RS-127445

RS-127445 is a potent, orally bioavailable, and highly selective small molecule antagonist of the serotonin 5-HT2B receptor, characterized by a pKi of 9.5. Developed by Roche (formerly Syntex), it demonstrates approximately 1,000-fold selectivity for the 5-HT2B receptor over the closely related 5-HT2A and 5-HT2C subtypes. The compound is widely utilized as a pharmacological research tool to investigate the role of 5-HT2B signaling in various physiological and pathological processes, including pulmonary arterial hypertension (PAH), cardiac remodeling, and migraine. Preclinical studies have shown that RS-127445 can prevent and reverse monocrotaline-induced pulmonary hypertension in animal models by inhibiting serotonin-mediated vascular smooth muscle cell proliferation and remodeling. Despite its high potency and selectivity, RS-127445 is intended solely for laboratory research and has not been developed for human or veterinary therapeutic use.

Other names

2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine