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Novel α-adrenoceptor antagonism by the fluroquinolone antibiotic trovafloxacin.

Eur. J. Pharmacol.. 2016-12; 
AngusJames A,WrightChristi
Products/Services Used Details Operation
Biochemicals … Drugs used and suppliers were: endothelin-1 (GenScript, Piscataway, NJ, USA); methoxamine hydrochloride (Sigma, St Louis, MO, USA); phenylephrine hydrochloride (Sigma); prazosin hydrochloride (Sigma); trovafloxacin mesylate (Tocris Bioscience, Bristol, UK) and U46619 … Get A Quote

摘要

Trovafloxacin, a fluroquinolone antibiotic, was recently found to be an inhibitor of pannexin-1 channels through which ATP is released as "find-me" signals in apoptotic Jurkat cells. Our interest in the role of pannexin-1 channels in α-adrenoceptor-mediated vasoconstriction led us to the novel finding reported here. Concentration-response curves to methoxamine and phenylephrine were competitively antagonised by trovafloxacin (1-30µM) with a pK of 5.54 and 5.32, respectively, in rat mesenteric small arteries isolated for myography. In comparison, prazosin (1-10nM) antagonised methoxamine concentration-response curves with a pK of 9.76. Trovafloxacin (1-30µM) had no effect on either the thromboxane m... More

关键词

Endothelin-1 (PubChem CID: 16132423),Methoxamine hydrochloride (PubChem CID: 6081),Pannexin-1 channels,Phenylephrine hydrochloride (PubChem CID: 5284443),Prazosin,Prazosin hydrochloride (PubChem CID: 68546),PubChem CID: 16219283),Trovafloxacin,Trovafloxacin mesylate (PubChem CID: 62960),U46619 (9,11-dideoxy-9α,11α-methanoepoxyprostaglandin F2α,Vascular contraction,α -adrenocep