 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. PubMed PMID: 22884720.

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Keywords

LSN2814617 1313498-17-7 LSN-2814617 LSN 2814617 inhibitor inhibit

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