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We report the synthesis of two new acyclic sulfated acyclic CB[n]-type receptors ( TriM0 and Me 4 TetM0 ) and investigations of their binding properties toward a panel of drugs of abuse ( 1 - 13 ) by a combination of 1 H NMR spectroscopy and isothermal titration calorimetry. TetM0 is the most potent receptor with K a ≥ 10 6 M -1 toward methamphetamine, fentanyl, MDMA and mephedrone. TetM0 is not cytotoxic toward HepG2 and HEK 293 cells below 100 m M according to MTS metabolic and adenylate kinase release assays and is well tolerated in v