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• W2068414196 abstract "N-(2-Benzoxazol-2-yl-ethyl)-guanidine hydrochloride (10) was synthesized and pharmacologically tested. This compound showed high affinity for the 5-HT(3) receptor (K(i)=0.77 nM) and potently triggered the von Bezold-Jarisch reflex (BJR) in rats with an ED(50)=0.52 microg/kg iv and intrinsic activity next to 1 (i.a.=0.94). This stimulant effect was abolished by pretreatment with the 5-HT(3) receptor antagonist granisetron and was subject to a rapid and pronounced tachyphylaxis, due to desensitization of the peripheric cardiac 5-HT(3) receptor. Consequently, 10 acts as an in vivo 5-HT(3) antagonist inhibiting the BJR responses evoked by submaximal doses of 5-HT with an ID(50)=5.8 microg/kg iv." @default.
• W2068414196 created "2016-06-24" @default.
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• W2068414196 date "2003-07-01" @default.
• W2068414196 modified "2023-10-16" @default.
• W2068414196 title "Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT 3 receptor agonist" @default.
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• W2068414196 doi "https://doi.org/10.1016/s0968-0896(03)00243-8" @default.
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