Background:

Irindalone is a novel serotonin 5-HT2 antagonist.

Irindalone causes a concentration-related inhibition of serotonin-induced contractions and shifts the serotonin curve to the right. Irindalone is more potent in inhibiting the serotonin-induced contractions. Irindalone has a similar profile in vitro, with a high affinity for serotonin 5-HT2 receptors and about a 10 times lower affinity for α1-adrenoceptors[1].

Irindalone dose dependently lowers the blood pressure in spontaneously hypertensive rats (SHR) and renal hypertensive dogs[1].

[1]. Mikkelsen EO, et al. Comparison of the effect of irindalone, a novel serotonin 5-HT2 antagonist and ketanserin on mechanical responses of rat thoracic aorta. Eur J Pharmacol. 1988 Apr 27;149(1-2):145-8.