Yohimbine derivatives, their preparation methods, and uses. This invention discloses compounds of Formula I and pharmaceutical compositions comprising compounds of Formula I. The compounds of Formula I of this invention, as adrenaline receptor α2A (ADRA2A) antagonists or partial antagonists, can treat and / or prevent inflammatory bowel disease (IBD), particularly ulcerative colitis (UC), Crohn's disease (CD), or enteritis.