Ketanserin is an inhibitor of 5-HT2A receptors that exhibits antihypertensive, vasodilatory, analgesic, and pro-angiogenic activities. In animal models of hypertension, ketanserin decreases blood pressure and improves baroreceptor sensitivity and vagal tonic activity, improving left ventricular remodeling and overall cardiac function. In animal models of myocardial infarction, ketanserin increases expression of VEGF and increases capillary density in myocardial tissue. In other animal models, this compound inhibits transient receptor potential vanilloid 1 (TRPV1) channel-evoked thermal hyperalgesia. Through downstream targets, ketanserin may also inhibit α1-adrenergic receptors.