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AS 19

Names

[ CAS No. ]:
1000578-26-6

[ Name ]:
AS 19

[Synonym ]:
2-Naphthalenamine, 1,2,3,4-tetrahydro-N,N-dimethyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)-, (2S)-
(2S)-N,N-Dimethyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydro-2-naphthalenamine
(2S)-N,N-Dimethyl-5-(1,3,5-trimethyl-1H-pyrazol-4-yl)-1,2,3,4-tetrahydronaphthalen-2-amine
AS-19

Biological Activity

[Description]:

AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia[1][2][3].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

Human 5-HT7 Receptor:0.83 nM (IC50)

Human 5-HT7 Receptor:0.6 nM (Ki)

5-HT1A Receptor:89.7 nM (Ki)

5-HT1B Receptor:490 nM (Ki)

5-HT1D Receptor:6.6 nM (Ki)

5-HT5 Receptor:98.5 nM (Ki)


[In Vitro]

The proliferation of T-cell from parachlorophenylalanine-treated mice is significantly reduced, addition of AS19 (1 μM) completely restores T-cell proliferation after 48 hours[2].

[In Vivo]

AS19 (0.5-10 mg/kg; subcutaneous injection; for 24 hours; male Wistar rats) treatment improves memory consolidation in an autoshaping Pavlovian/instrumental learning task[1]. Animal Model: Male Wistar rats (12-week-old) with autoshaping Pavlovian/instrumental learning task[1] Dosage: 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg Administration: Subcutaneous injection; for 24 hours Result: Enhanced memory formation in an autoshaping Pavlovian/instrumental learning task.

[References]

[1]. Perez-García GS, et al. Effects of the potential 5-HT7 receptor agonist AS 19 in an autoshaping learning task. Behav Brain Res. 2005 Aug 30;163(1):136-40.

[2]. León-Ponte M, et al. Serotonin provides an accessory signal to enhance T-cell activation by signaling through the 5-HT7 receptor. Blood. 2007 Apr 15;109(8):3139-46.

[3]. Brenchat A, et al. 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain. 2009 Feb;141(3):239-47.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
413.3±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H25N3

[ Molecular Weight ]:
283.411

[ Flash Point ]:
203.7±28.7 °C

[ Exact Mass ]:
283.204834

[ LogP ]:
3.71

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.595

[ Storage condition ]:
2-8°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds