Pitolisant 是一种有效的选择性的非咪唑类重组人组胺 H3 受体反相激动剂,Ki 为 0.16 nM。
CAS:362665-56-3
分子式:C17H26ClNO
分子量:295.85
纯度:98%
存储:Store at -20°C
Background:
Pitolisant 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