• 1
    Yanai K, Tashiro M. The physiological and pathophysiological roles of neuronal histamine: an insight from human positron emission tomography studies. Pharmacol Ther 2007; 113: 115.
  • 2
    Haas H, Panula P. The role of histamine and the tuberomamillary nucleus in the nervous system. Nat Rev Neurosci 2003; 4: 12130.
  • 3
    Holgate ST, Canonica GW, Simons FE, Taglialatela M, Tharp M, Timmerman H, Yanai K. Consensus Group on New-Generation Antihistamines (CONGA): present status and recommendations. Clin Exp Allergy 2003; 33: 130524.
  • 4
    Casale TB, Blaiss MS, Gelfand E, Gilmore T, Harvey PD, Hindmarch I, Simons FE, Spangler DL, Szefler SJ, Terndrup TE, Waldman SA, Weiler J, Wong DF. First do no harm: managing antihistamine impairment in patients with allergic rhinitis. J Allergy Clin Immunol 2003; 111: S83542.
  • 5
    Brown RE, Stevens DR, Haas HL. The physiology of brain histamine. Prog Neurobiol 2001; 63: 63772.
  • 6
    Yanai K, Ryu JH, Watanabe T, Iwata R, Ido T, Sawai Y, Ito K, Itoh M. Histamine H1 receptor occupancy in human brains after single oral doses of histamine H1 antagonists measured by positron emission tomography. Br J Pharmacol 1995; 116: 164955.
  • 7
    Okamura N, Yanai K, Higuchi M, Sakai J, Iwata R, Ido T, Sasaki H, Watanabe T, Itoh M. Functional neuroimaging of cognition impaired by a classical antihistamine, d-chlorpheniramine. Br J Pharmacol 2000; 129: 11523.
  • 8
    Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y, Arai H, Iwata R, Fujii T, Komemushi S, Ido T, Itoh M, Sasaki H, Watanabe T, Yanai K. 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 2001; 52: 5019.
  • 9
    Tashiro M, Sakurada Y, Iwabuchi K, Mochizuki H, Kato M, Aoki M, Funaki Y, Itoh M, Iwata R, Wong DF, Yanai K. Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography. J Clin Pharmacol 2004; 44: 890900.
  • 10
    Tashiro M, Mochizuki H, Sakurada Y, Ishii K, Oda K, Kimura Y, Sasaki T, Ishiwata K, Yanai K. Brain histamine H receptor occupancy of orally administered antihistamines measured by positron emission tomography with (11)C-doxepin in a placebo-controlled crossover study design in healthy subjects: a comparison of olopatadine and ketotifen. Br J Clin Pharmacol 2006; 61: 1626.
  • 11
    Ishibashi Y, Kawashima M, Harada S, Suzuki Y. [Phase I study of antiallergic agent, TAU-284 (betotastine besilate): study of inhibitory effect on intradermal reaction of histamine]. J Clin Therap Med 1997; 13: 5363.
  • 12
    Yokota H, Mizuuchi H, Maki T, Banno K, Sato T. [Phase I study of TAU-284: single oral administration in healthy male volunteers]. J Clin Therap Med 1997; 13: 319.
  • 13
    Kawashima M, Harada S, Nakajima M. [Phase III study of TAU-284 (betotastine besilate) on chronic urticaria: a multicenter double blind comparative study with placebo]. J Clin Therap Med 2002; 18: 1331.
  • 14
    Murata T, Matsumoto Y, Suzuki T, Naito K, Takata I, Tsuzurahara K. [Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitis]. Arerugi 1997; 46: 57684.
  • 15
    Yato N, Murata T, Saito N, Sakai A, Kikuchi M, Tsuzurahara K, Narita H. [Anti-allergic activity of betotastine besilate (TAU-284), a new anti-allergic drug]. Nippon Yakurigaku Zasshi 1997; 110: 1929.
  • 16
    Ueno M, Inagaki N, Nagai H, Koda A. Antiallergic action of betotastine besilate (TAU-284) in animal models: a comparison with ketotifen. Pharmacology 1998; 57: 20614.
  • 17
    Nakahara T, Urabe K, Moroi Y, Morita K, Furue M. Bepotastine besilate rapidly inhibits mite-antigen induced immediate reactions in atopic dermatitis. J Dermatol Sci 2003; 32: 2378.
  • 18
    Takahashi H, Ishida-Yamamoto A, Iizuka H. Effects of bepotastine, cetirizine, fexofenadine, and olopatadine on histamine-induced wheal-and flare-response, sedation, and psychomotor performance. Clin Exp Dermatol 2004; 29: 52632.
  • 19
    Kato M, Nishida A, Aga Y, Kita J, Kudo Y, Narita H, Endo T. Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate. Arzneimittelforschung 1997; 47: 111624.
  • 20
    Kay GG, Harris AG. Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy 1999; 29 (Suppl. 3): 14750.
  • 21
    Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y, Arai H, Fujii T, Komemushi S, Itoh M, Sasaki H, Watanabe T, Yanai K. Differential cognitive effects of ebastine and (+)-chlorpheniramine in healthy subjects: correlation between cognitive impairment and plasma drug concentration. Br J Clin Pharmacol 2002; 53: 296304.
  • 22
    Hindmarch I, Shamsi Z, Kimber S. An evaluation of the effects of high-dose fexofenadine on the central nervous system: a double-blind, placebo-controlled study in healthy volunteers. Clin Exp Allergy 2002; 32: 1339.
  • 23
    Tashiro M, Horikawa E, Mochizuki H, Sakurada Y, Kato M, Inokuchi T, Ridout F, Hindmarch I, Yanai K. Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use. Hum Psychopharmacol 2005; 20: 5019.
  • 24
    Kumar S, Rurak DW, Riggs KW. Simultaneous determination of diphenhydramine, its N-oxide metabolite and their deuterium-labeled analogues in ovine plasma and urine using liquid chromatography/electrospray tandem mass spectrometry. J Mass Spectrom 1998; 33: 117181.
  • 25
    Kanba S, Richelson E. Histamine H1 receptors in human brain labelled with [3H]doxepin. Brain Res 1984; 304: 17.
  • 26
    Inoue I, Yanai K, Kitamura D, Taniuchi I, Kobayashi T, Niimura K, Watanabe T, Watanabe T. Impaired locomotor activity and exploratory behavior in mice lacking histamine H1 receptors. Proc Natl Acad Sci USA 1996; 93: 1331620.
  • 27
    Iwata R, Pascali C, Bogni A, Miyake Y, Yanai K, Ido T. A simple loop method for the automated preparation of (11C) raclopride from (11C) methyl triflate. Appl Radiat Isot 2001; 55: 1722.
  • 28
    Nakamura T, Hayashi Y, Watabe H, Matsumoto M, Horikawa T, Fujiwara T, Ito M, Yanai K. Estimation of organ cumulated activities and absorbed doses on intakes of several 11C labelled radiopharmaceuticals from external measurement with thermoluminescent dosimeters. Phys Med Biol 1998; 43: 389405.
  • 29
    Fujiwara T, Watanuki S, Yamamoto S, Miyake M, Seo S, Itoh M, Ishii K, Orihara H, Fukuda H, Satoh T, Kitamura K, Tanaka K, Takahashi S. Performance evaluation of a large axial field-of-view PET scanner SET-2400w. Ann Nucl Med 1997; 11: 30713.
  • 30
    Bergstrom M, Eriksson L, Bohm C, Blomqvist G, Litton J. Correction for scattered radiation in a ring detector positron camera by integral transformation of the projections. J Comput Assist Tomogr 1983; 7: 4250.
  • 31
    Inoue T, Oriuchi N, Kunio M, Tomiyoshi K, Tomaru Y, Aoyagi K, Amano S, Suzuki H, Aoki J, Sato T, Endo K. Accuracy of standardized uptake value measured by simultaneous emission and transmission scanning in PET oncology. Nucl Med Commun 1999; 20: 84957.
  • 32
    Mochizuki H, Kimura Y, Ishii K, Oda K, Sasaki T, Tashiro M, Yanai K, Ishiwata K. Simplified PET measurement for evaluating histamine H1 receptors in human brains using [11C]doxepin. Nucl Med Biol 2004; 31: 100511.
  • 33
    Friston KJ, Holmes AP, Worsley KJ, Poline JP, Frith CD, Frackowiak RSJ. Statistical parametric maps in functional imaging: a general linear approach. Hum Brain Mapp 1995; 2: 189210.
  • 34
    Martinez D, Hwang D, Mawlawi O, Slifstein M, Kent J, Simpson N, Parsey RV, Hashimoto T, Huang Y, Shinn A, Van Heertum R, Abi-Dargham A, Caltabiano S, Malizia A, Cowley H, Mann JJ, Laruelle M. Differential occupancy of somatodendritic and postsynaptic 5HT (1A) receptors by pindolol: a dose-occupancy study with [11C]WAY 100635 and positron emission tomography in humans. Neuropsychopharmacology 2001; 24: 20929.
  • 35
    Rabiner EA, Wilkins MR, Turkheimer F, Gunn RN, De Haes JU, De Vries M, Grasby PM. 5-Hydroxytryptamine1A receptor occupancy by novel full antagonist 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzdioxyn-5-yl)-1-piperazinyl]butyl]-1,2-benzisothiazol-3-(2H)-one-1,1-dioxide: a[11C][O-methyl-3H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl) ethyl) -N-(2-py ridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) positron emission tomography study in humans. J Pharmacol Exp Ther 2002; 301: 114450.
  • 36
    Talairach J, Tournoux P. Co-planar Stereotaxic Atlas of the Human Brain. Stuttgart: Georg Thieme Verlag, 1988.
  • 37
    Van Rij CM, Huitema AD, Swart EL, Greuter HN, Lammertsma AA, Van Loenen AC, Franssen EJ. Population plasma pharmacokinetics of 11C-flumazenil at tracer concentrations. Br J Clin Pharmacol 2005; 60: 47785.
  • 38
    Martinez D, Broft A, Laruelle M. Imaging neurochemical endophenotypes: promises and pitfalls. Pharmacogenomics 2001; 2: 22337.
  • 39
    Yanai K, Okamura N, Tagawa M, Itoh M, Watanabe T. New findings in pharmacological effects induced by antihistamines: from PET studies to knock-out mice. Clin Exp Allergy 1999; 29 (Suppl. 3): 2936; discussion 37–8.
  • 40
    Yanai K, Ryu JH, Watanabe T, Iwata R, Ido T, Asakura M, Matsumura R, Itoh M. Positron emission tomographic study of central histamine H1-receptor occupancy in human subjects treated with epinastine, a second-generation antihistamine. Methods Find Exp Clin Pharmacol 1995; 17 (Suppl. C): 649.
  • 41
    Hindmarch I, Shamsi Z, Stanley N, Fairweather DB. A double-blind, placebo-controlled investigation of the effects of fexofenadine, loratadine and promethazine on cognitive and psychomotor function. Br J Clin Pharmacol 1999; 48: 2006.
  • 42
    Dogan AS, Catafau AM, Zhou Y, Yanai K, Ravert H, Brasic J, Hilton J, Dannals B, Offord S, Wong DF. In vivo cerebral histamine receptor occupancy of three antihistamine drugs: an 11C-doxepin PET study. J Nucl Med 2001; 42: 143P144P.
  • 43
    Ohashi R, Kamikozawa Y, Sugiura M, Fukuda H, Yabuuchi H, Tamai I. Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos 2006; 34: 7939.
  • 44
    Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, Kim RB. OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos 1999; 27: 86671.
  • 45
    Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I. Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther 2004; 308: 43845.