Temanogrel

Temanogrel is a highly selective 5-HT_2A receptor antagonist with a K_i of 4.9 nM. IC50 & Target: Ki: 4.9 nM (5-HT_2A receptor) In Vitro: Temanogrel is a highly selective 5-HT_2A receptor antagonist with a K_i of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC₅₀ of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC₅₀=8.7 and 23.1 nM, respectively)^[1]. Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC₅₀ of 13±7 nM^[3]. In Vivo: There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment^[3].