• Bosse JA, Wassermann O (1970). On the blood content of guinea-pig tissues. Pharmacology 4: 273277.
  • Chen C, Hanson E, Watson JW, Lee JS (2003). P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos 31: 312318.
  • Christophe B, Carlier B, Gillard M, Chatelain P, Peck M, Massingham R (2003). Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics. Eur J Pharmacol 470: 8794.
  • De Vos C, Maleux MR, Baltes E, Gobert J (1987). Inhibition of histamine and allergen skin wheal by cetirizine in four animal species. Ann Allergy 59: 278282.
  • Devalia JL, De Vos C, Hanotte F, Baltes E (2001). A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers. Allergy 56: 5057.
  • Gillard M, Van Der Perren C, Moguilevsky N, Massingham R, Chatelain P (2002). Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194). Mol Pharmacol 61: 391399.
  • Gupta A, Chatelain P, Massingham R, Jonsson EN, Hammarlund-Udenaes M (2006). Brain distribution of cetirizine enantiomers: Comparison of three different tissue-to-plasma partition coefficients: Kp, Kp, u, and Kp, uu. Drug Metab Dispos 34: 318323.
  • Hammarlund-Udenaes M, Paalzow LK, De Lange EC (1997). Drug equilibration across the blood-brain barrier – pharmacokinetic considerations based on the microdialysis method. Pharm Res 14: 128134.
  • Hindmarch I, Johnson S, Meadows R, Kirkpatrick T, Shamsi Z (2001). The acute and sub-chronic effects of levocetirizine, cetirizine, loratadine, promethazine and placebo on cognitive function, psychomotor performance, and weal and flare. Curr Med Res Opin 17: 241255.
  • Hindmarch I, Shamsi Z (1999). Antihistamines: models to assess sedative properties, assessment of sedation, safety and other side-effects. Clin Exp Allergy 29 (Suppl 3): 133142.
  • Kay GG (2000). The effects of antihistamines on cognition and performance. J Allergy Clin Immunol 105: S622S627.
  • Kreutner W, Hey JA, Chiu P, Barnett A (2000). Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist. 2nd communication: lack of central nervous system and cardiovascular effects. Arzneimittelforschung 50: 441448.
  • Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ et al. (2002). Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther 303: 10291037.
  • Polli JW, Baughman TM, Humphreys JE, Jordan KH, Mote AL, Salisbury JA et al. (2003). P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec(R)), a second-generation non-sedating antihistamine. J Pharm Sci 92: 20822089.
  • Snowman AM, Snyder SH (1990). Cetirizine: actions on neurotransmitter receptors. J Allergy Clin Immunol 86: 10251028.
  • Syvanen S, Xie R, Sahin S, Hammarlund-Udenaes M (2006). Pharmacokinetic consequences of active drug efflux at the blood-brain barrier. Pharm Res 23: 705717.
  • Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y et al. (2001). Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol 52: 501509.
  • Tamai I, Kido Y, Yamashita J, Sai Y, Tsuji A (2000). Blood-brain barrier transport of H1-antagonist ebastine and its metabolite carebastine. J Drug Target 8: 383393.
  • Tashiro M, Mochizuki H, Iwabuchi K, Sakurada Y, Itoh M, Watanabe T et al. (2002). Roles of histamine in regulation of arousal and cognition: functional neuroimaging of histamine H1 receptors in human brain. Life Sci 72: 409414.
  • Van Rossum JM, Hurkmans JATM, Wolters CJJ (1963). Cumulative dose–response curves. II. Technique for the making of dose–response curves in isolated organs and the evaluation of drug parameters. Arch Int Pharmacodyn Ther 143: 299330.
  • Verster JC, De Weert AM, Bijtjes SI, Aarab M, Van Oosterwijck AW, Eijken EJ et al. (2003a). Driving ability after acute and sub-chronic administration of levocetirizine and diphenhydramine: a randomized, double-blind, placebo-controlled trial. Psychopharmacology (Berlin) 169: 8490.
  • Verster JC, Volkerts ER, Van Oosterwijck AW, Aarab M, Bijtjes SI, De Weert AM et al. (2003b). Acute and subchronic effects of levocetirizine and diphenhydramine on memory functioning, psychomotor performance, and mood. J Allergy Clin Immunol 111: 623627.
  • Watanabe T, Yanai K (2001). Studies on functional roles of the histaminergic neuron system by using pharmacological agents, knockout mice and positron emission tomography. Tohoku J Exp Med 195: 197217.
  • Wiech NL, Martin JS (1982). Absence of an effect of terfenadine on guinea pig brain histamine H1-receptors in vivo determined by receptor binding techniques. Arzneimittelforschung 32: 11671170.
  • Yakuo I, Yabuuchi M, Ito T (2001). Preclinical comparison of ebastine and other second generation H1-antihistamines. Pharmacol Toxicol 89: 171176.
  • Yanai K, Okamura N, Tagawa M, Itoh M, Watanabe T (1999). New findings in pharmacological effects induced by antihistamines: from PET studies to knock-out mice. Clin Exp Allergy 29 (Suppl 3): 2936.