Serotonin (5-HT) transporter ligands affect plasma 5-HT in rats: Implications for medication development

Annals of the New York Academy of Sciences

Volumn 1139, Issue , 2008, Pages 268-284

  Rothman, Richard B ^a,c   Zolkowska, Dorota ^a,b   Baumann, Michael H ^a  

^a NATIONAL INSTITUTE ON DRUG ABUSE   (United States)

^b MEDICAL UNIVERSITY OF LUBLIN   (Poland)

^c NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

5 HT transporter; Amphetamine; Blood; Microdialysis; Plasma; Pulmonary hypertension; Serotonin (5 HT); Valvular heart disease

Indexed keywords

3,4 METHYLENEDIOXYMETHAMPHETAMINE; AMPHETAMINE; FENFLURAMINE; FLUOXETINE; METHAMPHETAMINE; PHENTERMINE; SEROTONIN; SEROTONIN TRANSPORTER;

ANIMAL EXPERIMENT; CONFERENCE PAPER; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABUSE; DRUG BLOOD LEVEL; DRUG DEPENDENCE; DRUG DEPENDENCE TREATMENT; EX VIVO STUDY; MALE; NONHUMAN; PULMONARY HYPERTENSION; SEROTONIN BLOOD LEVEL; VALVULAR HEART DISEASE;

RATTUS;

EID: 53549096261     PISSN: 00778923     EISSN: 17496632     Source Type: Book Series    
DOI: 10.1196/annals.1432.042     Document Type: Conference Paper

References (87)

1. Banken, J.A. 2004. Drug abuse trends among youth in the United States. Ann. N. Y. Acad. Sci. 1025 : 465 471.
2. Kresina, T.F. et al. 2004. Addressing the need for treatment paradigms for drug-abusing patients with multiple morbidities. Clin. Infect. Dis. 38 (Suppl 5 S398 S401.
3. Shearer, J. & L.R. Gowing. 2004. Pharmacotherapies for problematic psychostimulant use: a review of current research. Drug. Alcohol. Rev. 23 : 203 211.
4. Rothman, R.B., B.E. Blough & M.H. Baumann. 2002. Appetite suppressants as agonist substitution therapies for stimulant dependence. Ann. N. Y. Acad. Sci. 965 : 109 126.
5. Grabowski, J. et al. 2004. Agonist-like or antagonist-like treatment for cocaine dependence with methadone for heroin dependence: two double-blind randomized clinical trials. Neuropsychopharmacology 29 : 969 981.
6. Wojnicki, F.H.E. et al. 1999. Effects of phentermine on responding maintained under multiple fixed-ratio schedules of food-presentation and cocaine-delivery in the rhesus monkey. J. Pharmacol. Exp. Ther. 288 : 550 560.
7. Negus, S.S. & N.K. Mello. 2003. Effects of chronic d-amphetamine treatment on cocaine- and food-maintained responding under a progressive-ratio schedule in rhesus monkeys. Psychopharmacology (Berl.) 167 : 324 332.
8. Grabowski, J. et al. 2001. Dextroamphetamine for cocaine-dependence treatment: a double-blind randomized clinical trial. J. Clin. Psychopharmacol. 21 : 522 526.
9. Shearer, J. et al. 2003. Pilot randomized double blind placebo-controlled study of dexamphetamine for cocaine dependence. Addiction 98 : 1137 1141.
10. Wise, R.A. 1996. Neurobiology of addiction. Curr. Opin. Neurobiol. 6 : 243 251.
11. Rothman, R.B. & M.H. Baumann. 2000. Neurochemical mechanisms of phentermine and fenfluramine: therapeutic and adverse effects. Drug. Dev. Res. 51 : 52 65.
12. Woods, J.H. & R.E. Tessel. 1974. Fenfluramine: amphetamine congener that fails to maintain drug-taking behavior in the rhesus monkey. Science 185 : 1067 1069.
13. Bendotti, C. et al. 1980. Effect of fenfluramine and norfenfluramine stereoisomers on stimulant effects of d-amphetamine and apomorphine in the rat. Pharmacol. Res. Commun. 12 : 567 574.
14. Baumann, M.H. et al. 2000. Effects of phentermine and fenfluramine on extracellular dopamine and serotonin in rat nucleus accumbens: therapeutic implications. Synapse 36 : 102 113.
15. Rea, W.P., R.B. Rothman & T.S. Shippenberg. 1998. Evaluation of the conditioned reinforcing effects of phentermine and fenfluramine in the rat: concordance with clinical studies. Synapse 30 : 107 111.
16. Glatz, A.C. et al. 2002. Inhibition of cocaine self-administration by fluoxetine or D-fenfluramine combined with phentermine. Pharmacol. Biochem. Behav. 71 : 197 204.
17. Glowa, J.R. et al. 1997. Phentermine/fenfluramine decreases cocaine self-administration in rhesus monkeys. Neuroreport 8 : 1347 1351.
18. Walsh, S.L. & K.A. Cunningham. 1997. Serotonergic mechanisms involved in the discriminative stimulus, reinforcing and subjective effects of cocaine. Psychopharmacology (Berl.) 130 : 41 58.
19. Daw, N.D., S. Kakade & P. Dayan. 2002. Opponent interactions between serotonin and dopamine. Neural Netw. 15 : 603 616.
20. Burmeister, J.J. et al. 2004. Differential roles of 5-HT receptor subtypes in cue and cocaine reinstatement of cocaine-seeking behavior in rats. Neuropsychopharmacology 29 : 660 668.
21. Rothman, R.B. et al. 2005. Development of a rationally designed, low abuse potential, biogenic amine releaser that suppresses cocaine self-administration. J. Pharmacol. Exp. Ther. 313 : 1361 1369.
22. Wee, S. et al. 2005. Relationship between the serotonergic activity and reinforcing effects of a series of amphetamine analogs. J. Pharmacol. Exp. Ther. 313 : 848 854.
23. Rothman, R.B. & M. Baumann. 2002. Therapeutic and adverse actions of serotonin transporter substrates. Pharmacol. Ther. 95 : 73 88.
24. Rothman, R.B. & M.H. Baumann. 2006. Therapeutic potential of monoamine transporter substrates. Curr. Top Med. Chem. 6 : 1845 1859.
25. Roth, B.L. 2007. Drugs and valvular heart disease. N. Engl. J. Med. 356 : 6 9.
26. Setola, V. et al. 2003. 3,4-Methylenedioxymeth-amphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro. Mol. Pharmacol. 63 : 1223 1229.
27. Droogmans, S. et al. 2007. Possible association between 3,4-methylenedioxymethamphetamine abuse and valvular heart disease. Am. J. Cardiol. 100 : 442 445.
28. Rubin, L.J. 1997. Primary pulmonary hypertension. N. Engl. J. Med. 336 : 111 117.
29. Gurtner, H.P. 1990. Aminorex pulmonary hypertension. In The Pulmonary Circulation: Normal and Abnormal. A.P. Fishman, Ed 397 411. University of Pennsylvania Press. Philadelphia, PA.
30. Abenhaim, L. et al. 1996. Appetite-suppressant drugs and the risk of primary pulmonary hypertension. International primary pulmonary hypertension study group [see comments]. N. Engl. J. Med. 335 : 609 616.
31. Rich, S. et al. 2000. Anorexigens and pulmonary hypertension in the United States: results from the Surveillance of North American Pulmonary Hypertension. Chest 117 : 870 874.
32. Rothman, R.B. 2000. The age-adjusted mortality rate from primary pulmonary hypertension, in age range 20 to 54 years, did not increase during the years of peak "Phen/Fen" use. Chest 118 : 1516 1517.
33. Backmann, R. et al. 1972. Primary pulmonary hypertension: Report of the Commission of the German Society for Research on Blood Circulation. Verh. Dtsch. Ges. Kreislaufforsch. 38 : 134 141.
34. Schnabel, K.F. et al. 1976. Drug-induced primary vascular pulmonary hypertension. Med. Welt. 27 : 1300 1303.
35. Fishman, A.P. 1999. Aminorex to fen/phen: an epidemic foretold. Circulation 99 : 156 161.
36. MacLean, M.R. et al. 2000. 5-hydroxytryptamine and the pulmonary circulation: receptors, transporters and relevance to pulmonary arterial hypertension. Br. J. Pharmacol. 131 : 161 168.
37. Herve, P. et al. 1995. Increased plasma serotonin in primary pulmonary hypertension. Am. J. Med. 99 : 249 254.
38. Martin, F. & F. Artigas. 1992. Simultaneous effects of p-chloroamphetamine, d-fenfluramine, and reserpine on free and stored 5-hydroxytryptamine in brain and blood. J. Neurochem. 59 : 1138 1144.
39. Rothman, R.B. et al. 2000. Chronic treatment with the phentermine combined with fenfluramine lowers plasma serotonin. Am. J. Cardiol. 85 : 913 915.
40. Zolkowska, D., R.B. Rothman & M.H. Baumann. 2006. Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary disease. J. Pharmacol. Exp. Ther. 318 : 604 610.
41. Zolkowska, D., M.H. Baumann & R.B. Rothman. 2008. Chronic fenfluramine administration increases plasma serotonin (5-HT) to non-toxic levels. J. Pharmacol. Exp. Ther. 324 : 791 797.
42. Baumann, M.H. et al. 2001. 1-(m-Chlorophenyl)-piperazine (mCPP) dissociates in vivo serotonin release from long-term serotonin depletion in rat brain. Neuropsychopharmacology 24 : 492 501.
43. Lundmark, J., M. Reis & F. Bengtsson. 2001. Serum concentrations of fluoxetine in the clinical treatment setting. Ther. Drug Monit. 23 : 139 147.
44. Ni, W. & S.W. Watts. 2006. 5-hydroxytryptamine in the cardiovascular system: focus on the serotonin transporter (SERT). Clin. Exp. Pharmacol. Physiol. 33 : 575 583.
45. Cote, F. et al. 2004. Recent advances in understanding serotonin regulation of cardiovascular function. Trends Mol. Med. 10 : 232 238.
46. Celada, P., F. Martin & F. Artigas. 1994. Effects of chronic treatment with dexfenfluramine on serotonin in rat blood, brain and lung tissue. Life Sci. 55 : 1237 1243.
47. Lesch, K.P. et al. 1993. Primary structure of the human platelet serotonin uptake site: identity with the brain serotonin transporter. J. Neurochem. 60 : 2319 2322.
48. Buczko, W., G. De Gaetano & S. Garattini. 1975. Effect of some anorectic agents on the uptake and release of 5-hydroxytryptamine by blood platelets of rats. J. Pharm. Pharmacol. 27 : 366 368.
49. Schuldiner, S. et al. 1993. Amphetamine derivatives interact with both plasma membrane and secretory vesicle biogenic amine transporters. Mol. Pharmacol. 44 : 1227 1231.
50. Fanburg, B.L. & S.L. Lee. 1997. A new role for an old molecule: serotonin as a mitogen. Am. J. Physiol. 272 : L795 L806.
51. Cortijo, J. et al. 1997. Characterization of 5-HT receptors on human pulmonary artery and vein: functional and binding studies. Br. J. Pharmacol. 122 : 1455 1463.
52. Melega, W.P. et al. 2007. Methamphetamine blood concentrations in human abusers: application to pharmacokinetic modeling. Synapse 61 : 216 220.
53. Chin, K.M., R.N. Channick & L.J. Rubin. 2006. Is methamphetamine use associated with idiopathic pulmonary arterial hypertension? Chest 130 : 1657 1663.
54. Rothman, R.B. & M.H. Baumann. 2007. Methamphetamine and idiopathic pulmonary arterial hypertension: role of the serotonin transporter. Chest 132 : 1412 1413.
55. Rothman, R.B. et al. 1999. Aminorex, fenfluramine, and chlorphentermine are serotonin transporter substrates: implications for primary pulmonary hypertension. Circulation 100 : 869 875.
56. Eddahibi, S. et al. 1998. Effect of dexfenfluramine treatment in rats exposed to acute and chronic hypoxia. Am. J. Respir. Crit. Care. Med. 157 : 1111 1119.
57. Ortiz, J. & F. Artigas. 1992. Effects of monoamine uptake inhibitors on extracellular and platelet 5-hydroxytryptamine in rat blood: different effects of clomipramine and fluoxetine. Br. J. Pharmacol. 105 : 941 946.
58. Brammer, G.L. et al. 1991. Fenfluramine effects on serotonergic measures in vervet monkeys. Pharmacol. Biochem. Behav. 40 : 267 271.
59. Ho, H.H. et al. 1986. Blood serotonin concentrations and fenfluramine therapy in autistic children. J. Pediatr. 108 : 465 469.
60. Leventhal, B.L. et al. 1993. Clinical and neurochemical effects of fenfluramine in children with autism. J. Neuropsychiatry Clin. Neurosci. 5 : 307 315.
61. 3H-imipramine binding, 5-HT uptake and 5-HT content in major depressive disorder. J. Affect. Disord. 20 : 101 113.
62. Menys, V.C. et al. 1996. Platelet 5-hydroxytryptamine is decreased in a preliminary group of depressed patients receiving the 5-hydroxytryptamine re-uptake inhibiting drug fluoxetine. Clin. Sci. (Colch.) 91 : 87 92.
63. Tyrer, S.P., E.F. Marshall & H.W. Griffiths. 1990. The relationship between response to fluoxetine, plasma drug levels, imipramine binding to platelet membranes and whole-blood 5-HT. Prog. Neuropsychopharmacol. Biol. Psychiatry 14 : 797 805.
64. Alvarez, J.C. et al. 1999. Decreased platelet serotonin transporter sites and increased platelet inositol triphosphate levels in patients with unipolar depression: effects of clomipramine and fluoxetine. Clin. Pharmacol. Ther. 66 : 617 624.
65. Smith, B.M., W.J. Thomsen & A.J. Grottick. 2006. The potential use of selective 5-HT2C agonists in treating obesity. Expert Opin. Investig. Drugs. 15 : 257 266.
66. Eddahibi, S. et al. 2002. Is the serotonin transporter involved in the pathogenesis of pulmonary hypertension? J. Lab. Clin. Med. 139 : 194 201.
67. Robiolio, P.A. et al. 1995. Carcinoid heart disease: correlation of high serotonin levels with valvular abnormalities detected by cardiac catheterization and echocardiography. Circulation 92 : 790 795.
68. Gustafsson, B.I. et al. 2005. Long-term serotonin administration induces heart valve disease in rats. Circulation 111 : 1517 1522.
69. Kema, I.P. et al. 1992. Improved diagnosis of carcinoid tumors by measurement of platelet serotonin. Clin. Chem. 38 : 534 540.
70. Kema, I.P. et al. 2001. Profiling of tryptophan-related plasma indoles in patients with carcinoid tumors by automated, on-line, solid-phase extraction and HPLC with fluorescence detection. Clin. Chem. 47 : 1811 1820.
71. Meijer, W.G. et al. 2000. Discriminating capacity of indole markers in the diagnosis of carcinoid tumors. Clin. Chem. 46 : 1588 1596.
72. 2B receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation 102 : 2836 2841.
73. Eddahibi, S. et al. 2006. Cross talk between endothelial and smooth muscle cells in pulmonary hypertension: critical role for serotonin-induced smooth muscle hyperplasia. Circulation 113 : 1857 1864.
74. Marcos, E. et al. 2003. Serotonin transporter inhibitors protect against hypoxic pulmonary hypertension. Am. J. Respir. Crit. Care Med. 168 : 487 493.
75. Eddahibi, S. et al. 2001. Serotonin transporter overexpression is responsible for pulmonary artery smooth muscle hyperplasia in primary pulmonary hypertension. J. Clin. Invest. 108 : 1141 1150.
76. Pitt, B.R. et al. 1994. Serotonin increases DNA synthesis in rat proximal and distal pulmonary vascular smooth muscle cells in culture. Am. J. Physiol. 266 : L178 L186.
77. Eddahibi, S. et al. 1999. Induction of serotonin transporter by hypoxia in pulmonary vascular smooth muscle cells. Relationship with the mitogenic action of serotonin. Circ. Res. 84 : 329 336.
78. Artigas, F. et al. 1989. Increased plasma free serotonin but unchanged platelet serotonin in bipolar patients treated chronically with lithium. Psychopharmacology. (Berl.) 99 : 328 332.
79. Celada, P. et al. 1992. Effects of acute and chronic treatment with fluvoxamine on extracellular and platelet serotonin in the blood of major depressive patients:relationship to clinical improvement. J. Affect. Disord. 25 : 243 249.
80. Das, Y.T. et al. 2004. Safety of 5-hydroxy-L-tryptophan. Toxicol. Lett. 150 : 111 122.
81. Launay, J.M. et al. 2002. Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension. Nat. Med. 8 : 1129 1135.
82. Gurtner, H.P. 1985. Aminorex and pulmonary hypertension. Cor. Vasa. 27 : 160 171.
83. Gaine, S.P. et al. 2000. Recreational use of aminorex and pulmonary hypertension. Chest 118 : 1496 1497.
84. Eddahibi, S. et al. 2000. Attenuated hypoxic pulmonary hypertension in mice lacking the 5-hydroxytryptamine transporter gene. J. Clin. Invest. 105 : 1555 1562.
85. Guignabert, C. et al. 2005. Serotonin transporter inhibition prevents and reverses monocrotaline-induced pulmonary hypertension in rats. Circulation 111 : 2812 2819.
86. Kawut, S.M. et al. 2006. Selective serotonin reuptake inhibitor use and outcomes in pulmonary arterial hypertension. Pulm. Pharmacol. Ther. 19 : 370 374.
87. Lee, S.L., W.W. Wang & B.L. Fanburg. 2001. Dexfenfluramine as a mitogen signal via the formation of superoxide anion. FASEB J. 15 : 1324 1325.