Pitolisant草酸盐(BF2.649)是新型的人重组H3受体选择性反向激动剂,Ki为0.16 nM。
CAS:362665-57-4
分子式:C19H28ClNO5
分子量:385.88
纯度:98%
存储:Store at -20°C
Background:
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Ki: 0.16 nM (H3 receptor)[1]EC50: 1.5 nM (H3 receptor)[1]
On the stimulation of guanosine 5′-O-(3-[35S]thio)triphosphate binding to this receptor, Pitolisant (BF2.649) behaves as a competitive antagonist with a Ki value of 0.16 nM and as an inverse agonist with an EC50 value of 1.5 nM and an intrinsic activity