The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function

PLoS ONE

Volumn 9, Issue 1, 2014, Pages

  Lin, Olivia A ^a   Karim, Zubair A ^a   Vemana, Hari Priya ^a   Espinosa, Enma V P ^a   Khasawneh, Fadi T ^a  

^a WESTERN UNIVERSITY OF HEALTH SCIENCES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE DIPHOSPHATE; CALCIUM; CLOPIDOGREL; CYPROHEPTADINE; FIBRINOGEN RECEPTOR; PADGEM PROTEIN; PHOSPHATIDYLSERINE; PIZOTIFEN; PRUVANSERIN; SEROTONIN; ANTIDEPRESSANT AGENT; ANTITHROMBOCYTIC AGENT; DRUG DERIVATIVE; INDOLE DERIVATIVE; PIPERAZINE DERIVATIVE; SEROTONIN 2A RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; TICLOPIDINE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BLEEDING TIME; CALCIUM CELL LEVEL; CAROTID ARTERY THROMBOSIS; CONTROLLED STUDY; EX VIVO STUDY; FLOW CYTOMETRY; HUMAN; HUMAN CELL; IN VIVO STUDY; MOUSE; NONHUMAN; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; THROMBOCYTE AGGREGATION; THROMBOCYTE FUNCTION; ANIMAL; BLEEDING; BLOOD CLOTTING PARAMETERS; C57BL MOUSE; CHEMISTRY; DRUG EFFECT; IMMUNOPRECIPITATION; MALE; METABOLISM; PATHOLOGY; PHYSIOLOGY; THROMBOCYTE ACTIVATION; WESTERN BLOTTING;

ADENOSINE DIPHOSPHATE; ANIMALS; ANTIDEPRESSIVE AGENTS; BLOTTING, WESTERN; CALCIUM; CAROTID ARTERY THROMBOSIS; CYPROHEPTADINE; FLOW CYTOMETRY; HEMORRHAGE; HUMANS; IMMUNOPRECIPITATION; INDOLES; MALE; MICE; MICE, INBRED C57BL; PIPERAZINES; PIZOTYLINE; PLATELET ACTIVATION; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; PLATELET FUNCTION TESTS; RECEPTOR, SEROTONIN, 5-HT2A; SEROTONIN; SEROTONIN ANTAGONISTS; SEROTONIN RECEPTOR AGONISTS; TICLOPIDINE;

EID: 84899875224     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0087026     Document Type: Article

References (50)

1. Bembenek JP, Karlinski M, Kobayashi A, Czlonkowska A (2012) Deep venous thrombosis in acute stroke patients. Clin Appl Thromb Hemost 18: 258-264.
2. Ergelen M, Gorgulu S, Uyarel H, Norgaz T, Aksu H, et al. (2010) The outcome of primary percutaneous coronary intervention for stent thrombosis causing STelevation myocardial infarction. Am Heart J 159: 672-676.
3. Breet NJ, Sluman MA, van Berkel MA, van Werkum JW, Bouman HJ, et al. (2011) Effect of gender difference on platelet reactivity. Neth Heart J 19: 451-457.
4. Dowal L, Flaumenhaft R (2010) Targeting platelet G-protein coupled receptors (GPCRs): looking beyond conventional GPCR antagonism. Current vascular pharmacology 8: 140-154.
5. Moerland M, Kemme M, Dijkmans A, Bergougnan L, Burggraaf J (2011) Modulation of Vasoactivity and Platelet Aggregation by Selective 5-HT Receptor Antagonism in Humans. Journal of Cardiovascular Pharmacology 58: 575-580 510.1097/FJC.1090b1013e31822f31826b31828d.
6. Fanburg BL, Lee SL (1997) A new role for an old molecule: serotonin as a mitogen. Am J Physiol 272: L795-806.
7. Vanhoutte PM (1991) Platelet-derived serotonin, the endothelium, and cardiovascular disease. J Cardiovasc Pharmacol 17 Suppl 5: S6-12.
8. 2A receptor antagonist. European journal of pharmacology 586: 234-243.
9. Bampalis V, Dwivedi S, Shai E, Brandl R, Varon D, et al. (2011) Effect of 5-HT2A receptor antagonists on human platelet activation in blood exposed to physiologic stimuli and atherosclerotic plaque. Journal of Thrombosis and Haemostasis 9: 2112-2115.
10. Walsh M-T, Dinan TG, Condren RM, Ryan M, Kenny D (2002) Depression is associated with an increase in the expression of the platelet adhesion receptor glycoprotein Ib. Life Sciences 70: 3155-3165. (Pubitemid 34463092)
11. Kinugawa T, Fujita M, Lee JD, Nakajima H, Hanada H, et al. (2002) Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris. Am Heart J 144: E1.
12. Watanabe T, Koba S (2012) Roles of serotonin in atherothrombosis and related diseases. Traditional and novel risk factors in atherothrombosis InTech.
13. Raote I, Bhattacharya A, Panicker MM (2007) Serotonin 2A (5-HT2A) receptor function: ligand-dependent mechanisms and pathways. Serotonin receptors in neurobiology CRC, Boca Raton: 105-132.
14. Adams JW, Ramirez J, Shi Y, Thomsen W, Frazer J, et al. (2009) APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl) benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology. J Pharmacol Exp Ther 331: 96-103.
15. Nagatomo T, Rashid M, Abul Muntasir H, Komiyama T (2004) Functions of 5- HT2A receptor and its antagonists in the cardiovascular system. Pharmacology & Therapeutics 104: 59-81. (Pubitemid 39410563)
16. Przyklenk K, Frelinger A, Linden MD, Whittaker P, Li Y, et al. (2010) Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis. Journal of Thrombosis and Haemostasis 8: 331-340.
17. Schins A, Honig A, Crijns H, Baur L, Hamulyák K (2003) Increased coronary events in depressed cardiovascular patients: 5-HT2A receptor as missing link? Psychosomatic medicine 65: 729-737. (Pubitemid 37163376)
18. Eckert A, Gaan H, Riemann D, Aldenhoff J, Müller WE (1993) Elevated intracellular calcium levels after 5-HT2 receptor stimulation in platelets of depressed patients. Biological psychiatry 34: 565-568. (Pubitemid 23338515)
19. Konopka LM, Cooper R, Crayton JW (1996) Serotonin-induced increases in platelet cytosolic calcium concentration in depressed, schizophrenic, and substance abuse patients. Biological psychiatry 39: 708-713. (Pubitemid 26157606)
20. Delisi SM, Konopka LM, O'Connor FL, Crayton JW (1998) Platelet Cytosolic Calcium Responses to Serotonin in Depressed Patients and Controls: Relationship to Symptomatology and Medication. Biological psychiatry 43: 327-334. (Pubitemid 28137624)
21. Mendelson SD (2000) The current status of the platelet 5-HT2A receptor in depression. Journal of Affective Disorders 57: 13-24.
22. Laddha GP, Vidyasagar G, Bavaskar SR, Baile SB, Suralkar SS (2012) Serotonin: A Dive of Pleasure and Misery. Der Pharmacia Lettre 4: 443-455.
23. Vikenes K, Farstad M, Nordrehaug JE (1999) Serotonin is associated with coronary artery disease and cardiac events. Circulation 100: 483-489. (Pubitemid 29360156)
24. Ferreiro JL, Angiolillo DJ (2012) New directions in antiplatelet therapy. Circ Cardiovasc Interv 5: 433-445.
25. Miiller-Schweinitzer E (1986) Pizotifen, an anti-migraine drug with venocon-strictor activity in vivo. Journal of Cardiovascular Pharmacology 8: 805-810.
26. Van Zwieten P, Blauw G, Van Brummelen P (1990) Pathophysiological and pharmacotherapeutic aspects of serotonin and serotonergic drugs. Clinical physiology and biochemistry 8: 1.
27. Basaveswara Rao MV, Nagendrakumar AVD, Maiti S, Chandrasekhar N (2012) A Validated RP-HPLC Method for the Estimation of Pizotifen in Pharmaceutical Dosage Form. Chromatography Research International 2012: 5.
28. Mamo D, Sedman E, Tillner J, Sellers EM, Romach MK, et al. (2004) EMD 281014, a specific and potent 5HT2 antagonist in humans: a dose-finding PET study. Psychopharmacology (Berl) 175: 382-388. (Pubitemid 39361927)
29. 2A receptors by agonists and antagonists. Brain research bulletin 56: 441-451.
30. Cenajek D, Chodera A, Godlewski J, Wójciak Z (1980) Investigations on the interaction between cyproheptadine and amphetamine. Acta physiologica Polonica 31: 561.
31. Shad KF, Saeed SA (2007) The metabolism of serotonin in neuronal cells in culture and platelets. Experimental Brain Research 183: 411-416.
32. Morán A, Velasco C, Salvador T, Martin M, Román LS (1994) Inhibitory 5-hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats. British journal of pharmacology 113: 1358-1362.
33. Droogmans S, Roosens B, Cosyns B, Degaillier C, Hernot S, et al. (2009) Cyproheptadine prevents pergolide-induced valvulopathy in rats: an echocardiographic and histopathological study. American Journal of Physiology-Heart and Circulatory Physiology 296: H1940-H1948.
34. Zendehdel M, Taati M, Amoozad M, Hamidi F (2012) Antinociceptive effect of the aqueous extract obtained from Foeniculum vulgare in mice: the role of histamine H1 and H2 receptors. Iranian Journal of Veterinary research 13: 100-106.
35. Watemberg NM, Roth KS, Alehan FK, Epstein CE (1999) Central anticholinergic syndrome on therapeutic doses of cyproheptadine. Pediatrics 103: 158-160. (Pubitemid 29281945)
36. Hucker H, Hutt J (1983) Determination of cyproheptadine in plasma and urine by GLC with a nitrogen-sensitive detector. Journal of pharmaceutical sciences 72: 1069-1070. (Pubitemid 13003529)
37. Hargrove V, Molina DK (2009) A Fatality Due to Cyproheptadine and Citalopram. Journal of Analytical Toxicology 33: 564-567.
38. Nascimento EB Jr, Seniuk JGT, Godin AM, Ferreira WC, Dutra MB, et al. (2011) Peripheral 5-HT1B and 5-HT2A receptors mediate the nociceptive response induced by 5-hydroxytryptamine in mice. Pharmacology Biochemistry and Behavior 99: 598-603.
39. Glusa E, Markwardt F (1984) Inhibition of 5-hydroxytryptamine-potentiated aggregation of human blood platelets by 5-hydroxytryptamine receptor-blocking agents. Biomedica biochimica acta 43: 215.
40. Xiong Y, Teegarden BR, Choi J-SK, Strah-Pleynet S, Decaire M, et al. (2010) Discovery and Structure - Activity Relationship of 3-Methoxy-N-(3-(1- methyl-1 H-pyrazol-5-yl)-4-(2-morpholinoethoxy) phenyl) benzamide (APD791): A Highly Selective 5-Hydroxytryptamine2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis. Journal of medicinal chemistry 53: 4412-4421.
41. Saeed SA, Rasheed H, Gilani A (2003) Synergism interaction between arachidonic acid by 5-hydroxytryptamine in human platelet aggregation is mediated through multiple signalling pathways. Acta Pharmacologica Sinica 24: 958-964. (Pubitemid 37237952)
42. Berry CN, Lorrain J, Lochot S, Delahaye M, Lalé A, et al. (2001) Antiplatelet and antithrombotic activity of SL65. 0472, a mixed 5-HT1B/5-HT2A receptor antagonist. Thrombosis and haemostasis 85: 521.
43. Nishihira K, Yamashita A, Tanaka N, Kawamoto R, Imamura T, et al. (2006) Inhibition of 5-hydroxytryptamine2A receptor prevents occlusive thrombus formation on neointima of the rabbit femoral artery. Journal of Thrombosis and Haemostasis 4: 247-255.
44. Willerson JT, Eidt JF, McNatt J, Yao SK, Golino P, et al. (1991) Role of thromboxane and serotonin as mediators in the development of spontaneous alterations in coronary blood flow and neointimal proliferation in canine models with chronic coronary artery stenoses and endothelial injury. J Am Coll Cardiol 17: 101B-110B.
45. Kroeze WK, Kristiansen K, Roth BL (2002) Molecular biology of serotonin receptors structure and function at the molecular level. Curr Top Med Chem 2: 507-528.
46. Curial M, Nath E, Lang E (2013) Novel Antiplatelet Agent Use for Acute Coronary Syndrome in the Emergency Department: A Review. Cardiology Research and Practice 2013: 8.
47. Duerschmied D, Ahrens I, Mauler M, Brandt C, Weidner S, et al. (2012) Serotonin Antagonism Improves Platelet Inhibition in Clopidogrel Low-Responders after Coronary Stent Placement: An In Vitro Pilot Study. PloS one 7: e32656.
48. Karim ZA, Zhang J, Banerjee M, Chicka MC, Al Hawas R, et al. (2013) IkappaB kinase phosphorylation of SNAP-23 controls platelet secretion. Blood 121: 4567-4574.
49. Grynkiewicz G, Poenie M, Tsien RY (1985) A new generation of Ca2+ indicators with greatly improved fluorescence properties. J Biol Chem 260: 3440-3450. (Pubitemid 15114340)
50. 2 receptor exhibits antithrombotic properties in vivo. Biochemical and Biophysical Research Communications 421: 456-461.