Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT 3 receptor agonist

…, L Alonso-Cires, I Tapia, R Mosquera, A Orjales

Index: Lopez-Tudanca, Pedro Luis; Labeaga, Luis; Innerarity, Ana; Alonso-Cires, Luisa; Tapia, Ines; Mosquera, Ramon; Orjales, Aurelio Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 13 p. 2709 - 2714

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Citation Number: 22

Abstract

N-(2-Benzoxazol-2-yl-ethyl)-guanidine hydrochloride (10) was synthesized and pharmacologically tested. This compound showed high affinity for the 5-HT3 receptor (Ki= 0.77 nM) and potently triggered the von Bezold–Jarisch reflex (BJR) in rats with an ED50= 0.52 μg/kg iv and intrinsic activity next to 1 (ia= 0.94). This stimulant effect was abolished by pretreatment with the 5-HT3 receptor antagonist granisetron and was subject to a rapid ...