Preclinical characterization of BRL 44408: Antidepressant- and analgesic-like activity through selective α2A-adrenoceptor antagonism

International Journal of Neuropsychopharmacology

Volumn 13, Issue 9, 2010, Pages 1193-1205

  Dwyer, Jason M ^a   Platt, Brian J ^a   Sukoff Rizzo, Stacey J ^a   Pulicicchio, Claudine M ^a   Wantuch, Caitlin ^a   Zhang, Mei Yi ^a   Cummons, Terri ^a   Leventhal, Liza ^a   Bender, Corey N ^a   Zhang, Jean ^a   Kowal, Dianne ^a   Lu, Shendi ^a   Rajarao, S Johannes R ^a   Smith, Deborah L ^a   Shilling, Adam D ^a   Wang, Jianyao ^a   Butera, John ^a   Resnick, Lynn ^a   Rosenzweig Lipson, Sharon ^a   Schechter, Lee E ^a   Beyer, Chad E ^a   more..

^a PFIZER INC   (United States)

Author keywords

Adrenergic receptors; BRL 44408; depression; microdialysis; monoamines; pain

Indexed keywords

2 (1 METHYL 2 ISOINDOLINYLMETHYL) 2 IMIDAZOLINE; ACETYLCHOLINE; ALPHA 2A ADRENERGIC RECEPTOR; AUTORECEPTOR; CLONIDINE; DOPAMINE; IDAZOXAN; NORADRENALIN; PHENYLQUINONE; SEROTONIN; YOHIMBINE;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; BRAIN CORTEX; CENTRAL NERVOUS SYSTEM; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG RESPONSE; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; FLUID INTAKE; FORCED SWIMMING TEST; LOCOMOTION; MALE; MAXIMUM PLASMA CONCENTRATION; MOTOR COORDINATION; NEUROTRANSMITTER RELEASE; NONHUMAN; POLYDIPSIA; PREFRONTAL CORTEX; PRESYNAPTIC NERVE; PRIORITY JOURNAL; RAT; REGULATORY MECHANISM; TIME TO MAXIMUM PLASMA CONCENTRATION; VISCERAL PAIN;

ADRENERGIC ALPHA-2 RECEPTOR ANTAGONISTS; ANALGESICS; ANIMALS; ANTIDEPRESSIVE AGENTS; BIOGENIC MONOAMINES; BRAIN; CHO CELLS; CRICETINAE; CRICETULUS; DEPRESSION; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; IMIDAZOLES; ISOINDOLES; MALE; MICE; MICRODIALYSIS; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ADRENERGIC, ALPHA-2; SWIMMING; THIRST;

EID: 77957227893     PISSN: 14611457     EISSN: 14695111     Source Type: Journal    
DOI: 10.1017/S1461145709991088     Document Type: Article

References (50)

1. Apkarian AV, Bushnell MC, Treede RD, Zubieta JK (2005). Human brain mechanisms of pain perception and regulation in health and disease. European Journal of Pain 9, 463-484.
2. Bair MJ, Robinson RL, Katon W, Kroenke K (2003). Depression and pain comorbidity: a literature review. Archives of Internal Medicine 163, 2433-2445. (Pubitemid 37385786)
3. Beeley LJ, Berge JM, Chapman H, Hieble P, et al. (1995). Synthesis of a selective alpha-2A adrenoceptor antagonist, BRL 48962, and its characterization at cloned human alpha-adrenoceptors. Bioorganic Medicinal Chemistry 3, 1693-1698. (Pubitemid 26022444)
4. Beyer CE, Boikess S, Luo B, Dawson LA (2002). Comparison of the effects of antidepressants on norepinephrine and serotonin concentrations in the rat frontal cortex: an in-vivo microdialysis study. Journal of Psychopharmacology 16, 297-304. (Pubitemid 35470573)
5. Brody AL, Barsom MW, Bota RG, Saxena S (2001). Prefrontal-subcortical and limbic circuit mediation of major depressive disorder. Seminars in Clinical Neuropsychiatry 6, 102-112.
6. Brody AL, Saxena S, Silverman DH, Alborzian S, et al. (1999). Brain metabolic changes in major depressive disorder from pre- to post-treatment with paroxetine. Psychiatry Research 91, 127-139. (Pubitemid 29474048)
7. Cheng Y, Prusoff WH (1973). Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochemical Pharmacology 22, 3099-3108.
8. Chopin P, Colpaert FC, MarienM(2002). Effects of acute and subchronic administration of dexefaroxan, an alpha(2)- adrenoceptor antagonist, on memory performance in young adult and aged rodents. Journal of Pharmacology and Experimental Therapeutics 301, 187-196. (Pubitemid 34250294)
9. Civantos Calzada B, Aleixandre de Artinano A (2001). Alpha-adrenoceptor subtypes. Pharmacological Research 44, 195-208. (Pubitemid 32889462)
10. Cryan JF, Page ME, Lucki I (2005). Differential behavioral effects of the antidepressants reboxetine, fluoxetine, and moclobemide in a modified forced swim test following chronic treatment. Psychopharmacology (Berlin) 182, 335-344. (Pubitemid 41464645)
11. Dalley JW, Cardinal RN, Robbins TW (2004). Prefrontal executive and cognitive functions in rodents: neural and neurochemical substrates. Neuroscience and Biobehavioral Reviews 28, 771-784. (Pubitemid 39535871)
12. Dawson LA, Nguyen HQ, Geiger A (1999). Effects of venlafaxine on extracellular concentrations of 5-HT and noradrenaline in the rat frontal cortex: augmentation via 5-HT1A receptor antagonism. Neuropharmacology 38, 1153-1163. (Pubitemid 29292404)
13. Dennis T, LHeureux R, Carter C, Scatton B (1987). Presynaptic alpha-2 adrenoceptors play a major role in the effects of idazoxan on cortical noradrenaline release (as measured by in vivo dialysis) in the rat. Journal of Pharmacology and Experimental Therapeutics 241, 642-649. (Pubitemid 17111575)
14. Dunham NW, Miya TS (1957). A note on a simple apparatus for detecting neurological deficit in rats and mice. Journal of the American Pharmaceutical Association 46, 208-209.
15. Engleman EA, Perry KW, Mayle DA, Wong DT (1995). Simultaneous increases of extracellular monoamines in microdialysates from hypothalamus of conscious rats by duloxetine, a dual serotonin and norepinephrine uptake inhibitor. Neuropsychopharmacology 12, 287-295.
16. Fernandes KA, Yanpallewary SU, Vadodaria KC, Jhaveri D, et al. (2008). Alpha-2 adrenoceptors regulate adult hippocampal neurogenesis and accelerate the effects of chronic antidepressant treatment on gene expression, neurogenesis and behavior, 122.8/A8. 37th Annual Meeting for the Society for Neuroscience, Washington, DC.
17. Galeotti N, Bartolini A, Ghelardini C (2004). Alpha-2 agonist-induced memory impairment is mediated by the alpha-2A-adrenoceptor subtype. Behavioral Brain Research 153, 409-417. (Pubitemid 38953115)
18. Gilsbach R, Röser C, Beetz N, Brede M, et al. (2009). Genetic dissection of alpha2-adrenoceptor functions in adrenergic versus nonadrenergic cells. Molecular Pharmacology 75, 1160-1170.
19. Gobert A, Billiras R, Cistarelli L, Millan MJ (2004). Quantification and pharmacological characterization of dialysate levels of noradrenaline in the striatum of freely-moving rats: release from adrenergic terminals and modulation by alpha2-autoreceptors. Journal of Neuroscience Methods 140, 141-152. (Pubitemid 39625862)
20. Gobert A, Rivet JM, Audinot V, Newman-Tancredi A, et al. (1998). Simultaneous quantification of serotonin, dopamine and noradrenaline levels in single frontal cortex dialysates of freely-moving rats reveals a complex pattern of reciprocal auto- and heteroreceptor-mediated control of release. Neuroscience 84, 413-429. (Pubitemid 28122907)
21. Hein L, Altman JD, Kobilka BK (1999). Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission. Nature 402, 181-184.
22. Hertel P, Nomikos GG, Svensson TH (1999). Idazoxan preferentially increases dopamine output in the rat medial prefrontal cortex at the nerve terminal level. European Journal of Pharmacology 37, 153-158. (Pubitemid 29216997)
23. Hogg S, Dalvi A (2004). Acceleration of onset of action in schedule-induced polydipsia: combinations of SSRI and 5-HT1A and 5-HT1B receptor antagonists. Pharmacology Biochemistry and Behavior 77, 69-75. (Pubitemid 38076982)
24. Hoshaw BA, Malberg JE, Lucki I (2005). Central administration of IGF-I and BDNF leads to long-lasting antidepressant-like effects. Brain Research 1037, 204-208. (Pubitemid 40362398)
25. Kiss JP, Zsilla G, Mike A, Zelles T, et al. (1995). Subtype-specificity of the presynaptic alpha 2-adrenoceptors modulating hippocampal norepinephrine release in rat. Brain Research 674, 238-244.
26. Kobilka BK, Matsui H, Kobilka TS, Yang-Feng TL, et al. (1987). Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor. Science 238, 650-656. (Pubitemid 17158295)
27. Lahdesmaki J, Sallinen J, MacDonald E, Sirvio J, et al. (2003). Alpha2-adrenergic drug effects on brain monoamines, locomotion, and body temperature are largely abolished in mice lacking the alpha2Aadrenoceptor subtype. Neuropharmacology 44, 882-892. (Pubitemid 36515024)
28. Leventhal L, Smith V, Hornby G, Andree TH, et al. (2007). Differential and synergistic effects of selective norepinephrine and serotonin reuptake inhibitors in rodent models of pain. Journal of Pharmacology and Experimental Therapeutics 320, 1178-1185. (Pubitemid 46294041)
29. Meana JJ, Callado LF, Pazos A, Grijalba B, et al. (1996). The subtype-selective alpha 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. European Journal of Pharmacology 312, 385-388. (Pubitemid 26323522)
30. Mico JA, Ardid D, Berrocoso E, Eschalier A (2006). Antidepressants and pain. Trends in Pharmacological Sciences 27, 348-354. (Pubitemid 43963184)
31. Millan MJ, Gobert A, Girardon S, Dekeyne A (1999). Citalopram elicits a discriminative stimulus in rats at a dose selectively increasing extracellular levels of serotonin vs. dopamine and noradrenaline. European Journal of Pharmacology 364, 147-150. (Pubitemid 29065264)
32. Paxinos G, Watson C (1986). Rat Brain in Stereotactic Coordinates. San Diego: Academic Press.
33. Platt B, Beyer CE, Schechter LE, Rosenzweig-Lipson S (2008). Schedule-induced polydipsia: a rat model of obsessive-compulsive disorder. Current Protocols in Neuroscience, chapter 9, unit 9, 27.
34. Pudovkina OL, Kawahara Y, de Vries J, Westerink BH (2001). The release of noradrenaline in the locus coeruleus and prefrontal cortex studied with dual-probe microdialysis. Brain Research 906, 38-45. (Pubitemid 32595537)
35. Ramos BP, Arnsten AF (2007). Adrenergic pharmacology and cognition: focus on the prefrontal cortex. Pharmacology and Therapeutics 113, 523-536.
36. Rizk P, Salazar J, Raisman-Vozari R, Marien M, et al. (2006). The alpha2-adrenoceptor antagonist dexefaroxan enhances hippocampal neurogenesis by increasing the survival and differentiation of new granule cells. Neuropsychopharmacology 31, 1146-1157. (Pubitemid 43971832)
37. Rosenzweig-Lipson S, Sabb A, Stack G, Mitchell P, et al. (2007). Antidepressant-like effects of the novel, selective, 5-HT2C receptor agonist WAY-163909 in rodents. Psychopharmacology (Berlin) 192, 159-170. (Pubitemid 46669211)
38. Sallinen J, Link RE, Haapalinna A, Viitamaa T, et al. (1997). Genetic alteration of alpha 2C-adrenoceptor expression in mice: influence on locomotor, hypothermic, and neurochemical effects of dexmedetomidine, a subtype-nonselective alpha 2-adrenoceptor agonist. Molecular Pharmacology 51, 36-46.
39. Sanacora G, Berman RM, Cappiello A, Oren DA, et al. (2004). Addition of the alpha2-antagonist yohimbine to fluoxetine: effects on rate of antidepressant response. Neuropsychopharmacology 29, 1166-1171. (Pubitemid 38670053)
40. Scharfman H, Goodman J, Macleod A, Phani S, et al. (2005). Increased neurogenesis and the ectopic granule cells after intrahippocampal BDNF infusion in adult rats. Experimental Neurology 192, 348-356. (Pubitemid 40347259)
41. Schechter LE, Ring RH, Beyer CE, Hughes ZA, et al. (2005). Innovative approaches for the development of antidepressant drugs: current and future strategies. NeuroRx 2, 590-611. (Pubitemid 41393268)
42. Siegmund E, Cadmus R, Lu G (1957). A method for evaluating both non-narcotic and narcotic analgesics. Proceedings of the Society for Experimental Biology and Medicine 95, 729-731.
43. Smith MS, Schambra UB, Wilson KH, Page SO, et al. (1995). alpha 2-Adrenergic receptors in human spinal cord: specific localized expression of mRNA encoding alpha 2-adrenergic receptor subtypes at four distinct levels. Brain Research. Molecular Brain Research 34, 109-117.
44. Spiegel K, Kalb R, Pasternak GW (1983). Analgesic activity of tricyclic antidepressants. Annals of Neurology 13, 462-465. (Pubitemid 13116656)
45. Tavares A, Handy DE, Bogdanova NN, Rosene DL, et al. (1996). Localization of alpha 2A- and alpha 2B-adrenergic receptor subtypes in brain. Hypertension 27, 449-455. (Pubitemid 26082086)
46. van Veldhuizen MJ, Feenstra MG, Heinsbroek RP, Boer GJ (1993). In vivo microdialysis of noradrenaline overflow: effects of alpha-adrenoceptor agonists and antagonists measured by cumulative concentration-response curves. British Journal of Pharmacology 109, 655-660.
47. Whiteside GT, Harrison JE, Pearson MS, Chen Z, et al. (2004). DiPOA ([8-(3,3-diphenyl-propyl)x4-oxo-1-phenyl- 1,3,8-triazaspiro[4.5]dec-3-yl]-a cetic acid), a novel, systemically available, and peripherally restricted Mu opioid agonist with antihyperalgesic activity: II. In vivo pharmacological characterization in the rat. Journal of Pharmacology and Experimental Therapeutics 310, 793-799. (Pubitemid 38988926)
48. Woods A, Smith C, Szewczak M, Dunn RW, et al. (1993). Selective serotonin re-uptake inhibitors decrease scheduleinduced polydipsia in rats: a potential model for obsessive compulsive disorder. Psychopharmacology (Berlin) 112, 195-198. (Pubitemid 23278278)
49. Young P, Berge J, Chapman H, CawthorneMA(1989). Novel alpha 2-adrenoceptor antagonists show selectivity for alpha 2A- and alpha 2B-adrenoceptor subtypes. European Journal of Pharmacology 168, 381-386. (Pubitemid 19231516)
50. Zaborszky L, Rosin DL, Kiss J (2004). Alpha-adrenergic receptor (alpha(2 A)) is colocalized in basal forebrain cholinergic neurons: a light and electron microscopic double immunolabeling study. Journal of Neurocytology 33, 265-276. (Pubitemid 39361295)