KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels

British Journal of Pharmacology
Bin-Nan WuIng-Jun Chen

Abstract

7-[2-[4-(2-chlorophenyl)piperazinyl]ethyl]-1,3-dimethylxanthine (KMUP-1) produces tracheal relaxation, intracellular accumulation of cyclic nucleotides, inhibition of phosphodiesterases (PDEs) and activation of K+ channels. KMUP-1 (0.01-100 microm) induced concentration-dependent relaxation responses in guinea-pig epithelium-intact trachea precontracted with carbachol. Relaxation responses were also elicited by the PDE inhibitors theophylline, 3-isobutyl-1-methylxanthine (IBMX), milrinone, rolipram and zaprinast (100 microm), and a KATP channel opener, levcromakalim. Tracheal relaxation induced by KMUP-1 was attenuated by epithelium removal and by pretreatment with inhibitors of soluble guanylate cyclase (sGC) (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), 1 microm), nitric oxide synthase (Nomega-nitro-L-arginine methyl ester, 100 microm), K+ channels (tetraethylammonium, 10 mm), KATP channels (glibenclamide, 1 microm), voltage-dependent K+ channels (4-aminopyridine, 100 microm) and Ca2+-dependent K+ channels (charybdotoxin, 0.1 microm or apamin, 1 microm). Both KMUP-1 (10 microm) and theophylline nonselectively and slightly inhibited the enzyme activity of PDE3, 4 and 5, suggesting that they are able to inhibit the metabo...Continue Reading

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Citations

Jan 31, 2008·Pflügers Archiv : European journal of physiology·Yongping Chai, Yu-Fung Lin
Nov 26, 2009·American Journal of Respiratory Cell and Molecular Biology·Peter J OldenburgJoseph H Sisson
Jan 3, 2012·The Kaohsiung Journal of Medical Sciences·Jun-Yih ChenBin-Nan Wu
May 25, 2011·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Patrícia F S CastroMatheus L Rocha
Mar 18, 2009·Journal of Veterinary Pharmacology and Therapeutics·M Koutsoviti-PapadopoulouG C Batzias
Oct 11, 2008·Fundamental & Clinical Pharmacology·Theophano A PsarraMaria Koutsoviti-Papadopoulou
Apr 19, 2015·Journal of Ethnopharmacology·Amber Hanif Palla, Anwarul-Hassan Gilani
Mar 1, 2006·Bioorganic & Medicinal Chemistry·Michel Legraverend, David S Grierson
Mar 22, 2014·Molecular Pharmacology·Rene RaphemotJerod S Denton
Jul 2, 2008·The Journal of Pharmacology and Experimental Therapeutics·Luciana Pontes CoelhoMarco Aurélio Martins
Aug 19, 2011·Organic & Biomolecular Chemistry·Yih-Dih ChengPei-Wen Hsieh

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