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Environmental Science: Processes & Impacts Electronic Supplementary Information Electronic Supplementary Material (ESI) for Environmental Science: Processes & Impacts. This journal is © The Royal Society of Chemistry 2017 Environmental Science: Processes & Impacts Electronic Supplementary Information Baseline toxicity and ion-trapping models to describe the pH-dependence of bacterial toxicity of pharmaceuticals Andreas Baumer,a,b Kai Bittermann,a Nils Klüver,a and Beate I. Eschera,c S1. Additional information on the Microtox assay Phenol pH 5.5 pH 6 pH 7 pH 8 pH 9 -1.5 100 80 A.fischeri [%] 60 -2.0 40 20 (M) for inhibition 0 50 -2.5 Aliivibrio fischeri in -20 logEC Inhibition of bioluminescence -40 of bioluminescence in -3.0 -5 -4 -3 -2 -1 -4 -3 -2 -1 -4 -3 -2 -1 -4 -3 -2 -1 -4 -3 -2 -1 log concentration [M] log concentration [M] log concentration [M] log concentration [M] log concentration [M] pH 6 pH 7 pH 8 pH 9 pH 5.5 Fig. S1 A. Reference compound phenol as a measure of repeatability and robustness of the 384-well plate set up of the Microtox assay. S2. Additional information on the chemicals Table S1 Additional information on the pharmaceuticals tested; CAS numbers, purity supplier and counterion if a salt was used. All calculations are done in molar, i.e., the counterion of the salt was not considered. The pharmaceuticals are sorted in groups of acidic, basic, multiprotic chemicals and alphabetically within the groups. Name CAS Batch Purity Supplier Salt Caffeine 58-08-2 1378801 >99% Sigma-Alrich - Carbamazepine 298-46-4 0455124-10 >98% Sigma-Aldrich - Acetyl-sulfamethoxazole 21312-10-7 BCBQ9726V >98,5% Sigma-Aldrich - Bezafibrate 41859-67-0 BCBQ1675V >98% Fluka - Clofibric acid 882-09-7 BCBK9475V >99% Fluka - Diclofenac 15307-86-5 0457729-34 >99% Cayman Chemical Company Sodium Furosemide 54-31-9 0473175-1 >98% Cayman Chemical Company - Ibuprofen 15687-27-1 015K0586 n.b. Sigma-Aldrich Sodium Ketoprofen 22071-15-4 BCBP4500V >98% Sigma-Aldrich - Losartan 114798-26-4 0443154-54 >98% Cayman Chemical Company Potassium Mefenamic acid 61-68-7 BCBM5220V >99% Fluka - Naproxen 22204-53-1 0430295-34 >99% Cayman Chemical Company - Paracetamol 103-90-2 1061901 n.b. - - Electronic Supplementary Information S1 Electronic Supplementary Information Environmental Science: Processes & Impacts Name CAS Batch Purity Supplier Salt Salicylic acid 69-72-7 MKBG8728V >99% Sigma-Aldrich - Sulfadimidine 57-68-1 065M4186V >99% Sigma-Aldrich - Sulfamethoxazole 723-46-6 BCBN0016V n.b. Fluka - Theophylline 58-55-9 10148004 n.b. Alfa Aesar - Torasemide 56211-40-6 1340038 n.b. abcr GmbH - Triclosan 3380-34-5 LRAA1072 n.b. Fluka - Warfarin 81-81-2 MKBS1257V n.b. Fluka - Atenolol 29122-68-7 BCBN4825V >98% Sigma-Aldrich - Cimetidine 51481-61-9 MKBV2403V n.b. Sigma-Aldrich - Cinnarizine 298-57-7 BCBP4836V n.b. Sigma-Aldrich - Citalopram 59729-33-8 WG0121801 n.b. Fluorochem Ltd. Hydrobromide Diphenhydramine 58-73-1 MKBQ9569V >98% Sigma-Aldrich Hydrochloride Doxylamine 469-21-6 109K1438V n.b. Sigma-Aldrich Succinate Fluoxetine 54910-89-3 129K2148 n.b. Sigma-Aldrich Hydrochloride Lamotrigine 84057-84-1 0455123-14 >98% Cayman Chemical Company - Lidocaine 137-58-6 SLBJ7206V 99.70% Sigma-Aldrich Hydrochloride Loratadine 79794-75-5 LRAA9165 n.b. Sigma-Aldrich - Metoprolol 37350-58-6 BCBH0239V >98% Sigma-Aldrich Tartrate Propranolol 525-66-6 BCBL8710V >99% Sigma-Aldrich Hydrochloride Tramadol 27203-92-5 n.b. n.b. n.b. Hydrochloride Venlafaxine 93413-69-5 2593609 99.10% LKT Laboratories Hydrochloride Verapamil 52-53-9 SLBH9660V >99% Sigma-Aldrich Hydrochloride Candesartan 139481-59-7 F17X009 >98% Alfa Aesar - Cetirizine 83881-51-0 BCBK5848V >98% Sigma-Aldrich Dihydrochloride Enalapril 75847-73-3 0458574-16 >98% Cayman Chemical Company - Fexofenadine 83799-24-0 G0K303 n.b. Twinbrook Pkwy Hydrochloride Genistein 446-72-0 Bertin Pharma - Irbesartan 138402-11-6 0440822-9 >98% Cayman Chemical Company - Labetalol 36894-69-6 077K1824V >98% Sigma-Aldrich Hydrochloride Telmisartan 144701-48-4 0437940-22 >98% Cayman Chemical Company - Valsartan 137862-53-4 LRAA0634 n.b. Fluka - Table S2 Additional information on the physicochemical properties (some data are reprinted from (Escher et al., 2017)). The data are sorted in groups of acidic, basic, multiprotic chemicals and alphabetically within the groups. log Klipw Name log Kow Reference pKa Reference (neutral) Reference log Klipw (ion) Reference (25°C) S2 Electronic Supplementary Information Environmental Science: Processes & Impacts Electronic Supplementary Information log Klipw Name log Kow Reference pKa Reference (neutral) Reference log Klipw (ion) Reference (25°C) NEUTRAL PHARMACEUTICALS a PhysProp (Newton and Kluza, Caffeine -0.07 0.6; 14 0.28 PP-LFERb - - exp. 1978) Carbama- PhysProp 2.45 - - 3.10 PP-LFER - - zepine exp. ACIDIC PHARMACEUTICALS Acetyl- sulfametho- 1.18 PP-LFER 5.54 (Prankerd, 2007) 1.74 PP-LFER 1.61 COSMOmicd xazole Bezafibrate 4.07 PP-LFER 3.6 (Huber et al., 2003b) 4.25 PP-LFER 1.81 COSMOmic PhysProp Clofibric acid 2.57 2.5 (Drillia et al., 2005) 2.62 PP-LFER 1.83 COSMOmic exp. PhysProp Diclofenac 4.51 3.99 (Avdeef et al., 1998) 4.45 (Avdeef et al., 1998) 2.64 (Avdeef et al., 1998) exp. PhysProp (Newton and Kluza, Furosemide 2.03 3.9 2.40 PP-LFER 2.46 COSMOmic exp. 1978) PhysProp Ibuprofen 3.97 4.45 (Avdeef et al., 1998) 3.80 (Avdeef et al., 1998) 1.81 (Avdeef et al., 1998) exp. PhysProp Ketoprofen 3.12 4.22 (Geiser et al., 2005) 3.78 PP-LFER 1.69 COSMOmic exp. Losartan 5.06 PP-LFER 4.9 (Williams et al., 1996) 5.41 PP-LFER 2.40 COSMOmic Mefenamic PhysProp 5.12 4.55 (Prankerd, 2007) 5.39 PP-LFER 2.67 COSMOmic acid exp. PhysProp Naproxen 3.18 4.18 (Bouchard et al., 2002) 3.84 PP-LFER 1.92 COSMOmic exp. Paracetamol 0.48 PP-LFER 9.38 PhysProp, exp. 1.02 COSMOmic 1.35 COSMOmic PhysProp (Ottiger and Wunderli- (Ottiger and Wunderli- Salicylic acid 2.26 2.93 (Geiser et al., 2005) 2.50 1.04 exp. Allenspach, 1997) Allenspach, 1997) PhysProp PhysProp, exp. Sangster Sulfadimidine 0.19 7.59 1.53 PP-LFER 1.61 COSMOmic exp. (1994) Sulfametho- PhysProp 0.89 5.70 (Huber et al., 2003a) 1.26 PP-LFER 1.56 COSMOmic xazole exp. PhysProp Theophylline -0.04 8.81 (Kortüm et al., 1961) -0.37 COSMOmic 1.06 COSMOmic exp. Torasemide 3.54 PP-LFER 6.68 (Masereel, 1993) 3.48 PP-LFER 2.23 COSMOmic PhysProp Triclosan 4.76 7.9 (Lindström et al., 2002) 5.43 PP-LFER 3.41 COSMOmic exp. PhysProp (Ottiger and Wunderli- (Ottiger and Wunderli- (Ottiger and Wunderli- Warfarin 2.7 4.9 3.39 1.40 exp. Allenspach, 1997) Allenspach, 1997) Allenspach, 1997) BASIC PHARMACEUTICALS PhysProp (Betageri and Rogers, Atenolol 0.16 9.55 -0.08 pp-LFER 1.79 (Escher et al., 2006) exp. 1987) Cimetidine 0.19 PP-LFERb 7.11 (Prankerd, 2007) 0.46 COSMOmic 0.22 COSMOmic PhysProp 3.5e/ Cinnarizine 5.77 (Belsner et al., 1993) 5.73 pp-LFER 3.55 COSMOmic exp. 7.47 Citalopram 3.58 PP-LFER 9.59 (Vasskog et al., 2006) 3.30 PP-LFER 1.31 COSMOmic Diphen- PhysProp 3.27 9.02 (Prankerd, 2007) 4.80 COSMOmic 2.11 COSMOmic hydramine exp. Doxylamine 2.46 PP-LFER 9.2 (Prankerd, 2007) 4.46 COSMOmic 1.24 COSMOmic Fluoxetine 4.62 PP-LFER 9.62 (Balon et al., 1999) 4.28 pp-LFER 3.84 (Neuwoehner et al., 2009) Lamotrigine 2.25 PP-LFER 5.34 (Ishihama et al., 2002) 2.74 PP-LFER 1.74 COSMOmic PhysProp PhysProp, exp. Sangster Lidocaine 2.44 8.01 2.39 (Avdeef et al., 1998) 1.22 (Avdeef et al., 1998) exp. 1994 Loratadine 5.2 PhysProp 4.75 ACD/pKa GALAS 4.31 COSMOmic 1.76 COSMOmic Electronic Supplementary Information S3 Electronic Supplementary Information Environmental Science: Processes & Impacts log Klipw Name log Kow Reference pKa Reference (neutral) Reference log Klipw (ion) Reference (25°C) exp. PhysProp (Newton and Kluza, Metoprolol 1.88 9.68 1.27 PP-LFER 1.43 (Escher et al., 2006) exp. 1978) PhysProp Propranolol 3.48 9.53 (Avdeef et al., 1998) 3.40 (Barzanti et al., 2007) 2.60 (Barzanti et al., 2007) exp. PhysProp (Azodi-Deilamia et al., Tramadol 2.51 9.41 2.44 PP-LFER 1.55 COSMOmic exp. 2010) Venlafaxine 3.40 PP-LFER 9.5 (Prankerd, 2007) 2.76 PP-LFER 1.80 COSMOmic PhysProp Verapamil 3.79 8.92 (Hasegawa et al., 1984) 3.82 PP-LFER 1.27 COSMOmic exp. COMPLEX & MULTIPROTIC PHARMACEUTICALS 2.61(A);3.7 3.13 (anion), 3.13 Candesartan 4.21 ppLFER 3(A); ACD/pKa GALAS 4.91 pp-LFER COSMOmic (dianion) 4.85(B) 2.2 (B), 2.9 (Plemper van Balen 2.3 (zwitterion and (Plemper van Balen et al., Cetirizine 3.96 PP-LFER 3.60 pp-LFER (A), 8.0 (B) et al., 2001) anion), 3.2 (cation) 2001) 3.0 (A); 5.5 (Loftsson et al., 1.39 (anion), 0.34 Enalapril 0.07 PP-LFER 2.66 pp-LFER COSMOmic (B) 2010) (zwitterion) 4.25 (A); 4.31 (cation), 3.31 (Yasui-Furukori et Fexofenadine 7.21 PP-LFER 9.53 (B) 6.58 pp-LFER (zwitterion), 5.1 COSMOmic al., 2005) (anion) 7. (A)2; (Zielonka et al., 3.30 (anion), 3.7 Genistein 3.08 PP-LFER 10.0 (A); 3.65 PP-LFER COSMOmic 2003) (dianion) 13.1 (A) 3.7 (A); 1.2 (zwitterion), Irbesartan 6.38 PP-LFER ACD/pKa GALAS 6.54 pp-LFER COSMOmic 10.2 (B) 2.13 (anion) 7.35 (A), 2.32 (cation), 1.84 Labetalol 2.55 PP-LFER 9.11 (B) ACD/pKa GALAS 2.20 pp-LFER (anion), 3.01 COSMOmic (zwitterion) 3.65 (A); 1.59 (zwitterion), Telmisartan 7.74 PP-LFER 4.78 (B); (Chemaxon, 2016) 7.81 pp-LFER COSMOmic 5.01 (zwitterion) 6.54 (B) 3.9 (A); Valsartan 3.84 PP-LFER (Flesch et al., 1997) 5.00 pp-LFER 2.99 (dianion) COSMOmic 4.73 (A) a b PhysProp database accessed via Episuite (U.S.
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