(2S)-(+)-5-(1,3,5-Trimethylpyrazol-4-yl)-2-(dimethylamino)tetralin

Uses

A potent 5-HT7 receptor agonist

Biological Activity

Reported potent 5-HT 7 receptor agonist (IC 50 = 0.83 nM). In vivo, enhances memory consolidation and reverses scopolamine- or dizocilpine-induced amnesia.

in vivo

IC 50

Human 5-HT₇ Receptor: 0.83 nM (IC₅₀); Human 5-HT₇ Receptor: 0.6 nM (Ki); 5-HT_1A Receptor: 89.7 nM (Ki); 5-HT_1B Receptor: 490 nM (Ki); 5-HT_1D Receptor: 6.6 nM (Ki); 5-HT₅ Receptor: 98.5 nM (Ki)

storage

Desiccate at -20°C

References

[1]. perez-garcía gs and meneses a. effects of the potential 5-ht7 receptor agonist as 19 in an autoshaping learning task. behav brain res, 2005, 163(1):136-40.
[2]. thomas dr and hagan jj. 5-ht7 receptors. current drug targets-cns & neurological disorders, 2004, 3(1): 81-90.
[3]. ulugol a, oltulu c, gunduz o, et al. 5-ht7 receptor activation attenuates thermal hyperalgesia in streptozocin-induced diabetic mice. pharmacol biochem behav, 2012, 102(2):344-8.
[4]. león-ponte m, ahern gp and o'connell pj. serotonin provides an accessory signal to enhance t-cell activation by signaling through the 5-ht7 receptor. blood, 2007, 109(8):3139-46.
[5]. hoffman ms and mitchell gs. spinal 5-ht7 receptor activation induces long-lasting phrenic motor facilitation. j physiol, 2011, 589(pt 6):1397-407.