Chemical Name:4-[2-(Methylthio)phenyl]-N-(1,2,3,4-tetrahydro-1-naphth
alenyl)-1-piperazinehexanamide hydrochloride
Biological Activity:
High
affinity 5-HT7 receptor agonist (Ki = 0.22 nM) that
displays selectivity over 5-HT1A and 5-HT2A receptors
(200- and > 1000-fold respectively). Induces relaxation of substance
P-stimulated guinea pig ileum (EC50 = 2.56 μM).
Leopoldoet al (2004)
Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides,
a new class of 5-hydroxytryptamine7 receptor agents. J.Med.Chem. 47
6616.
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.