Temanogrel 是一种高度选择性的 5-HT2A 受体拮抗剂，Ki值为 4.9 nM。

Temanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Temanogrel inhibits inositol phosphate accumulation (IC50: 5.2 nM). Temanogrel shows effective inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). 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 (IC50: 13±7 nM) [1][3].

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 in dogs assigned to receive Temanogrel. There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment [3].

887936-68-7

C24H28N4O4

436.5

APD791;Temanogrel

DMSO:125 mg/mL (286.37 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years