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Acute toxicity profile of boron containing arylethanolamines and their precursors in mice
Author(s) -
Amezcua-Gutierrez Marcos A,
Lopez-Cabrera Yessica,
Cipres-Flores Fabiola J,
Soriano-Ursua Marvin A,
Trujillo-Ferrara José G
Publication year - 2012
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.26.1_supplement.lb587
Subject(s) - toxicity , gastrointestinal tract , acute toxicity , pharmacology , chemistry , potency , lethal dose , boron , sedation , biochemistry , medicine , in vitro , organic chemistry
Arylethanolamines modulate the activity of catecholamine systems. Our working group has found that the addition of functional groups with boron to arylethanolamines confers them greater potency and efficacy on their receptor‐targets in smooth muscle or central nervous system (CNS). However, the use of boronic acids in drug development is limited due to disputes on the toxicological profile of these compounds. This study evaluated the acute toxicity of boronic acids, arylethanolamines and boron containing arylethanolamines by determining its toxic (DT50) and lethal dose (LD50) in CD1 male mice with 22±2 g as well as by general observations from necropsy of treated animals. In our study,3 of the 7 tested boronic acids induced dose‐dependent events presumably mediated by action on the CNS (sedation, hypnosis and/or shaking motion) in live mice, but also eye damage and gastrointestinal effects (as gastric‐gut dilatation and fecal retention)were observed in death mice. On the other hand, the boron containing adducts induced acute toxicity in higher or similar dose than other arylethanolamines, excepting one tested compounds which induced sedation. These data allows a framework for the toxic evaluation of these compounds which can be considered potential therapeutic agents. Supported by grants from SIP‐IPN and CONACYT programs.