纯度:>98% by HPLC;NMR (Conforms)
分子式:C22H27FN4O
分子量:382.47
溶剂:DMSO (50 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):?-Arrestin-biased 5-HT7 antagonist
Function / Pharmacology: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 ?-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 ?-arrestin-biased ligand for pain relief. Blood-brain barrier permeable.