Serotonin autoreceptor function and antidepressant drug action

Journal of Psychopharmacology

Volumn 14, Issue 2, 2000, Pages 177-185

  Hjorth, Stephan ^a   Bengtsson, H J ^a   Kullberg, A ^a   Carlzon, D ^a   Peilot, H ^a   Auerbach, S B ^b  

^a UNIVERSITY OF GOTHENBURG   (Sweden)

^b RUTGERS UNIVERSITY   (United States)

Author keywords

5 HT; 5 HT(1A); 5 HT(1B); Antidepressants; Autoreceptors; CNS; Microdialysis; Rat

Indexed keywords

2 DIPROPYLAMINO 5 FLUORO 8 HYDROXYTETRALIN; 2 DIPROPYLAMINO 8 HYDROXYTETRALIN; 2,3,6,7 TETRAHYDRO 1' METHYL 5 [[2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL) 4 BIPHENYLYL]CARBONYL]SPIRO[FURO[2,3 F]INDOLE 3,4' PIPERIDINE]; 5 METHOXY 3 (1,2,3,6 TETRAHYDRO 4 PYRIDYL) 1H INDOLE; ALNESPIRONE; ANTIDEPRESSANT AGENT; AUTORECEPTOR; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; CITALOPRAM; FLUOXETINE; IPSAPIRONE; METITEPINE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL)[1,1' BIPHENYL] 4 CARBOXAMIDE; NAS 181; PENBUTOLOL; PINDOLOL; SEROTONIN; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN 1B ANTAGONIST; SEROTONIN 1B RECEPTOR; SEROTONIN UPTAKE INHIBITOR; TERTATOLOL; UNCLASSIFIED DRUG;

CONTROLLED STUDY; DENDRITE; DRUG SELECTIVITY; FEEDBACK SYSTEM; HIPPOCAMPUS; LONG TERM EXPOSURE; MICRODIALYSIS; NERVE ENDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN LOCALIZATION; RAPHE NUCLEUS; RAT; RECEPTOR DOWN REGULATION; REVIEW;

EID: 0034123688     PISSN: 02698811     EISSN: None     Source Type: Journal    
DOI: 10.1177/026988110001400208     Document Type: Review

References (100)

1. Adell A, Artigas F (1991) Differential effects of clomipramine given locally or systemically on extracellular 5-hydroxytryptamine in raphe nuclei and frontal cortex - an in vivo brain microdialysis study. Naunyn-Schmiedeberg's Arch Pharmacol 343: 237-244
2. Aghajanian G K, Sprouse J S, Rasmussen K (1987) Physiology of midbrain serotonin systems. In Meltzer H Y (ed.). Psychopharmacology: the third generation of progress, Raven Press, New York, pp. 141-149
3. 1A receptor antagonist (S)-UH-301 augments the increase in extracellular concentrations of 5-HT in the frontal cortex produced by both acute and chronic treatment with citalopram. Naunyn-Schmiedeberg's Arch Pharmacol 353: 630-640
4. Artigas F (1993) 5-HT and antidepressants - new views from microdialysis studies. Trends Pharmacol Sci 14: 262
5. Artigas F, Perez V, Alvarez E (1994) Pindolol induces a rapid improvement of depressed patients treated with serotonin reuptake inhibitors. Arch Gen Psychiatry 51: 248-251
6. 1B receptors. Neuropharmacology 35: 213-222
7. Auerbach S B, Hjorth S (1995) Effect of chronic administration of the selective serotonin (5-HT) uptake inhibitor citalopram on extracellular 5-HT and apparent autoreceptor sensitivity in rat forebrain in vivo. Naunyn-Schmiedeberg's Arch Pharmacol 352: 597-606
8. Auerbach S B, Lundberg J F, Hjorth S (1995) Differential inhibition of serotonin release by 5-HT and NA reuptake blockers after systemic administration. Neuropharmacology 34: 89-96
9. B/D autoreceptors. Synapse 31: 13-19
10. Bel N, Artigas F (1993) Chronic treatment with fluvoxamine increases extracellular serotonin in frontal cortex but not in raphe nuclei. Synapse 15: 243-245
11. 1A autoreceptor antagonist WAY100635 on the 5-HT-elevating response to the SSRI citalopram in vivo. Nordic J Psychiatry 51: 101
12. Berman R M, Darnell A M, Miller H L, Anand A, Charney D S (1997) Effect of pindolol in hastening response to fluoxetine in the treatment of major depression: a double-blind, placebo-controlled trial. Am J Psychiatry 154: 37-43
13. Berman R M, Anand A, Cappiello A, Miller H L, Hu X S, Oren D A, Charney D S (1999) The use of pindolol with fluoxetine in the treatment of major depression: final results from a double-blind, placebo-controlled trial. Biol Psychiatry 45: 1170-1177
14. Blier P, Bergeron R (1995) Effectiveness of pindolol with selected antidepressant drugs in the treatment of major depression. J Clin Psychopharmacol 15: 217-222
15. Blier P, de Montigny C, Chaput Y (1987) Modifications of the serotonin system by antidepressant treatments: implications for the therapeutic response in major depression. J Clin Psychopharmacol 7: 24S-35S
16. 1 receptor agonists and p-chloroamphetamine. Synapse 5: 120-133
17. Bordet R, Thomas P, Dupuis B (1998) Effect of pindolol on onset of action of paroxetine in the treatment of major depression: Intermediate analysis of a double-blind, placebo-controlled trial. Am J Psychiatry 155: 1346-1351
18. Bosker F J, Donker M G, Klompmakers A A, Kurata K, Westenberg H G (1994) 5-Hydroxytryptamine release in dorsal hippocampus of freely moving rats: modulation by pindolol. Prog Neuropsychopharmacol Biol Psychiatry 18: 765-778
19. Bosker F J, Klompmakers A A, Westenberg H G (1995a) Effects of single and repeated oral administration of fluvoxamine on extracellular serotonin in the median raphe nucleus and dorsal hippocampus of the rat. Neuropharmacology 34: 501-508
20. 1B receptors, as measured by in vivo microdialysis in dorsal hippocampus of conscious rats. Psychopharmacology 117: 358-363
21. 1A receptors mediate 5-hydroxytryptamine release in the amygdala through a feedback to the caudal linear raphe. Eur J Pharmacol 333: 147-157
22. Cadieux R J (1998) Practical management of treatment-resistant depression. Am Family Physician 58: 2059-2062
23. Carlsson A, Lindqvist M (1978) Effects of antidepressant agents on the synthesis of brain monoamines. J Neural Transm 43: 73-91
24. Casanovas J M, Artigas F (1996) Differential effects of ipsapirone on 5-hydroxytryptamine release in the dorsal and median raphe neuronal pathways. J Neurochem 67: 1945-1952
25. 1A agonists alnespirone (S-20499) and 8-OH-DPAT on extracellular 5-hydroxytryptamine in different regions of rat brain. Br J Pharmacol 122: 733-741
26. Ceci A, Baschirotto A, Borsini F (1994) The inhibitory effect of 8-OH-DPAT on the firing activity of dorsal raphe serotoninergic neurons in rats is attenuated by lesion of the frontal cortex. Neuropharmacology 33: 709-713
27. 1A autoreceptor in vivo. Br J Pharmacol 124: 206-212
28. 1A agonists. Synapse 14: 297-304
29. 1A receptor antagonists on fluoxetine induced changes in extracellular serotonin concentrations in rat frontal cortex. Eur J Pharmacol 345: 41-46
30. A receptors. Neurochem Res 21: 557-562
31. Fornal C A, Martin F J, Mendlin A, Metzler C W, Bjorvatn B, Jacobs B L (1999) Pindolol increases extracellular 5-HT while inhibiting serotonergic neuronal activity. Eur J Pharmacol 377: 187-191
32. 1A receptor antagonist and an SSRI in vivo: effects on 5-HT cell firing and extracellular 5-HT. Br J Pharmacol 115: 1064-1070
33. Gartside S E, Clifford E M, Cowen P J, Sharp T (1999) Effects of (-)-tertatolol (-)-penbutolol and (±)-pindolol in combination with paroxetine on presynaptic 5-HT function: an in vivo microdialysis and electrophysiological study. Br J Pharmacol 127: 145-152
34. 1B receptor inverse agonist 1′-methyl-5[[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4′- piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem 41: 1218-1235
35. 1B receptors with WAY 100 635 and GR 127 935. J Neurochem 68: 1159-1163
36. Gundlah C, Hjorth S, Auerbach S B (1997) Autoreceptor antagonists enhance the effect of the reuptake inhibitor citalopram on extracellular 5-HT: this effect persists after repeated citalopram treatment. Neuropharmacology 36: 475-482
37. Gur E, Dremencov E, Lerer B, Newman M E (1999) Venlafaxine: acute and chronic effects on 5-hydroxytryptamine levels in rat brain in vivo. Eur J Pharmacol 372: 17-24
38. Hajos M, Gartside S E, Sharp T (1995) Inhibition of median and dorsal raphe neurones following administration of the selective serotonin reuptake inhibitor paroxetine. Naunyn-Schmiedeberg's Arch Pharmacol 351: 624-629
39. 1A receptor-induced inhibition of 5-HT neuronal activity in the rat. Br J Pharmacol 126: 1741-1750
40. 1A receptors. In Baumgarten H G, Gothert M (eds), Handbook of experimental pharmacology, serotoninergic neurons and 5-HT receptors in the CNS. Springer-Verlag, Berlin, Germany, pp. 239-268
41. Hensler J G, Kovachich G B, Frazer A (1991) A quantitative autoradiographic study of serotonin-1A receptor regulation - effect of 5,7-dihydroxytryptamine and antidepressant treatments. Neuropsychopharmacology 4: 131-144
42. Hervas I, Artigas F (1998) Effect of fluoxetine on extracellular 5-hydroxytryptamine in rat brain. Role of 5-HT autoreceptors. Eur J Pharmacol 358: 9-18
43. Hervas I, Bel N, Fernandez A G, Palacios J M, Artigas F (1998) In vivo control of 5-hydroxytryptamine release by terminal autoreceptors in rat brain areas differentially innervated by the dorsal and median raphe nuclei. Naunyn-Schmiedeberg's Arch Pharmacol 358: 315-322
44. Hillegaart V (1991) Functional topography of brain serotonergic pathways in the rat. Acta Physiol Scand 142 (Suppl 598): 1-54
45. Hjorth S (1992) Functional differences between ascending 5-HT systems. In S L Handley, S J Cooper, B J Key, N M Barnes and J H Coote (eds) Advances in the biosciences, vol. 85: Serotonin, CNS receptors and brain function. Pergamon Press, New York, pp. 203-218
46. 1A autoreceptor blockade potentiates the ability of the 5-HT reuptake inhibitor citalopram to increase nerve terminal output of 5-HT in vivo - a microdialysis study. J Neurochem 60: 776-779
47. Hjorth S (1996) (-)-Pindolol, but not buspirone, potentiates the citalopram-induced rise in extracellular 5-HT. Eur J Pharmacol 303: 183-186
48. 1B receptor antagonist NAS-181. Soc Neurosci Abstr 24: 1109
49. 1A autoreceptors in the action of selective serotonin reuptake inhibitors. Eur J Pharmacol 260: 251-255
50. 1A autoreceptor desensitization following chronic citalopram treatment, as determined by in vivo microdialysis. Neuropharmacology 33: 331-334
51. Hjorth S, Auerbach S B (1999) Autoreceptors remain functional after prolonged treatment with a serotonin reuptake inhibitor. Brain Res 835: 224-228
52. 1A (auto)receptor-mediated decrease in 5-HT release in the rat brain in vivo. Presented at the 4th IUPHAR Satellite Meeting on Serotonin, Rotterdam, The Netherlands, 23-25 July 1998, p. 143
53. Hjorth S, Carlsson A (1985) (-)-Pindolol stereospecifically inhibits rat brain serotonin (5-HT) synthesis. Neuropharmacology 24: 1143-1146
54. Hjorth S, Carlsson A (1986) Is pindolol a mixed agonist antagonist at central serotonin (5-HT) receptors? Eur J Pharmacol 129: 131-138
55. 1A agonist 8-OH-DPAT preferentially activates cell body 5-HT autoreceptors in rat brain in vivo. Naunyn-Schmiedeberg's Arch Pharmacol 338: 463-471
56. 1B autoreceptor blocking properties of the beta-adrenoceptor antagonist (-)penbutolol. J Pharmacol Exp Ther 265: 707-712
57. 1B receptor agonist CP-93129 suppresses rat hippocampal 5-HT release in vivo: comparison with RU 24969. Eur J Pharmacol 209: 249-252
58. 1A receptors or beta-adrenoceptors, restrain the citalopram-induced increase in extracellular 5-hydroxytryptamine in vivo. Eur J Pharmacol 316: 43-47
59. 1A (auto)receptor blocker versus that of the 5-HT reuptake inhibitor. Neuropharmacology 36: 461-465
60. 1B receptor antagonist NAS-181 on rat brain 5-HT release: basic characteristics and regional differences. Nordic J Psychiatry 53: 110
61. Invernizzi R, Belli S, Samanin R (1992) Citalopram's ability to increase the extracellular concentrations of serotonin in the dorsal raphe prevents the drug's effect in the frontal cortex. Brain Res 584: 322-324
62. 1A receptors. Eur J Pharmacol 260: 243-246
63. Invernizzi R, Bramante M, Samanin R (1995) Extracellular concentrations of serotonin in the dorsal hippocampus after acute and chronic treatment with citalopram. Brain Res 696: 62-66
64. 1A receptors in the effects of acute and chronic fluoxetine on extracellular serotonin in the frontal cortex. Pharmacol Biochem Behav 54: 143-147
65. 1A receptor antagonists on citalopram-induced increase in extracellular serotonin in the frontal cortex, striatum and dorsal hippocampus. Neuropharmacology 36: 467-473
66. 1A receptors in rats treated chronically with a novel antidepressant, cericlamine. J Pharmacol Exp Ther 268: 1432-1443
67. Kreiss D S, Lucki I (1995) Effects of acute and repeated administration of antidepressant drugs on extracellular levels of 5-hydroxytryptamine measured in vivo. J Pharmacol Exp Ther 274: 866-876
68. 1A autoreceptors in rats treated with fluoxetine or paroxetine. Naunyn-Schmiedeberg's Arch Pharmacol 352: 141-148
69. Levine E S, Jacobs B L (1992) Neurochemical afferents controlling the activity of serotonergic neurons in the dorsal raphe nucleus - microiontophoretic studies in the awake cat. J Neurosci 12: 4037-4044
70. Maes M, Libbrecht I, van Hunsel F, Campens D, Meltzer H Y (1999) Pindolol and mianserin augment the antidepressant activity of fluoxetine in hospitalized major depressed patients, including those with treatment resistance. J Clin Psychopharm 19: 177-182
71. Malagié I, Trillat A C, Douvier E, Anmella M C, Dessalles M C, Jacquot C, Gardier A M (1996) Regional differences in the effect of the combined treatment of WAY 100635 and fluoxetine: an in vivo microdialysis study. Naunyn-Schmiedeberg's Arch Pharmacol 354: 1-6
72. Mamounas L A, Mullen C A, O'Hearn E, Molliver M E (1991) Dual serotoninergic projections to forebrain in the rat: morphologically distinct 5-HT axon terminals exhibit differential vulnerability to neurotoxic amphetamine derivatives. J Comp Neurol 314: 558-586
73. McQuade R, Sharp T (1997) Functional mapping of dorsal and median raphe 5-hydroxytryptamine pathways in forebrain of the rat using microdialysis. J Neurochem 69: 791-796
74. 1B receptors. Ann NY Acad Sci 600: 132-147
75. Millan M J, Lejeune F, Gobert A (1999) Reciprocal autoreceptor and heteroreceptor control of serotonergic, dopaminergic and adrenergic transmission in frontal cortex: a review, and relevance to the actions of antidepressant agents. J Psychopharmacol, in press
76. Molliver M E (1987) Serotonergic neuronal systems: what their anatomic organization tells us about function. J Clin Psychopharmacol 7 (Suppl): 3S-23S
77. Moret C, Briley M (1996) Effects of acute and repeated administration of citalopram on extracellular levels of serotonin in rat brain. Eur J Pharmacol 295: 189-197
78. 1B/D receptor antagonists. Gen Pharmacol 29: 293-303
79. Peilot H, Bengtsson H J, Hjorth S (1998) Regional differences in autoreceptor control of 5-HT release in the rat CNS in vivo? Nordic J Psychiatry 52: 128
80. Perez V, Gilaberte I, Faries D, Alvarez E, Artigas F (1997) Randomised, double-blind, placebo-controlled trial of pindolol in combination with fluoxetine antidepressant treatment. Lancet 349: 1594-1597
81. Rasanen P, Hakko H, Tiihonen J (1999)Mitchell B. Balter Award - 1998. Pindolol and major affective disorders: a three-year follow-up study of 30 485 patients. J Clin Psychopharmacol 19: 297-302
82. 1B/(1D) receptor antagonists in dorsal and median raphe innervated brain regions. Eur J Pharmacol 346: 175-180
83. 1A receptor antagonists in the dorsal raphe pathway: role of somatodendritic autoreceptors. J Neurochem 68: 2593-2603
84. 1A receptors: in vivo microdialysis and electrophysiological studies in the rat brain. Neuropsychopharmacology 15: 349-360
85. 1A antagonist WAY100635 selectively potentiates the presynaptic effects of serotonergic antidepressants in rat brain. Neurosci Lett 219: 123-126
86. Romero L, Casanovas J M, Hervas I, Cortes R, Artigas F (1997) Strategies to optimize the antidepressant action of selective serotonin reuptake inhibitors. In Skolnick P (ed), Antidepressants: new pharmacological strategies. Humana Press Inc, Totowa, NJ, pp. 1-33
87. Rutter J J, Gundlah C, Auerbach S B (1994) Increase in extracellular serotonin produced by uptake inhibitors is enhanced after chronic treatment with fluoxetine. Neurosci Lett 171: 183-186
88. Rutter J J, Gundlah C, Auerbach S B (1995) Systemic uptake inhibition decreases serotonin release via somatodendritic autoreceptor activation. Synapse 20: 225-233
89. 1B receptor antagonist with negative intrinsic activity. Br J Pharmacol 125: 202-208
90. 1A receptor antagonist on 5-hydroxytryptamine cell firing and release. Eur J Pharmacol 320: 15-19
91. 1B receptor antagonists on extracellular 5-HT in rat frontal cortex in vivo. Br J Pharmacol 121: 941-946
92. 1 receptor. Eur J Pharmacol 157: 173-181
93. 1B agonists: a comparative study with dorsal raphe neurons. Neuropharmacology 27: 707-715
94. Thase M E, Rush A J (1995) Treatment-resistant depression. In Bloom F E, Kupfer D J (eds), Psychopharmacology: the fourth generation of progress. Raven Press, New York, pp. 1081-1097
95. Tome M B, Isaac M T, Harte R, Holland C (1997) Paroxetine and pindolol: a randomized trial of serotonergic autoreceptor blockade in the reduction of antidepressant latency. Int Clin Psychopharmacol 12: 81-89
96. Vinar O, Vinarova E, Horacek J (1996) Pindolol accelerates the therapeutic action of selective serotonin reuptake inhibitors (SSRI) in depression. Homeostasis Health Dis 37: 93-95
97. 1 receptor subtypes in the rat brain. Naunyn-Schmiedeberg's Arch Pharmacol 337: 609-620
98. 1Dbeta receptors. Eur J Pharmacol 314: 365-372
99. 1A receptors negatively coupled to adenylyl cyclase activity in rat hippocampal membranes. Mol Pharmacol 41: 1066-1072
100. Zanardi R, Artigas F, Franchini L, Sforzini L, Gasperini M, Smeraldi E, Perez J (1997) How long should pindolol be associated with paroxetine to improve the antidepressant response? J Clin Psychopharmacol 17: 446-450