Chemical Name: 1-(5-(4-(4-Fluorophenyl)piperazin-1-yl)pentyl)-1H-benzo[d]imidazole-2(3H)-one
ß-Arrestin-biased 5-HT7 antagonist
Molecular Weight:
382.47
Purity:
>98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[1814929-81-1]
Formula:
C22H27FN4O
Application Notes:
Serodolin is a potent dual antagonist of the serotonin receptors 5-HT7 (Ki = 6.2 nM, IC50 = 5.7 nM cAMP response) and 5-HT2A (Ki = 19 nM, IC50 = 110 nM IP1 response) with significant selectivity over 5-HT1A and 5-HT6.1 Serodolin has recently been found to act as a ß-arrestin-biased inverse agonist on Gs signaling while inducing ERK activation requiring c-SRS activation, a unique pharmacological profile among 5-HT7 ligands.2 It decreased hyperalgesia and pain sensation in response to inflammatory, thermal, and mechanical stimulation in a mouse model demonstrating the therapeutic potential of a ß-arrestin-biased ligand for pain relief. Blood-brain barrier permeable.
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