Agents and Actions

, Volume 9, Issue 2, pp 133–140 | Cite as

FPL 55712 — An antagonist of slow reacting substance of anaphylaxis (SRS-A): A review

  • Naresh Chand
Histamine and Kinins Review

Abstract

Compound FPL 55712 is a highly selective antagonist of SRS-A derived from guinea-pig, rat, man and dog. It equally antagonizes SRS (slow reacting substance) released by calcium ionophore from rat basophilic leukemia cells and peritoneal mono-nuclear cells and by compound 48/80 from cat paw. In comparatively high doses FPL 55712 significantly inhibits passive cutaneous anaphylaxis in rat and anaphylactic bronchoconstriction in guinea-pig and rat and antigen-induced rhythmic mechanical activity in chicken ileum and late phase of Schultz-Dale reaction in guinea-pig trachea and human bronchus. In addition, FPL 55712 inhibits the SRS-A-induced release of rabbit aorta contracting substance (RCS) from guinea-pig lung. FPL 55712 facilitates sputum clearance in allergic canine asthma. This compound also inhibits the guinea-pig ECF-A (eosinophil chemotactic factor of anaphylaxis)-induced eosinophil chemotactic response of guinea-pig eosinophils in vitro. Compound FPL 55712 is an invaluable pharmacological tool for the identification of SRS(A) and to help define the role of SRS-A in the pathophysiology of immediate hypersensitivity (e.g. anaphylaxis and allergic asthma). Clinical trials of FPL 55712 as an aerosol in allergic obstructive respiratory diseases in man and animals may help to further understand the mechanism(s) and chemical mediator(s) involved in these conditions.

Keywords

Allergic Asthma Passive Cutaneous Anaphylaxis Human Bronchus Obstructive Respiratory Disease Eosinophil Chemotactic Factor 

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References

  1. [1]
    K.F. Austen andR.P. Orange,Bronchial Asthma: the possible Role of the Chemical Mediators of Immediate Hypersensitivity in the Pathogenesis of Subacute Chronic Disease, Am. Rev. Resp. Dis.112, 423–436 (1975).PubMedGoogle Scholar
  2. [2]
    R.P. Orange, R.C. Murphy andK.F. Austen,Inactivation of Slow Reacting Substance of Anaphylaxis (SRS-A) by Arylsulfatases, J. Immun.113, 316–322 (1974).PubMedGoogle Scholar
  3. [3]
    R.P. Orange, R.C. Murphy, M.L. Karnovsky andK.F. Austen,The Physiochemical Characteristics and Purification of Slow Reacting Substance of Anaphylaxis, J. Immun.110, 760–770 (1973).PubMedGoogle Scholar
  4. [4]
    P.J. Piper,Anaphylaxis and the Release of Active Substances in the Lungs, Pharmac. and Ther. B.3, 75–98 (1977).Google Scholar
  5. [5]
    W.E. Brocklehurst,The Release of Histamine and Formation of a Slow-Reacting Substance (SRS-A) during Anaphylactic Shock, J. Physiol.151, 416–435 (1960).PubMedGoogle Scholar
  6. [6]
    W.E. Brocklehurst,Slow Reacting Substance and Related Compounds, Progr. Allergy6, 539–558 (1962).Google Scholar
  7. [7]
    P. Sheard andA.M.J.N. Blair,Disodium Cromoglycate. Activity in Three In Vitro Models of the Immediate Hypersensitivity Reactions in Lung, Int. Arch. Allergy Appl. Immun.38, 217–224 (1970).Google Scholar
  8. [8]
    G.K. Adams andL.M. Lichtenstein,Antagonism of Antigen-Induced Contraction of Guinea-Pig and Human Airways, Nature270, 255–257 (1977).PubMedGoogle Scholar
  9. [9]
    J.F. Burka andP. Eyre,The Immunological Release of Slow Reacting Substance of Anaphylaxis from Bovine Lung, Can. J. Physiol. Pharmac.52, 1201–1203 (1974).Google Scholar
  10. [10]
    P.A. Berry andH.O.J. Collier,Bronchoconstrictor Action and Antagonism of a Slow-Reacting Substances from Anaphylaxis of Guinea-Pig Isolated Lung, Br. J. Pharmac. Chemother.23, 201–216 (1964).Google Scholar
  11. [11]
    A.A. Mathé, A. Åstrom andN.A. Persson,Some Bronchoconstricting and Bronchodilating Responses of Human Isolated Bronchi. Evidence for the Existence of α-Adrenoceptors, J. Pharm. Pharmac.23, 905–910 (1971).Google Scholar
  12. [12]
    A.A. Mathé andK. Strandberg,Antagonism of Slow Reacting Substancy by Polyphloretin Phosphate on Isolated Human Bronchi, Acta Physiol. Scand.82, 460–465 (1971).PubMedGoogle Scholar
  13. [13]
    A.A. Mathé, K. Strandberg andA. Åstrom,Blockade by Polyphloretin Phosphate of the Prostaglandin F Action on Isolated Human Bronchi, Nat. New Biol.230, 215–216 (1971).PubMedGoogle Scholar
  14. [14]
    N. Chand andP. Eyre,Histamine Relaxes Constricted Trachea and Bronchi of Horse. Vet. Sci. Comm.1, 85–90 (1977).Google Scholar
  15. [15]
    N. Chand andP. Eyre,Spasmolytic Action of Histamine in Airway Smooth Muscle of Horse, Agents and Actions8, 191–198 (1978).PubMedGoogle Scholar
  16. [16]
    N. Chand andP. Eyre,Autacoid and Anaphylactic Reactivity of Pulmonary and Hepatic Smooth Musculature of the Cat, Eur. J. Pharmac.45, 213–220 (1977).Google Scholar
  17. [17]
    J.F. Burka andP. Eyre,Effects of Bovine SRS-A (SRS-A bov) on Bovine Respiratory Tract and Lung Vasculature In Vitro, Eur. J. Pharmac.44, 169–178 (1977).Google Scholar
  18. [18]
    R.D. Krell andL.W. Chakrin,The Effect of Metiamide in In Vitro and In Vivo Canine Models of Type I Hypersensitivity Reactions, Eur. J. Pharmac.44, 35–44 (1977).Google Scholar
  19. [19]
    R.D. Krell andL.W. Chakrin,Pharmacologic Regulation of Antigen-Induced Mediator Release from Canine Lung, Int. Arch. Allergy Appl. Immun.56, 39–47 (1978).Google Scholar
  20. [20]
    R.D. Krell,Investigation of the Role of Histamine-Induced Bronchoconstriction in the Ascaris-Hypersensitive Dogs, Br. J. Pharmac.62, 519–528 (1978).Google Scholar
  21. [21]
    K.M. Lulich, H.W. Michell andM.P. Sparrow,The Cat Lung Strip as an In Vitro Preparation of Peripheral Airways: a Comparison of β-Adrenoceptor Agonists, Autacoids and Anaphylactic Challenge of the Lungs Strip and Trachea, Br. J. Pharmac.58, 71–79 (1976).Google Scholar
  22. [22]
    A.B. Kay, J. Stechschulte andK.F. Austen,An Eosinophil Leucocyte Chemotactic Factor of Anaphylaxis, J. Exp. Med.133, 602–618 (1971).PubMedGoogle Scholar
  23. [23]
    P.R. Mann andC.N.D. Cruickshank,An Eosinophilotactic Factor Derived from Rat Mast Cells, J. Path.115, 91–96 (1975).PubMedGoogle Scholar
  24. [24]
    S.I. Wasserman, D. Whitmer, E.J. Goetzl andK.F. Austen,Chemotactic Deactivation of Human Eosinophils by the Eosinophil Chemotactic Factor of Anaphylaxis, Proc. Soc. Exp. Biol. Med.148, 301–306 (1975).PubMedGoogle Scholar
  25. [25]
    S.I. Wasserman, E.J. Goetzl andK.F. Austen,Inactivation of Slow Reacting Substance of Anaphylaxis by Human Eosinophil Arylsulfatase, J. Immun.114, 645–649 (1975).PubMedGoogle Scholar
  26. [26]
    J. Augstein, J.B. Farmer, T.B. Lee, P. Sheard andM.L. Tattersall,Selective Inhibitor of Slow-Reacting Substance of Anaphylaxis, Nature New Biol.245, 215–217 (1973).PubMedGoogle Scholar
  27. [27]
    D.G. Jones andA.B. Kay,Inhibition of Eosinophil Chemotaxis by the Antagonist of Slow Reacting Substance of Anaphylaxis-Compound FPL 55712, J. Pharm. Pharmac.26, 917–918 (1974).Google Scholar
  28. [28]
    P. Sheard, T.B. Lee andM.L. Tattersall,Further Studies on the SRS-A Antagonist FPL 55712, Monogr. Allergy12, 245–249 (1977).PubMedGoogle Scholar
  29. [29]
    D.M. Engineer, U. Niederhauser, P.J. Piper andP. Sirois,Release of Mediators of Anaphylaxis: Inhibition of Prostaglandin Synthesis and the Modification of Release of Slow Reacting Substance of Anaphylaxis and Histamine, Br. J. Pharmac.62, 61–66 (1978).Google Scholar
  30. [30]
    B.A. Jakschik, A. Kulczycki, H.H. McDonnald andC.W. Parker,Release of Slow Reacting Substance (SRS) from Rat Basophilic Leukemia (RBL-1) Cells, J. Immun.119, 618–622 (1977).PubMedGoogle Scholar
  31. [31]
    M.K. Bach, J.R. Brashler andR.R. Gorman,Structure of Slow Reacting Substance of Anaphylaxis — Evidence of Biosynthesis from Arachidonic Acid, Prostaglandins14, 21–28 (1977).PubMedGoogle Scholar
  32. [32]
    J.F. Burka andP. Eyre,A Pharmacological Study of SRS-A on the Bovine Cutaneous Vasculature, Can. J. Physiol. Pharmac.55, 904–908 (1977).Google Scholar
  33. [33]
    N. Chand andP. Eyre,Pharmacology of Anaphylaxis in Chicken Intestine, Br. J. Pharmac.57, 399–408 (1976).Google Scholar
  34. [34]
    N. Chand,A Pharmacological Study of Anaphylaxis in Domestic Fowl, Ph.D. Thesis, University of Guelph (1977).Google Scholar
  35. [35]
    J.B. Farmer, I.M. Richards, P. Sheard andA.M. Woods,Mediators of Passive Lung Anaphylaxis in the Rat, Br. J. Pharmac.55, 57–64 (1975).Google Scholar
  36. [36]
    D.M. Engineer, P.J. Piper andP. Sirois,Release of Prostaglandins and Rabbit Aorta Contracting Substance (RCS) from Guinea-Pig Lung by Slow Reacting Substance of Anaphylaxis (SRS-A), Br. J. Pharmac.59, 444p (1977).Google Scholar
  37. [37]
    A. Wanner, S. Zarzecki, J. Hirsch andS. Epstein,Tracheal Mucous Transport in Experimental Canine Asthma, J. Appl. Physiol.39, 950–957 (1975).PubMedGoogle Scholar
  38. [38]
    R. Liebig, W. Bernauer andB.A. Peskar,Prostaglandin, Slow-Reacting Substance, and Histamine Release from Anaphylactic Guinea-Pig Hearts, and its Pharmacological Modification, Naunyn-Schmiedeberg's Arch. Pharmac.289, 65–76 (1975).Google Scholar
  39. [39]
    A.A. Mathé, K. Strandberg andS.S. Yen,Prostaglandin Release by Slow Reacting Substance from Guinea-Pig and Human Lung Tissue, Prostaglandins14, 1105–1115 (1977).PubMedGoogle Scholar
  40. [40]
    K. Pavek,Anaphylactic Shock in the Monkey: Its Hemodynamics and Mediators, Acta Anaesth. Scand.21, 293–307 (1977).PubMedGoogle Scholar
  41. [41]
    L.S. Dunlop andA.P. Smith,Reduction of Antigen-Induced Contraction of Sensitized Human Bronchus In Vitro by Indomethacin, Br. J. Pharmac.54, 495–497 (1975).Google Scholar
  42. [42]
    L.S. Dunlop andThe Effect of Histamine Antagonists on Antigen-Induced Contractions of Sensitized Human Bronchus In Vitro, Br. J. Pharmac.59, 475p (1977).Google Scholar
  43. [43]
    N. Chand andP. Eyre,The Schultz-Dale Reaction. A Review, Agents and Actions8, 171–184 (1978).PubMedGoogle Scholar
  44. [44]
    E.F. Grower,Studies in Anaphylaxis in the Rabbit. IV. On the Simonds Explanation of the Different Pathology of Acute Anaphylactic Shock in Different Animal Species. V. On the Role of Unstripped Muscle in Acute Anaphylaxis in the Rabbit, J. Immun.23, 147–152 (1932).Google Scholar
  45. [45]
    N. Chand andP. Eyre,A Pharmacological Study of Chicken Airway Smooth Muscle, J. Pharm. Pharmac.30, 432–435 (1978).Google Scholar
  46. [46]
    H.W. Mitchell andM.P. Sparrow,The Effect of Catecholamines on the In Vivo and In Vitro Responses of the Cat Lung During Anaphylaxis, Br. J. Pharmac.61, 533–540 (1977).Google Scholar
  47. [47]
    J.C. Castillo andE.J. DeBeer,The Tracheal Chain, I. A. Preparation for the Study of Antispasmodics with Special Reference to Bronchodilator Drugs. J. Pharmac. Exp. Ther.90, 104–109 (1947).Google Scholar
  48. [48]
    R. Patterson, T. Miyamoto, L. Reynolds andJ. Pruzansky,Comparative Studies of Two Models of Allergic Respiratory Disease, Int. Arch. Allergy Appl Immun.32, 31–45 (1967).Google Scholar
  49. [49]
    P.D. Joiner, M. Wall, L.B. Davis andF. Hahn,Role of Amines in Anaphylactic Contraction of Guinea-Pig Isolated Smooth Muscle, J. Allergy Clin. Immun.53, 261–270 (1974).PubMedGoogle Scholar
  50. [50]
    L.A. Antonissen, R.W. Mitchell, E.A. Koeger andN.L. Sephens,Airway Smooth Muscle Pharmacology in a Canine Asthmatic Model, Fed. Proc.37, 639 (1978).Google Scholar
  51. [51]
    L. Sörenby,Inhibition of Antigen-Induced Tone in Isolated Trachea, Eur. J. Pharmac.31, 374–376 (1975).Google Scholar
  52. [52]
    R. Santa Cruz, J. Linda, J. Hirsch andM.A. Sackner,Tracheal Mucous Velocity in Normal Mar and Patients with Obstructive Lung Disease: Effects of Terbutaline, Am. Rev. Resp. Dis.109, 458–463 (1974).PubMedGoogle Scholar
  53. [53]
    M.S. Dunnill,The Pathology of Asthma with Special Reference to Changes in the Bronchial Mucosa, J. Clin. Path.13, 27–33 (1960).PubMedGoogle Scholar
  54. [54]
    B.M. Zussman,Surveillance of Ambulatory Asthmatics by Means of Total Circulating Eosinophil Count, Annals Allergy40, 195–199 (1978).Google Scholar
  55. [55]
    A.A. Glynn andM. Michaels,Bronchial Biopsy in Chronic Bronchitis and Asthma, Thorax15, 142–153 (1960).Google Scholar

Copyright information

© Birkhäuser-Verlag 1979

Authors and Affiliations

  • Naresh Chand
    • 1
  1. 1.Département d'Anatomie et de Physiologie Animales, Faculté de Médecine VétérinaireUniversité de MontréalSaint-HyacintheCanada

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