Consensus group on new‐generation antihistamines (CONGA): present status and recommendations
2003; Wiley; Volume: 33; Issue: 9 Linguagem: Inglês
10.1046/j.1365-2222.2003.01769.x
ISSN1365-2222
AutoresStephen T. Holgate, Giorgio Walter Canonica, F. Estelle R. Simons, Maurizio Taglialatela, Marjorie Tharp, H. Timmerman, Kazuhiko Yanai,
Tópico(s)Asthma and respiratory diseases
ResumoClinical & Experimental AllergyVolume 33, Issue 9 p. 1305-1324 Consensus group on new-generation antihistamines (CONGA): present status and recommendations S. T. Holgate, S. T. Holgate (chairman)Search for more papers by this authorG. W. Canonica, G. W. CanonicaSearch for more papers by this authorF. E. R. Simons, F. E. R. SimonsSearch for more papers by this authorM. Taglialatela, M. TaglialatelaSearch for more papers by this authorM. Tharp, M. TharpSearch for more papers by this authorH. Timmerman, H. TimmermanSearch for more papers by this authorK. Yanai, K. YanaiSearch for more papers by this authorThis Consensus Group was convened under the auspices of the British Society for Allergy and Clinical Immunology., This Consensus Group was convened under the auspices of the British Society for Allergy and Clinical Immunology.Search for more papers by this author S. T. Holgate, S. T. Holgate (chairman)Search for more papers by this authorG. W. Canonica, G. W. CanonicaSearch for more papers by this authorF. E. R. Simons, F. E. R. SimonsSearch for more papers by this authorM. Taglialatela, M. TaglialatelaSearch for more papers by this authorM. Tharp, M. TharpSearch for more papers by this authorH. Timmerman, H. TimmermanSearch for more papers by this authorK. Yanai, K. YanaiSearch for more papers by this authorThis Consensus Group was convened under the auspices of the British Society for Allergy and Clinical Immunology., This Consensus Group was convened under the auspices of the British Society for Allergy and Clinical Immunology.Search for more papers by this author First published: 22 September 2003 https://doi.org/10.1046/j.1365-2222.2003.01769.xCitations: 138 Stephen T Holgate, MRC Clinical Professor of Immunopharmacology, IIR Division, Mailpoint 810, Level D, Centre Block, Southampton General Hospital, Southampton SO16 6YD, UK. E-mail: [email protected] Read the full textAboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onEmailFacebookTwitterLinkedInRedditWechat References 1 Hanifin JM. The role of antihistamines in atopic dermatitis. J Allergy Clin Immunol 1990; 86: 666 – 9. 2 Sabbah A. The rebirth of the H1-antagonists. Allergie Immunol 1992; 24: 224 – 30. 3 Caproni M, Palleschi GM, Falcos D, Papi C, Lotti T. Pharmacologic modulation by cetirizine of some adhesion molecules expression in psoriatic skin lesions. Int J Dermatol 1995; 34: 510 – 3. 4 Pagliara A, Testa B, Carrupt P-A et al. Molecular properties and pharmacokinetic behaviour of cetirizine, a zwitterionic H1-receptor antagonist. J Med Chem 1998; 41: 853 – 63. 5 Moguilevsky N, Varsalona F, Guillaume JP et al. Pharmacological and functional characterization of the wild-type and site directed mutants of the human H1 histamine receptor stably expressed in CHO cells. J Receptor Signal Transduc Res 1995; 15: 91 – 102. 6 Ohta K, Hayashi H, Mizugichi H et al. Site-directed mutagenesis of the histamine H1 receptor: roles of aspartic acid107, asparagine198, and threonine194. Biochem Biophys Res Commun 1994; 203: 1096 – 101. 7 Leurs R, Smit MJ, Tensen CP et al. Site-directed mutagenesis of the histamine H1 receptor reveals a selective interaction of asparagine207 with subclasses of H1 receptor agonists. Biochem Biopys Res Commun 1994; 201: 295 – 301. 8 Timmerman H. Why are non-sedating antihistamines non sedating ? Clin Exp Allergy 1999; 29 (Suppl. 3): 13 – 8. 9 Smit MJ, Hoffman M, Timmerman H, Leurs R. Molecular properties and signalling pathways of the histamine H1 receptor. Clin Exp Allergy 1999; 29 (Suppl. 3): 19 – 28. 10 Bakker RA, Wieland K, Timmerman H, Leurs R. Constitutive activity of the histamine H1 receptor reveals inverse agonism of histamine H1 receptor antagonists. Eur J Pharmacol 2000; 387: R5 – 7. 11 Timmerman H. Factors involved in the absence of sedative effects by the second-generation antihistamines. Allergy 2000; 55: 1 – 6. 12 Rapoport SI. Modulation of blood brain barrier permeability. J Drug Target 1996; 3: 417 – 25. 13 Hindmarch I, Shamsi Z. Antihistamines: Models to assess sedative properties, assessment of sedation, safety and side-effects. Clin Exp Allergy 1999; 29 (Suppl. 3): 133 – 42. 14 Yanai K, Okamura A, Tagawa M et al. New findings in pharmacological effects induced by antihistamines: from PET studies to knock out mice. Clin Exp Allergy 1999; 29 (Suppl. 3): 29 – 36. 15 Zhang M-Q. Chemistry underlying the cardiotoxicity of antihistamines. Curr Med Chem 1997; 4: 171 – 84. 16 Edwards DJ, Bellevue II, Woster PM. Identification of 6′7′-dihydroxybergamottin, a cytochrome P450 inhibitor in grapefruit juice. Drug Metab Dispos 1996; 24: 1287 – 90. 17 Rau SE, Bend JR, Arnold JMO et al. Grapefruit juice-terfenadine single-dose interaction: magnitude, mechanism and relevance. Clin Pharmacol Ther 1997; 61: 401 – 9. 18 Clifford CP, Adams DA, Murray S et al. The cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice. Eur J Clin Pharmacol 1997; 52: 311 – 5. 19 Renwick AG. The metabolism of antihistamines and drug interactions: the role of cytochrome P450 enzymes. Clin Exp Allergy 1999; 29 (Suppl. 3): 116 – 24. 20 Handley DA, McCullough JR, Fang Y et al. Descarboethoxyloratadine is a superior antihistamine. Ann Allergy Asthma Immunol 1997; 78: 143 (Abstract). 21 Nicolas JM, Whomsley R, Collard P, Roba J. In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem-Biol Interact 1999; 123: 63 – 79. 22 Hamelin BA, Bouayad A, Drolet B, Gravel A, Turgeon J. In vitro characterization of cytochrome P450 2D6 by classic histamine H receptor antagonists. Drug Metab Dispos 1998; 26: 536 – 9. 23 Jones BC, Hyland R, Ackland M et al. Interaction of terfenadine and its primary metabolites with cytochrome P450 2D6. Mol Pharmacol 1998; 26: 875 – 82. 24 Woolsey RL, Chen Y, Freiman JP, Gilles RA. Mechanism of the cardiotoxic actions of terfenadine. J Am Med Assoc 1993; 269: 1532 – 6. 25 Salata JJ, Jurkiewicz NK, Wallace AA et al. Cardiac electrophysiological actions of the histamine H 1-receptor antagonists astemizole and terfenadine compared with chloropheniramine and prilamine. Circ Res 1995; 76: 110 – 9. 26 Suessbrich H, Waldegger S, Lang F, Busch AE. Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. FEBS Lett 1996; 385: 77 – 80. 27 De Buske LM. Second generation antihistamines: the risk of ventricular arrhythmias. Clin Ther 1999; 21: 281 – 95. 28 Crumb W. Loratadine blockade of K+ channels in human heart: Comparison with terfenadine under physiological conditions. J Pharmacol Exp Ther 2000; 292: 261 – 4. 29 Caballero R, Delpaaon E, Valenzuela C et al. Effect of descarboethoxyloratadine, the major metabolite of loratadine on the human cardiac potassium channel kv1.5. Br J Pharmacol 1997; 122: 796 – 8. 30 Crumb WJ. Rate dependent blockade of a potassium current in human atrium by the antihistamine loratadine. Br J Pharmacol 1999; 126: 575 – 80. 31 Church MK. Non-H1-receptor effects of antihistamines. Clin Exp Allergy 1999; 29 (Suppl. 3): 39 – 48. 32 Sehmi R, Walsh G, Hartnell A et al. Modulation of human eosinophil chemotaxis and adhesion by anti-allergic drugs in vitro. Pediatr Allergy Immunol 1993; 4 (Suppl. 4): 13 – 8. 33 Fadel R, Heprin-Richard N, Rihoux J-P, Henocq E. Inhibitory effect of oral cetirizine on eosinophil migration in vivo. Clin Allergy 1987; 17: 373 – 9. 34 Charlesworth EN, Kagey-Sobotka A, Norman PS, Lichtenstein LM. Effect of cetirizine on mast cell mediator release and cellular traffic during the cutaneous late-phase reaction. J Allergy Clin Immunol 1989; 83: 905 – 12. 35 Fadel R, Heprin-Richard N, Dufresne F, Rihoux J-P. Pharmacological modulation by cetirizine and loratadine of antigen- and histamine-induced skin wheals and flares and late accumulation of eosinophils. J Int Med Res 1990; 18: 366 – 71. 36 Ciprandi G, Pronzato C, Ricca V et al. Loratdine reduces ICAM-1 expression on conjunctiva after specific challenge in pollen allergic patients. Allergy 1998; 53: 545 – 6. 37 Ciprandi G, Buscaglia S, Pesce G et al. Cetirizine reduces inflammatory cell recruitment and ICAM-1 (CD54) expression on conjunctival epithelium in both early and late phase reactions after allergen challenge. J Allergy Clin Immunol 1995; 95: 612 – 21. 38 ETAC study group. Allergic factors associated with the development of asthma and the influence of cetirizine on this progression in a double-blind, randomised, placebo-controlled trial: first results of ETAC. Ped Allergy Immunol 1998; 9: 116 – 24. 39 Van Ganse E, Kaufman L, Derde MP et al. Effects of antihistamines in adult asthma: a meta-analysis of clinical trials. Eur Respir J 1997; 10: 2216 – 24. 40 Corren J, Harris AG, Aaronson D et al. Efficacy and safety of loratadine plus pseudoephredine in patients with seasonal allergic rhinitis and mild asthma. J Allergy Clin Immunol 1997; 100: 781 – 8. 41 Grant JA, Nicodemus CF, Findlay SR et al. Cetirizine in patients with seasonal rhinitis and concomitant asthma: prospective, randomized, placebo-controlled trial. J Allergy Clin Immunol 1995; 95: 923 – 32. 42 Handley DA, Magnetti A, Higgins AJ. Therapeutic advantages of third generation antihistamines. Exp Opinion Invest Drugs 1998; 7: 1045 – 54. 43 Segura T, Casale P. Allergic rhinitis: basic pathophysiology and therapeutic strategies. Can J Allergy Clin Immunol 1999; 4: 18 – 30. 44 McFadden ER. What new pharmacological trends could mean for allergy and asthma treatment. American College of Allergy Asthma & Immunology Annual Meeting 1999. Day 1, November 12. 45 Holgate ST, (Chair). Antihistamines: back to the future, summary of the conclusions. Clin Exp Allergy 1999; 29 (Suppl. 3): iv – vi. 46 Timmerman H. European Academy of Allergology and Clinical Immunology; requirements for anti-allergic treatment in the new millennium. Third Generation Antihistamines: Feasible or a Dream? Brussels, 3–7 July 1999. 47 Abdelaziz MM, Khair OA, Devalia JL. The potential of active metabolites in the management of allergic disease. Allergy 2000; 55: 425 – 34. 48 Kay AB. Allergy and allergic diseases. Second of two parts. N Engl J Med 2001; 344: 109 – 13. 49 Borish LC, Nelson H, Lanz MJ et al. Interleukin-4 receptor in moderate atopic asthma. A phase I/II randomized, placebo-controlled trial. Am J Respir Crit Care Med 1999; 160: 1816 – 23. 50 Leckie MJ, Ten Bincke A, Khan J et al. Effects of an interleukin-5 blocking monoclonal antibody on eosinophils, airway hyper-responsiveness, and the late asthmatic response. Lancet 2000; 356: 2144 – 8. 51 Donnelly AL, Glass M, Minkwitz T, Casale TB. The leukotriene D4 receptor antagonist ICI204,219 relieves symptoms of acute seasonal allergic rhinitis. Am J Respir Crit Care Med 1995; 151: 1734 – 9. 52 Pullerits T, Praks L, Skoog BE et al. Randomized placebo controlled study comparing a leukotriene receptor antagonist and a nasal glucocorticoid in seasonal allergic rhinitis. Am J Respir Crit Care Med 1999; 159: 1814 – 8. 53 Casale TB, Bernstein IL, Busse WW et al. Use of an anti IgE humanized monoclonal antibody in ragweed induced allergic rhinitis. J Allergy Clin Immunol 1997; 100: 110 – 21. 54 Milgrom H, Fick RB, Su JQ et al. Treatment of allergic asthma with monoclonal anti IgE antibody. N Engl J Med 1999; 341: 1966 – 73. 55 Mor S, Nagler A, Barak V, Handzel ZT, Geller-Bernstein C, Fabian I. Histamine enhances granulocyte-macrophage colony-stimulating factor and interleukin-6 production by human peripheral blood mononuclear cells. J Leukoc Biol 1995; 58: 445 – 50. 56 Schmidt J, Fleissner S, Heimann-Weitschat I, Lindstaedt R, Szelenyi I. Histamine increases anti-CD3 induced IL-5 production of TH2-type T cells via histamine H2-receptors. Agents-Actions 1994; 42: 1 – 85. 57 Jeannin P, Delneste Y, Gosset P et al. Histamine induces interleukin-8 secretion by endothelial cells. Blood 1994; 84: 2229 – 33. 58 Delneste Y, Lassalle P, Jeannin P, Joseph M, Tonnel AB, Gosset P. Histamine induces IL-6 production by human endothelial cells. Clin Exp Immunol 1994; 98: 44 – 9. 59 Meltzer EO. Concomitant montelukast and loratadine as treatment for seasonal allergic rhinitis: a randomized, placebo-controlled clinical trial. J Allergy Clin Immunol 2000; 105: 917 – 22. 60 Wilson AM, Orr LC, Sims EJ, Lipworth BJ. Effects of monotherapy with intra-nasal corticosteroid or combined oral histamine and leukotriene receptor antagonists in seasonal allergic rhinitis. Clin Exp Allergy 2001; 31: 61 – 8. 61 Leurs R, Church MK, Taglialatela M. H1 antihistamines: inverse agonism, antiinflammatory actions and cardiac effects. Clin Exp Allergy 2002: 489 – 98. 62 Baarody FM, Naclerio RM. Antiallergic effects of H1-receptor antagonists. Allergy 2000; 55 (Suppl. 64): 17 – 27. 63 Marshall GD Jr. Therapeutic options in allergic disease: antihistamines as systemic antiallergic agents. J Allergy Clin Immunol 2000; 106 (Suppl. 5): S303 – 9. 64 Ciprandi G, Passalacqua G, Canonica GW. Effect of H1 antihistamines on adhesion molecules: a possible rationale for long term treatment. Clin Exp Allergy 1999; 29: 49 – 52. 65 Perzanowska M, Malhotra D, Skinner SP et al. The effect of cetirizine and loratadine on codeine induced histamine release in human skin assessed by microdialysis. Inflam Res 1996; 45: 486 – 90. 66 Ciprandi G, Tosca M, Passalacqua G et al. Continuous versus on demand treatment with cetirizine for allergic rhinitis. Ann Allergy Asthma Immunol 1997; 79: 507 – 11. 67 Ciprandi G, Pronzato C, Ricca V et al. Loratadine treatment of rhinitis due to pollen allergy reduces epithelial ICAM-1 expression. Clin Exp Allergy 1997; 27: 1175 – 83. 68 Wang DY, Hanotte F, De Vos C, Clement P. Effect of cetirizine, levocetirizine and dextrocetirizine on histamine-induced nasal response in healthy adult volunteers. Allergy 2001; 56: 339 – 43. 69 Wang D, Clement P, Smitz J. Effect of H1 and H2 antagonists on nasal symptoms and mediator release in atopic patients after nasal allergen challenge during the pollen season. Acta Otolaryngol (Stockh) 1996; 116: 91 – 6. 70 Simons FER. H1-antihistamines: more relevant than ever in the treatment of allergic disorders. J Allergy Clin Immunol 2003; 112, (in press). 71 Bousquet J, Van Cauwenberge PB et al. Allergic rhinitis and its impact on asthma. J Allergy Clin Immunol 2001; 108 (part 2): S147 – S334. 72 Kaplan AP. Clinical practice. Chronic urticaria and angioedema. N Engl J Med 2002; 346: 175 – 9. 73 Spencer CM, Faulds D, Peters DH. Cetirizine. A reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. Drugs 1993; 46: 1055 – 80. 74 Geha RS, Meltzer EO. Desloratadine: a new, nonsedating, oral antihistamine. J Allergy Clin Immunol 2001; 107: 752 – 62. 75 Hurst M, Spencer CM. Ebastine. An update of its use in allergic disorders. Drugs 2000; 59: 981 – 1006. 76 Simons FER. Fexofenadine. J Drug Eval 2002; 1: 13 – 33. 77 Xyzal product monograph. UCB Pharma, 2001. 78 Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs 1994; 48: 617 – 37. 79 Simons FER. Mizolastine: antihistaminic activity from preclinical data to clinical evaluation. Clin Exp Allergy 1999; 29 (Suppl. 1): 3 – 8. 80 Simons FER, Simons KJ. Clinical pharmacology of new histamine H1-receptor antagonists. Clin Pharmacokinet 1999; 36: 329 – 52. 81 Juniper EF. Quality of life in adults and children with asthma and rhinitis. Allergy 1997; 52: 971 – 7. 82 Welch MJ, Meltzer EO, Simons FER. H1-antihistamines and the central nervous system. In: FER Simons, ed. Histamine and H1– antihistamines in allergic disease, 2nd Edn. New York: Marcel Dekker, Inc., 2002: 337 – 88. 83 Yap YG, Camm J. Risk of torsades de pointes with non-cardiac drugs. Doctors need to be aware that many drugs can cause QT prolongation. Br Med J 2000; 320: 1158 – 9. 84 Committee for Proprietary Medicinal Products (CPMP/ICH/423/02). Safety pharmacologicy studies for assessing the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals. EMEA ICH S7B, February 2002. 85 Shieh C-C, Coghlan M, Sullivan JP, Gopalakrishnan M. Potassium channels: molecular defects, diseases, and therapeutic opportunities. Pharmacol Rev 2000; 52: 557 – 93. 86 Taglialatela M, Timmerman H, Annunziato L. Cardiotoxic potential and CNS effects of first-generation antihistamines. Trends in Pharmacol Sci 2000; 21: 52 – 6. 87 Taglialatela M. Heterologous expression systems and screening technologies in ion channel drug discovery. In: MK Pugsley, ed. Cardiac drug development guide. Totowa, NJ: Humana Press, 2002, (in press). 88 Woosley RL. Cardiac actions of antihistamines. Annu Rev Pharmacol Toxicol 1996; 36: 233 – 52. 89 Morganroth J, Brozovich FV, McDonald JT, Jacobs RA. Variability of the QT measurement in healthy men, with implications for selection of an abnormal QT value to predict drug toxicity and proarrhythmia. Am J Cardiol 1991; 67: 774 – 6. 90 http://www.dml.georgetown.edu/depts/pharmacology/torsades.html 91 Pratt CM, Ruberg S, Morganroth J et al. The dose response relationship between terfenadine (Seldane) and the QTc interval on the scalar electrocardiogram in normals and patients with cardiovascular diseases and the QTc interval variability. Am Heart J 1996; 131: 472 – 80. 92 Gonzalea MA, Estes KS. Pharmacokinetic overview of oral second-generation H1 antihistamines. Int J Clin Pharmacol Ther 1998; 36: 292 – 300. 93 Tozer TN. Concepts basic to pharmacokinetics. Pharmacol Ther 1981; 12: 109 – 31. 94 Tillement J-P. A low distribution, as a determinant of efficacy and safety for histamine (H1) antagonists. Allergy 1995; 50: 12–16. 95 Tillement J-P. The apparent volumes of distribution of H1 receptor antagonists. Dermatologic Ther 2000; 13: 337 – 43. 96 Testa JB, Pagliara A, Carrupt P-A. The molecular behavior of cetirizine. Clin Exp Allergy 1997; 27: 13 – 8. 97 Simons FER. H1- receptors antagonists: safety issues. Ann Allergy Asthma Immunol 1999; 83: 481 – 8. 98 Mann RD, Pearce GL, Dunn N, Shakir S. Sedation with 'non-sedating' antihistamines: four prescription-event studies in general practice. BMJ 2000; 320: 1184 – 7. 99 Ramaekers JG, Vermeeren A. All antihistamines cross blood–brain barrier. BMJ 2000; 321: 572. 100 Hindmarch I, Shamsi Z. Sedation and antihistamines: a review of inter-drug differences using proportional impairment ratios. Hum Psychopharmacol Clin Exp 2000; 15: S3 – 30. 101 O'Hanlon JF, Ramaekers JG. Antihistamine effects on actual driving performance in a standard test: a summary of Dutch experience, 1989–94. Allergy 1995; 50: 234 – 42. 102 Yanai K, Ryu JH, Watanabe T et al. 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: 1649 – 55. 103 Okamura N, Yanai K, Higuchi M et al. Functional neuroimaging of cognition impaired by a classical antihistamine, d-chlorpheniramine. Br J Pharmacol 2000; 129: 115 – 23. 104 Tagawa M, Kano M, Okamura N et al. Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and d-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol 2001; 52: 501 – 509. 105 Hill SJ, Ganellin CR, Timmerman H et al. International union of pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev 1997; 49: 253 – 78. 106 De Backer MD, Gommeren W, Moereels H et al. Genomic cloning, heterologous expression and pharmacological characterisation of a human histamine H1-receptor. Biochem Biophys Res Commun 1993; 197: 1601 – 1608. 107 Ter Laak AM, Tsai RS, Donné-Op den Kerlder GM, Carrupt PA, Testa B, Timmerman H. Lipophilicity and hydrogen-bonding capacity of H1-antihistaminic agents in relation to their central sedative side-effects. Eur J Pharm Sci 1994; 2: 373 – 84. 108 Yanai K, Son LZ, Endou M et al. Behavioural characterisation and amounts of brain monoamines and their metabolites in mice lacking histamine H1-receptors. Neuroscience 1998; 312: 479 – 87. 109 Quach T, Duchemin AM, Rose C, Schwartz JC. In vivo occupation of cerebral histamine H1-receptors evaluated with 3H-merypiramine may predict sedative properties of psychotropic drugs. Eur J Pharmacol 1979; 60: 391 – 2. 110 Morse KL, Behan J, Laz TM et al. Cloning and characterisation of a novel human histamine receptor. J Pharmacol Exp Ther 2001; 296: 1058 – 66. 111 Liu C, Ma XJ, Jiang X et al. Cloning and pharmacological characterisation of a fourth histamine receptor (H4) expressed in bone marrow. Mol Pharmacol 2001; 59: 420 – 6. 112 Ter Laak AM, Timmerman H, Leurs R, Nederkoorn PHJ, Smit MJ, Donné-Op den Kelder GM. Modelling and mutation studies on the histamine H1 receptor agonist binding site reveal different binding modes for H1-agonists: Asp116 (TM3) has a constitutive role in receptor stimulation. J Computer Aided Mol Design 1995; 9: 319 – 30. 113 Leurs R, Smit MJ, Meeder R, Ter Laak AM, Timmerman H. Lysine200 located in the fifth transmembrane domain of the histamine H1– receptor interacts with histamine but not with all H1-antagonists. Biochem Biophys Res Commun 1995; 214: 110 – 7. 114 Zhang MQ, Van de Stolpe A, Zuiderveld OP, Timmerman H. Synthesis and pharmacological evaluation of some amino – acid – containing cyproheptadine derivatives as dual antagonists of histamine H1– leukotriene D4– receptors. Eur J Med Chem 1997; 32: 95 – 102. 115 Alewijnse AE, Smit MJ, Hoffmann M, Verzijl D, Timmerman H, Leurs R. Constitutive activity and structural instability of the wild-type human H2 receptor. J Neurochem 1998; 71: 799 – 807. 116 Smit MJ, Leurs R, Alewijnse AE et al. Inverse agonism of histamine H2-antagonist accounts for upregulation of spontaneously active histamine H2-receptors. Proc Natl Acad Sci USA 1996; 93: 6802 – 7. Citing Literature Volume33, Issue9September 2003Pages 1305-1324 ReferencesRelatedInformation
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