- About this Journal ·
- Abstracting and Indexing ·
- Aims and Scope ·
- Article Processing Charges ·
- Articles in Press ·
- Author Guidelines ·
- Bibliographic Information ·
- Citations to this Journal ·
- Contact Information ·
- Editorial Board ·
- Editorial Workflow ·
- Free eTOC Alerts ·
- Publication Ethics ·
- Reviewers Acknowledgment ·
- Submit a Manuscript ·
- Subscription Information ·
- Table of Contents
Advances in Pharmacological Sciences
Volume 2012 (2012), Article ID 312041, 9 pages
Assessment of 5-HT7 Receptor Agonists Selectivity Using Nociceptive and Thermoregulation Tests in Knockout versus Wild-Type Mice
1Department of Pharmacology, Drug Discovery and Preclinical Development, ESTEVE, Avenida Mare de Déu de Montserrat 221, 08041 Barcelona, Spain
2UMR 894 INSERM-CPN/UPMC, Faculté de Médecine Pierre et Marie Curie, Site Pitié-Salpêtrière, 91 boulevard de l'Hôpital, 75634 Paris Cedex 13, France
Received 17 February 2012; Accepted 27 April 2012
Academic Editor: Karim A. Alkadhi
Copyright © 2012 Alex Brenchat et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
- P. B. Hedlund, “The 5-HT7 receptor and disorders of the nervous system: an overview,” Psychopharmacology, vol. 206, no. 3, pp. 345–354, 2009.
- M. Leopoldo, E. Lacivita, F. Berardi, R. Perrone, and P. B. Hedlund, “Serotonin 5-HT7 receptor agents: structure-activity relationships and potential therapeutic applications in central nervous system disorders,” Pharmacology and Therapeutics, vol. 129, no. 2, pp. 120–148, 2011.
- D. J. Cushing, J. M. Zgombick, D. L. Nelson, and M. L. Cohen, “LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery,” Journal of Pharmacology and Experimental Therapeutics, vol. 277, no. 3, pp. 1560–1566, 1996.
- I. T. Forbes, S. Dabbs, D. M. Duckworth et al., “(R)-3,N-Dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1- yl)propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist,” Journal of Medicinal Chemistry, vol. 41, no. 5, pp. 655–657, 1998.
- C. Kikuchi, H. Nagaso, T. Hiranuma, and M. Koyama, “Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor,” Journal of Medicinal Chemistry, vol. 42, no. 4, pp. 533–535, 1999.
- P. J. Lovell, S. M. Bromidge, S. Dabbs et al., “A novel, potent, and selective 5-HT7 antagonist: (R)-3-(2-(2-(4- methylpiperidin-1-yl)- ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970),” Journal of Medicinal Chemistry, vol. 43, no. 3, pp. 342–345, 2000.
- I. T. Forbes, S. Douglas, A. D. Gribble et al., “SB-656104-A: a novel 5-HT7 receptor antagonist with improved in vivo properties,” Bioorganic and Medicinal Chemistry Letters, vol. 12, no. 22, pp. 3341–3344, 2002.
- A. M. Johansson, M. Brisander, A. Sanin, S. Rosqvist, N. Mohell, A. Malmberg, et al., “5-Aryl substituted (S)-2-(dimethylamino)-tetralins: novel serotonin 5-HT7 receptor ligands,” in Proceedings of the 226th American Chemical Society National Meeting, New York, NY, USA, 2003.
- A. Sanin, M. Brisander, S. Rosqvist, N. Mohell, A. Malberg, A. Johansson, et al., “5-Aryl substituted (S)-2-(dimethylamino)-tetralins novel serotonin 5HT7 receptor ligands,” in Proceedings of the 14th Camerino-Noord Symposium, Ongoing Progress in the Receptor Chemistry, Camerino, Italy, 2003.
- C. G. Thomson, M. S. Beer, N. R. Curtis, H. J. Diggle, E. Handford, and J. J. Kulagowski, “Thiazoles and thiopyridines: novel series of high affinity h5HT7 ligands,” Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 3, pp. 677–680, 2004.
- M. Leopoldo, F. Berardi, N. A. Colabufo et al., “Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine 7 receptor agents,” Journal of Medicinal Chemistry, vol. 47, no. 26, pp. 6616–6624, 2004.
- M. Leopoldo, E. Lacivita, P. De Giorgio et al., “Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1- piperazinehexanamides: Influence on lipophilicity and 5-HT7 receptor activity. Part III,” Journal of Medicinal Chemistry, vol. 51, no. 18, pp. 5813–5822, 2008.
- A. Brenchat, L. Romero, M. García et al., “5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice,” Pain, vol. 141, no. 3, pp. 239–247, 2009.
- A. Brenchat, X. Nadal, L. Romero et al., “Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity,” Pain, vol. 149, no. 3, pp. 483–494, 2010.
- M. Leopoldo, E. Lacivita, M. Contino, N. A. Colabufo, F. Berardi, and R. Perrone, “Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1- yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents,” Journal of Medicinal Chemistry, vol. 50, no. 17, pp. 4214–4221, 2007.
- P. B. Hedlund, M. Leopoldo, S. Caccia et al., “LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor,” Neuroscience Letters, vol. 481, no. 1, pp. 12–16, 2010.
- A. Brenchat, D. Zamanillo, M. Hamon, L. Romero, J. M. Vela, et al., “Role of peripheral versus spinal 5-HT7 receptors in the modulation of pain under sensitizing conditions,” European Journal of Pain, vol. 16, no. 1, pp. 72–81, 2012.
- M. I. Diaz-Reval, R. Ventura-Martinez, M. Deciga-Campos, J. A. Terron, F. Cabre, F. J. Lopez-Munoz, et al., “Evidence for a central mechanism of action of S-(+)-ketoprofen,” European Journal of Pharmacology, vol. 483, no. 2–3, pp. 241–248, 2004.
- S. Doly, J. Fischer, M. J. Brisorgueil, D. Vergé, and M. Conrath, “Pre- and postsynaptic localization of the 5-HT7 receptor in rat dorsal spinal cord: immunocytochemical evidence,” Journal of Comparative Neurology, vol. 490, no. 3, pp. 256–269, 2005.
- S. E. Harte, R. G. Kender, and G. S. Borszcz, “Activation of 5-H and 5-HT7 receptors in the parafascicular nucleus suppresses the affective reaction of rats to noxious stimulation,” Pain, vol. 113, no. 3, pp. 405–415, 2005.
- T. Meuser, C. Pietruck, A. Gabriel, G. X. Xie, K. J. Lim, and P. Pierce Palmer, “5-HT7 receptors are involved in mediating 5-HT-induced activation of rat primary afferent neurons,” Life Sciences, vol. 71, no. 19, pp. 2279–2289, 2002.
- J. F. Neumaier, T. J. Sexton, J. Yracheta, A. M. Diaz, and M. Brownfield, “Localization of 5-HT7 receptors in rat brain by immunocytochemistry, in situ hybridization, and agonist stimulated cFos expression,” Journal of Chemical Neuroanatomy, vol. 21, no. 1, pp. 63–73, 2001.
- H. I. Rocha-González, A. Meneses, S. M. Carlton, and V. Granados-Soto, “Pronociceptive role of peripheral and spinal 5-HT7 receptors in the formalin test,” Pain, vol. 117, no. 1-2, pp. 182–192, 2005.
- M. R. Guscott, E. Egan, G. P. Cook et al., “The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor,” Neuropharmacology, vol. 44, no. 8, pp. 1031–1037, 2003.
- M. Guscott, L. J. Bristow, K. Hadingham et al., “Genetic knockout and pharmacological blockade studies of the 5-HT7 receptor suggest therapeutic potential in depression,” Neuropharmacology, vol. 48, no. 4, pp. 492–502, 2005.
- J. J. Hagan, G. W. Price, P. Jeffrey et al., “Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist,” British Journal of Pharmacology, vol. 130, no. 3, pp. 539–548, 2000.
- P. B. Hedlund, P. E. Danielson, E. A. Thomas, K. Slanina, M. J. Carson, and J. G. Sutcliffe, “No hypothermic response to serotonin in 5-HT7 receptor knockout mice,” Proceedings of the National Academy of Sciences of the United States of America, vol. 100, no. 3, pp. 1375–1380, 2003.
- P. B. Hedlund, L. Kelly, C. Mazur, T. Lovenberg, J. G. Sutcliffe, and P. Bonaventure, “8-OH-DPAT acts on both 5-H and 5-HT7 receptors to induce hypothermia in rodents,” European Journal of Pharmacology, vol. 487, no. 1–3, pp. 125–132, 2004.
- M. Zimmermann, “Ethical guidelines for investigations of experimental pain in conscious animals,” Pain, vol. 16, no. 2, pp. 109–110, 1983.
- F. E. D’Amour, D. L. Smith, et al., “A method for determining loss of pain sensation,” Journal of Pharmacology and Experimental Therapeutics, vol. 72, no. 1, pp. 74–79, 1941.
- K. Ramabadran, M. Bansinath, H. Turndorf, and M. M. Puig, “Tail immersion test for the evaluation of a nociceptive reaction in mice. Methodological considerations,” Journal of Pharmacological Methods, vol. 21, no. 1, pp. 21–31, 1989.
- G. Woolfe, A. D. MacDonald, et al., “The evaluation of the analgesic action of pethidine hydrochloride (Demerol),” Journal of Pharmacology and Experimental Therapeutics, vol. 80, no. 3, pp. 300–307, 1944.
- S. Hunskaar and K. Hole, “The formalin test in mice: dissociation between inflammatory and non-inflammatory pain,” Pain, vol. 30, no. 1, pp. 103–114, 1987.
- R. Galici, J. D. Boggs, K. L. Miller, P. Bonaventure, and J. R. Atack, “Effects of SB-269970, a 5-HT7 receptor antagonist, in mouse models predictive of antipsychotic-like activity,” Behavioural Pharmacology, vol. 19, no. 2, pp. 153–159, 2008.
- P. B. Hedlund, S. Huitron-Resendiz, S. J. Henriksen, and J. G. Sutcliffe, “5-HT7 receptor inhibition and inactivation induce antidepressantlike behavior and sleep pattern,” Biological Psychiatry, vol. 58, no. 10, pp. 831–837, 2005.
- J. Liu, T. Akay, P. B. Hedlund, K. G. Pearson, and L. M. Jordan, “Spinal 5-HT7 receptors are critical for alternating activity during locomotion: In vitro neonatal and in vivo adult studies using 5-HT7 receptor knockout mice,” Journal of Neurophysiology, vol. 102, no. 1, pp. 337–348, 2009.
- J. Shelton, P. Bonaventure, X. Li, S. Yun, T. Lovenberg, and C. Dugovic, “5-HT7 receptor deletion enhances REM sleep suppression induced by selective serotonin reuptake inhibitors, but not by direct stimulation of 5-H receptor,” Neuropharmacology, vol. 56, pp. 448–454, 2009.
- A. J. Roberts, T. Krucker, C. L. Levy, K. A. Slanina, J. G. Sutcliffe, and P. B. Hedlund, “Mice lacking 5-HT7 receptors show specific impairments in contextual learning,” European Journal of Neuroscience, vol. 19, no. 7, pp. 1913–1922, 2004.
- G. Sarkisyan and P. B. Hedlund, “The 5-HT7 receptor is involved in allocentric spatial memory information processing,” Behavioural Brain Research, vol. 202, no. 1, pp. 26–31, 2009.
- S. Semenova, M. A. Geyer, J. G. Sutcliffe, A. Markou, and P. B. Hedlund, “Inactivation of the 5-HT7 receptor partially blocks phencyclidine-induced disruption of prepulse inhibition,” Biological Psychiatry, vol. 63, no. 1, pp. 98–105, 2008.
- T. J. Coderre and R. Melzack, “The contribution of excitatory amino acids to central sensitization and persistent nociception after formalin-induced tissue injury,” Journal of Neuroscience, vol. 12, no. 9, pp. 3665–3670, 1992.
- A. Tjølsen, O. G. Berge, S. Hunskaar, J. H. Rosland, and K. Hole, “The formalin test: an evaluation of the method,” Pain, vol. 51, no. 1, pp. 5–17, 1992.
- K. Vissers, V. Hoffmann, F. Geenen, R. Biermans, and T. Meert, “Is the second phase of the formalin test useful to predict activity in chronic constriction injury models? A pharmacological comparison in different species,” Pain Practice, vol. 3, pp. 298–309, 2003.
- A. Brenchat, M. Ejarque, D. Zamanillo, J. M. Vela, L. Romero, et al., “Potentiation of morphine analgesia by adjuvant activation of 5-HT7 receptors,” Journal of Pharmacological Sciences, vol. 116, no. 4, pp. 388–391, 2011.
- A. Dogrul, M. H. Ossipov, and F. Porreca, “Differential mediation of descending pain facilitation and inhibition by spinal 5HT3 and 5HT7 receptors,” Brain Research, vol. 1280, pp. 52–59, 2009.
- A. Dogrul and M. Seyrek, “Systemic morphine produce antinociception mediated by spinal 5-HT7, but not 5-H and 5-HT2 receptors in the spinal cord,” British Journal of Pharmacology, vol. 149, no. 5, pp. 498–505, 2006.
- O. Yanarates, A. Dogrul, V. Yildirim et al., “Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, o-desmethyltramadol, via activation of descending serotonergic pathways,” Anesthesiology, vol. 112, no. 3, pp. 696–710, 2010.
- H. O. Kalkman and V. Neumann, “Evidence for a 5-H receptor-mediated hypothermic effect of the α1-adrenoceptor agonist, SDZ NVI-085, in guinea-pigs,” European Journal of Pharmacology, vol. 285, no. 3, pp. 313–315, 1995.