Inverse agonist is a new type of classification.Different form antagonist that blocks the effect of agonist,inverse agonist produces opposite effect to that of agonist.The characteristics of inverse agonists acting on different receptors including H_2,H_3,μ opioid,adrenergic β, and 5-HT_((1B)) receptors are discussed in this paper.Recent investigation suggested that inverse agonist has potential clinical application.