The importance of 5-HT1A receptor agonism in antipsychotic drug action: Rationale and perspectives

Current Opinion in Investigational Drugs

Volumn 11, Issue 7, 2010, Pages 802-812

  Newman Tancredi, Adrian ^a  

^a NeuroAct Communication   (France)

Author keywords

5 HT1Areceptor; antipsychotic; aripiprazole; cariprazine; D2receptor; dopamine; lurasidone; perospirone; schizophrenia; serotonin

Indexed keywords

ARIPIPRAZOLE; BIFEPRUNOX; BUSPIRONE; CARIPRAZINE; CLOZAPINE; F 15063; F 97013; LURASIDONE; NEUROLEPTIC AGENT; PEROSPIRONE; PF 217830; SEROTONIN 1A RECEPTOR; TANDOSPIRONE; UNCLASSIFIED DRUG; ZIPRASIDONE; DOPAMINE 2 RECEPTOR; NEW DRUG;

ANXIETY DISORDER; CATALEPSY; COGNITION; DRUG STRUCTURE; FRONTAL CORTEX; NONHUMAN; REVIEW; AFFECT; ANIMAL; BIOLOGICAL MODEL; DRUG ANTAGONISM; DRUG DELIVERY SYSTEM; DRUG EFFECT; DRUG POTENTIATION; FRONTAL LOBE; HUMAN; METABOLISM; METHODOLOGY; PARTIAL AGONISM; SCHIZOPHRENIA;

AFFECT; ANIMALS; ANTIPSYCHOTIC AGENTS; CATALEPSY; COGNITION; DRUG DELIVERY SYSTEMS; DRUG PARTIAL AGONISM; DRUGS, INVESTIGATIONAL; FRONTAL LOBE; HUMANS; MODELS, BIOLOGICAL; RECEPTOR, SEROTONIN, 5-HT1A; RECEPTORS, DOPAMINE D2; SCHIZOPHRENIA;

EID: 77954122304     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (98)

1. Rössler W, Salize HJ, van Os J, Riecher-Rössler A: Size of burden of schizophrenia and psychotic disorders. Eur Neuropsychopharmacol (2005) 15(4):399-409.
2. Arnt J, Bang-Andersen B, Dias R, Bogesø KP: Strategies or pharmacotherapy of schizophrenia. Drugs Future (2008) 33(9):777-791.
3. Kapur S, Agid O, Mizrahi R, Li M: How antipsychotics work - From receptors to reality. NeuroRx (2006) 3(1):10-21.
4. 2-selective ex vivo but not in vitro. Neuropsychopharmacology (2010):doi:10.1038/npp.2010.50.
5. Meltzer HY, Li Z, Kaneda Y, Ichikawa J: Serotonin receptors: Their key role in drugs to treat schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry (2003) 27(7):1159-1172.
6. Goff DC, Shader RI: Non-neurological side-effects of antipsychotic drugs. In: Schizophrenia. Hirsch SR, Weinberger D (Eds), Blackwell Publishing, Oxford, UK (2003):573-588.
7. Meltzer HY, Huang M: In vivo actions of atypical antipsychotic drug on serotonergic and dopaminergic systems. In: Serotonin-Dopamine Interaction. Experimental, Clinical and Therapeutic Evidence (Progress in Brain Research). Di Giovanni G, Di Matteo V and Esposito E (Eds), Elsevier BV, Amsterdam, the Netherlands (2008) 172:177-198.
8. 1A receptor activation: A possible mechanism of atypical antipsychotic-induced cortical dopamine release. J Neurochem (2001) 76(5):1521-1531.
9. Ichikawa J, Meltzer HY: Relationship between dopaminergic and serotonergic neuronal activity in the frontal cortex and the action of typical and atypical antipsychotic drugs. Eur Arch Psychiatry Clin Neurosci (1999) 249(Suppl 4):90-98.
10. Lahti AC, Holcomb HH, Weiler MA, Medoff DR, Tamminga CA: Functional effects of antipsychotic drugs: Comparing clozapine with haloperidol. Biol Psychiatry (2003) 53(7):601-608.
11. Richtand NM, Welge JA, Logue AD, Keck PE, Strakowski SM, McNamara RK: Role of serotonin and dopamine receptor binding in antipsychotic efficacy. In: Serotonin-Dopamine Interaction. Experimental, Clinical and Therapeutic Evidence (Progress in Brain Research). Di Giovanni G, Di Matteo V and Esposito E (Eds), Elsevier BV, Amsterdam, the Netherlands (2008) 172:155-175.
12. Newman-Tancredi A, Cussac D, Depoortere R: Neuro-pharmacological profile of bifeprunox: Merits and limitations in comparison with other third generation antipsychotics. Curr Opin Investig Drugs (2007) 8(7):539-554.
13. Jones CA, McCreary AC: Serotonergic approaches in the development of novel antipsychotics. Neuropharmacology (2008) 55(6):1056-1065.
14. Broekkamp CL, Oosterloo SK, Berendsen HH, Van Delft AM: Effect of metergoline, fenfluramine, and 8-OHDPAT on catalepsy induced by haloperidol or morphine. Naunyn Schmiedebergs Arch Pharmacol (1988) 338(2):191-195.
15. Haleem DJ, Samad N, Haleem MA: Reversal of haloperidol-induced tardive vacuous chewing movements and supersensitive somatodendritic serotonergic response by buspirone in rats. Pharmacol Biochem Behav (2007) 87(1):115-121.
16. 1A agonistic anxiolytic agent, on haloperidol-induced catalepsy and forebrain Fos expression in mice. J Pharmacol Sci (2009) 109(4):593-599.
17. 1A receptor activation and anti-cataleptic effects: High-efficacy agonists maximally inhibit haloperidol-induced catalepsy. Eur J Pharmacol (2002) 453(2-3):217-221.
18. 1A agonist properties. Neuropsychopharmacology (2006) 31(9):1869-1879.
19. Christoffersen CL, Meltzer LT: Reversal of haloperidol-induced extrapyramidal side effects in cebus monkeys by 8-hydroxy-2-(di-n-propylamino) tetralin and its enantiomers. Neuropsychopharmacology (1998) 18(5):399-402.
20. 1A antipsychotics on catalepsy-associated behaviour in cynomolgus monkeys. Behav Brain Res (2009) 203(2):288-295.
21. Sovner R, Parnell-Sovner N: Use of buspirone in the treatment of schizophrenia. J Clin Psychopharmacol (1989) 9(1):61-62.
22. Goff DC, Midha KK, Brotman AW, McCormick S, Waites M, Amico ET: An open trial of buspirone added to neuroleptics in schizophrenic patients. J Clin Psychopharmacol (1991) 11(3): 193-197.
23. Moss LE, Neppe VM, Drevets WC: Buspirone in the treatment of tardive dyskinesia. J Clin Psychopharmacol (1993) 13(3):204-209.
24. Yoshida K, Sugita T, Higuchi H, Hishikawa Y: Effect of tandospirone on tardive dyskinesia and parkinsonian symptoms. Eur Psychiatry (1998) 13(8):421-422.
25. 1A receptors in human brain tissue. Eur J Pharmacol (1992) 221(2-3):397-398.
26. 1A receptors. Neuropharmacology (1996) 35(1):119-121.
27. 1A receptors: Affinity, efficacy and potential implications for treatment of schizophrenia. Int J Neuropsychopharmacol (2005) 8(3):341-356.
28. 2S receptors coupled to extracellular signalregulated kinase. Eur J Pharmacol (2006) 534(1-3):63-70.
29. Ase AR, Amdiss F, Hébert C, Huang N, van Gelder NM, Reader TA: Effects of antipsychotic drugs on dopamine and serotonin contents and metabolites, dopamine and serotonin transporters, and serotonin 1A receptors. J Neural Transm (1999) 106(1):75-105.
30. 1A receptors are not involved in clozapine's lack of cataleptogenic potential. Neuropharmacology (1996) 35(11):1645-1646.
31. 1A receptor activation. Eur J Pharmacol (1997) 338(2):R3-R5.
32. 1A receptor activation: A possible mechanism of atypical antipsychotic-induced cortical dopamine release. J Neurochem (2001) 76(5):1521-1531.
33. 1A receptors. Can J Physiol Pharmacol (2002) 80(12):1158-1166.
34. 1A agonists and the antipsychotics, clozapine, ziprasidone and S16924, but not haloperidol, to the discriminative stimuli elicited by PD128,907 and 7-OH-DPAT. Neuropharmacology (2001) 40(7):899-910.
35. Prus AJ, Philibin SD, Pehrson AL, Porter JH: Discriminative stimulus properties of the atypical antipsychotic drug clozapine in rats trained to discriminate 1.25 mg/kg clozapine vs 5.0 mg/kg clozapine vs vehicle. Behav Pharmacol (2006) 17(2):185-194.
36. 1A receptors. Eur J Pharmacol (1994) 260(1):79-83.
37. 1A agonist properties: II. Functional profile in comparison to clozapine and haloperidol. J Pharmacol Exp Ther (1998) 286(3):1356-1373. (Pubitemid 29135550)
38. 1A receptors by clozapine in the primate brain: A PET study. Psychopharmacology (Berl) (2003) 166(3):234-240.
39. 1A receptor in schizophrenia and during clozapine treatment. J Psychopharmacol (2004) 18(3):346-354.
40. 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia. Neurochem Int (1997) 30(6):565-574.
41. 11C]WAY-100635. Arch Gen Psychiatry (2002) 59(6): 514-520.
42. 11C]WAY 100635. Psychopharmacology (Berl) (2006) 189(2):155-164.
43. 1A receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry (2000) 48(3):229-237.
44. Yoshino T, Nisijima K, Shioda K, Yui K, Katoh S: Perospirone, a novel atypical antipsychotic drug, potentiates fluoxetine-induced increases in dopamine levels via multireceptor actions in the rat medial prefrontal cortex. Neurosci Lett (2004) 364(1):16-21.
45. Li Z, Ichikawa J, Dai J, Meltzer HY: Aripiprazole, a novel antipsychotic drug, preferentially increases dopamine release in the prefrontal cortex and hippocampus in rat brain. Eur J Pharmacol (2004) 493(1-3):75-83.
46. Assié MB, Ravailhe V, Faucillon V, Newman-Tancredi A: Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: Frontocortical dopamine and hippocampal serotonin release in rat brain. J Pharmacol Exp Ther (2005) 315(1):265-272
47. 1A receptors in the rat medial prefrontal and entorhinal cortices - Immunohistochemical studies. J Physiol Pharmacol (2008) 59(2):229-238.
48. 2A receptors. Int J Neuropsychopharmacol (2010):doi:10.1017/ S146114571000009X.
49. Akimova E, Lanzenberger R, Kasper S: The serotonin-1A receptor in anxiety disorders. Biol Psychiatry (2009) 66(7):627-635.
50. 2A receptors in depression. J Psychiatry Neurosci (2004) 29(4):252-265.
51. 1A agonist properties on PCP-induced social interaction deficits in the rat. Neuropharmacology (2005) 49(7):996-1006.
52. 1A receptors. Behav Brain Res (2008) 191(1):26-31.
53. 4 partial agonist properties. III. Activity in models of cognition and negative symptoms. Br J Pharmacol (2007) 151(2):266-277.
54. Bruins Slot LA, Bardin L, Auclair AL, Depoortere R, Newman-Tancredi A: Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol (2008) 19(2):145-152.
55. Dahan L, Husum H, Mnie-Filali O, Arnt J, Hertel P, Haddjeri N: Effects of bifeprunox and aripiprazole on rat serotonin and dopamine neuronal activity and anxiolytic behaviour. J Psychopharmacol (2009) 23(2):177-189.
56. 1A agonist improves glutamatergic-induced memory impairment and demonstrates anxiolytic- and antidepressant-like effects in rodents. Society for Neuroscience, Washington DC, USA (2008) 38:Abs 155.16.
57. 1A receptors improve cognition in schizophrenia? Behav Brain Res (2008) 195(1):98-102.
58. 1A receptors in learning and memory. Behav Brain Res (2008) 195(1):54-77.
59. 1A receptors. Psychopharmacology (Berl) (2009) 202(1-3):315-328.
60. 1A receptors. Eur Neuropsychopharmacol (2008) 18(6):448-454.
61. Ishiyama T, Tokuda K, Ishibashi T, Ito A, Toma S, Ohno Y: Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance test. Eur J Pharmacol (2007) 572(2-3):160-170.
62. Enomoto T, Ishibashi T, Tokuda K, Ishiyama T, Toma S, Ito A: Lurasidone reverses MK-801-induced impairment of learning and memory in the Morris water maze and radial-arm maze tests in rats. Behav Brain Res (2008) 186(2):197-207.
63. López-Gil X, Artigas F, Adell A: Role of different monoamine receptors controlling MK-801-induced release of serotonin and glutamate in the medial prefrontal cortex: Relevance for antipsychotic action. Int J Neuropsychopharmacol (2009) 12(4):487-499.
64. Schechter LE, Smith DL, Rosenzweig-Lipson S, Sukoff SJ, Dawson LA, Marquis K, Jones D, Piesla M, Andree T, Nawoschik S, Harder JA et al: Lecozotan (SRA-333): A selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. J Pharmacol Exp Ther (2005) 314(3):1274-1289.
65. Chamberlain SR, Muller U, Deakin JB, Corlett PR, Dowson J, Cardinal R, Aitken MR, Robbins TW, Sahakian BJ: Lack of deleterious effects of buspirone on cognition in healthy male volunteers. J Psychopharmacol (2007) 21(2):210-215.
66. Sumiyoshi T, Matsui M, Nohara S, Yamashita I, Kurachi M, Sumiyoshi C, Jayathilake K, Meltzer HY: Enhancement of cognitive performance in schizophrenia by addition of tandospirone to neuroleptic treatment. Am J Psychiatry (2001) 158(10):1722-1725.
67. Sumiyoshi T, Matsui M, Yamashita I, Nohara S, Kurachi M, Uehara T, Sumiyoshi S, Sumiyoshi C, Meltzer HY: The effect of tandospirone, a serotonin 1A agonist, on memory function in schizophrenia. Biol Psychiatry (2001) 49(10):861-868.
68. 1A receptor agonist. Hum Psychopharmacol (2009) 24(6):437-446.
69. Reynolds GP, Kirk SL: Metabolic side effects of antipsychotic drug treatment - Pharmacological mechanisms. Pharmacol Ther (2010) 125(1):169-179.
70. Kato T, Hirose A, Ohno Y, Shimizu H, Tanaka H, Nakamura M: Binding profile of SM-9018, a novel antipsychotic candidate. Jpn J Pharmacol (1990) 54(4):478-481.
71. 1A receptor activity. J Pharmacol Exp Ther (2010):doi:10.1124/ jpet.110.167346.
72. Lattanzi L, Dell'Osso L, Cassano P, Pini S, Rucci P, Houck PR, Gemignani A, Battistini G, Bassi A, Abelli M, Cassano GB: Pramipexole in treatment-resistant depression: A 16-week naturalistic study. Bipolar Disord (2002) 4(5):307-314.
73. 2 dopamine receptor antagonist-partial agonist antipsychotic candidate: In vitro and neurochemical profile. J Pharmacol Exp Ther (2010) 333(1):328-340.
74. Auclair AL, Cathala A, Sarrazin F, Depoortère R, Vincenzo Piazza P, Newman-Tancredi A, Spampinato U: The central serotonin(2B) receptor: A new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity. J Neurochem (2010):doi:10.1111/j.1471-4159.2010.06848.x
75. Graham JM, Coughenour LL, Barr BM, Rock DL, Nikam SS: 1-Aminoindanes as novel motif with potential atypical antipsychotic properties. Bioorg Med Chem Lett (2008) 18(2): 489-493.
76. 2A antagonist targeting the treatment of positive and negative symptoms of schizophrenia. Society for Neuroscience, Chicago, IL, USA (2009) 39:Abs 646.23.
77. 2A antagonist. Society for Neuroscience, Chicago, IL, USA (2009) 39:Abs 646.18.
78. 1A agonist with antipsychotic- and antiparkinsonian-like properties. Neuropharmacology (2006) 51(1):129-140.
79. Stoddard MA, Kounnas MZ, Mexal S, Elmeri KE, Senson KD, Fick DB, Pfadenhuer EH, Kumar A, Helton DR: Receptor binding profile of CM-2,395: A novel therapeutic for the treatment of schizophrenia. Society for Neuroscience, Chicago, IL, USA (2009) 39:Abs 645.14.
80. 1A receptor dual ligands. Bioorg Med Chem (2008) 16(18):8335-8338.
81. 1A receptors. Bioorg Med Chem (2010) 18(5):1925-1935.
82. 2 receptors disrupt basal PPI of the startle reflex in rats. Psychopharmacology (Berl) (2007) 193(1):45-54.
83. Khan A, Batool F, Haleem DJ: Behavioral effects of 8-OH-DPAT in single and repeated haloperidol injected rats. Pak J Pharm Sci (2001) 14(2):9-17.
84. Gogos A, Bogeski M, van den Buuse M: Role of serotonin-1A receptors in the action of antipsychotic drugs: Comparison of prepulse inhibition studies in mice and rats and relevance for human pharmacology. Behav Pharmacol (2008) 19(5-6): 548-561.
85. 1A receptor activation: New molecular and neuroadaptive mechanisms of pain relief. Curr Opin Investig Drugs (2006) 7(1):40-47.
86. Annual Report: Pierre Fabre SA, Paris, France (2004). www.pierre-fabre.com/file/1125311967437-rapport-2004-gb.pdf
87. Ferger B, Shimasaki M, Ceci A, Ittrich C, Allers KA, Sommer B: Flibanserin, a drug intended for treatment of hypoactive sexual desire disorder in pre-menopausal women, affects spontaneous motor activity and brain neurochemistry in female rats. Naunyn Schmiedebergs Arch Pharmacol (2010) 381(6):573-9
88. Boehringer Ingelheim Corp: Boehringer Ingelheim announces pivotal phase III data of fibanserin in pre-menopausal women with hypoactive sexual desire disorder. Press Release (2009): November 16.
89. Lawrence AJ: Optimisation of anti-psychotic therapeutics: A balancing act? Br J Pharmacol (2007) 151(2):161-162.
90. 1A autoreceptor levels determine vulnerability to stress and response to antidepressants. Neuron (2010) 65(1):40-52.
91. Le François B, Czesak M, Steubl D, Albert PR: Transcriptional regulation at a HTR1A polymorphism associated with mental illness. Neuropharmacology (2008) 55(6):977-985.
92. 1A receptor gene polymorphism on negative and depressive symptom response to antipsychotic treatment of drug-naïve psychotic patients. Am J Psychiatry (2006) 163(10):1826-1829.
93. 1A receptor gene is associated with negative symptom response to risperidone treatment in schizophrenia patients. J Psychopharmacol (2008) 22(8):904-909.
94. Mössner R, Schuhmacher A, Kühn KU, Cvetanovska G, Rujescu D, Zill P, Quednow BB, Rietschel M, Wölwer W, Gaebel W, Wagner M et al: Functional serotonin 1A receptor variant influences treatment response to atypical antipsychotics in schizophrenia. Pharmacogenet Genomics (2009) 19(1):91-94.
95. 1A receptor proteins in the prefrontal cortex of subjects with major depressive disorder. Int J Neuropsychopharmacol (2009) 12(2): 155-168.
96. 1A receptors. Br J Pharmacol (2010):doi:10.1111/j.1476-5381.2010.00738.x.
97. 1A receptor agonists. Eur Neuropsychopharmacol (2010):doi:10.1016/j. euroneuro.2010.04.005.
98. 1A receptor agonist: In-vivo profile in behavioural models of antidepressant and serotonergic activity. Int J Neuropsychopharmacol (2010) 11:1-14.