Inhibitory effect of amitriptyline on contraction of the rat isolated trachea
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AbstractThe effects of amitriptyline, a tricyclic antidepressant, on contractile responses to exogenously applied acetylcholine, endothelin 1 and high K+ were examined in the rat isolated trachea. Amitriptyline (0.3-30 mu mol/l) produced a shift to the right of the logarithmic acetylcholine concentration-contraction curve without affecting the maximum contraction. Amitriptyline (10-100 mu mol/l) significantly reduced the maximal contractile response to endothelin 1. The IC50 values were 10.3 and 30.2 mu mol/l for inhibition of the submaximal contractile response to 1 mmol/l acetylcholine and to 50 nmol/l endothelin 1, respectively. Amitriptyline inhibited the high K+ (60 mmol/l)-evoked contraction with an IC50 of 0.225 mu mol/l. The inhibitory effect of amitriptyline was unchanged by the K+ channel blockers, charybdotoxin (100 nmol/l) and glibenclamide (up to 10 mu mol/l). These results indicate that amitriptyline could antagonize the effect of acetylcholine and also exert direct inhibitory effect on muscle contraction of the rat trachea as a nonselective muscle relaxant.
All Author(s) ListHuang Y, Lau CW
Journal namePharmacology
Volume Number54
Issue Number6
Pages312 - 318
LanguagesEnglish-United Kingdom
Keywordsacetylcholine; amitriptyline; contraction; endothelin 1; rat; trachea
Web of Science Subject CategoriesPharmacology & Pharmacy; PHARMACOLOGY & PHARMACY

Last updated on 2020-26-10 at 02:25