caa a22 4500 469077891 CHVBK 20180323132940.0 cr unu---uuuuu 170328e19920701xx s 000 0 eng 10.1007/BF00167580 doi (NATIONALLICENCE)springer-10.1007/BF00167580 Cicletanine sulfate: inhibition of anion transport systems and natriuretic activity [Elektronische Daten] [R.P. Garay, C. Rosati, C. Nazaret, A. Esanu, T. Tarrade, P. Braquet] Summary: In contrast with cicletanine, its urinary sulfoconjugate metabolite (cicletanine sulfate) was active on membrane ion transport in human red blood cells. Cicletanine sulfate was a more potent inhibitor of the Na+ dependent [Cl−/HC03 −] exchanger (IC50 = 9±3 × 10−5 mol/l; mean±SD of 4 experiments) than cicletanine (IC50 = 10−3 mol/l). This inhibitory potency was intermediate between that of xipamide (IC50 = 2 × 10−5 mol/l) and that of furosemide (IC50 = 2 × 10−4 mol/l). Moreover, cicletanine sulfate exhibited modest inhibitory potency against the [Na+,K+,Cl−]-cotransport system (IC50 = 1±0.3 × 10−3 mol/I; mean±SD of 4 experiments) and poor inhibitory activity against the [K+,CI−]-cotransport system. Cicletanine sulfate was unable to modify the activity of Cl−-independent membrane carriers(Na+ : H+exchanger,Ca 2+pump, Na+ : Li+ countertransport system and Na+,K+ pump). Following renal intraarterial administration in rats, cicletanine sulfate and not cicletanine, exhibited salidiuretic activity. In conclusion, the urinary sulfo-conjugate of cicletanine is an active anion transport inhibitor and natriuretic metabolite. In fact, this metabolite may be responsible for the salidiuretic action of cicletanine. Springer-Verlag, 1992 Sulfates nationallicence Cicletanine nationallicence Cell membranes nationallicence Ion transport nationallicence Na+ transport nationallicence Cl− transport nationallicence HC03 transport nationallicence [CI−/HCO3−] anion exchanger nationallicence Garay R.P. INSERM U2/CNRS UA 130251, Faculté de Médicine, 8 rue du Général Sarrail, F-94010, Créteil, France aut Rosati C. CRASH, F-36140, Crevant aut Nazaret C. INSERM U2/CNRS UA 130251, Faculté de Médicine, 8 rue du Général Sarrail, F-94010, Créteil, France aut Esanu A. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut Tarrade T. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut Braquet P. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/1(1992-07-01), 114-119 0028-1298 346:1<114 1992 346 210 https://doi.org/10.1007/BF00167580 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00167580 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Garay R.P. INSERM U2/CNRS UA 130251, Faculté de Médicine, 8 rue du Général Sarrail, F-94010, Créteil, France aut NATIONALLICENCE 700 1- Rosati C. CRASH, F-36140, Crevant aut NATIONALLICENCE 700 1- Nazaret C. INSERM U2/CNRS UA 130251, Faculté de Médicine, 8 rue du Général Sarrail, F-94010, Créteil, France aut NATIONALLICENCE 700 1- Esanu A. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut NATIONALLICENCE 700 1- Tarrade T. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut NATIONALLICENCE 700 1- Braquet P. I.H.B., 17 av. Descartes, F-92350, Le Plessis-Robinson, France aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/1(1992-07-01), 114-119 0028-1298 346:1<114 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer