Proxyfan acts as a neutral antagonist of histamine H3 receptors in the feeding-related hypothalamic ventromedial nucleus

British Journal of Pharmacology

Volumn 167, Issue 5, 2012, Pages 1099-1110

  Clapp, R H ^a   Luckman, S M ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

appetite; histamine; obesity; proxyfan; thioperamide; ventromedial nucleus

Indexed keywords

HISTAMINE; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; IMETIT; PROXYFAN; THIOPERAMIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BEHAVIOR DISORDER; BRAIN ELECTROPHYSIOLOGY; CONTROLLED STUDY; DECREASED APPETITE; DIET RESTRICTION; FEEDING; FEEDING BEHAVIOR; HYPOTHALAMUS VENTROMEDIAL NUCLEUS; IMMUNOHISTOCHEMISTRY; MALE; MOUSE; NERVE CELL STIMULATION; NONHUMAN; PRIORITY JOURNAL; PROTEIN DETERMINATION; RAT;

ANIMALS; EATING; HISTAMINE; HISTAMINE AGONISTS; HISTAMINE ANTAGONISTS; IMIDAZOLES; MALE; MICE; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; THIOUREA; VENTROMEDIAL HYPOTHALAMIC NUCLEUS;

EID: 84867303417     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.02056.x     Document Type: Article

References (59)

1. Alexander SPH, Mathie, A., Peters JA, (2011). Guide to Receptors and Channels (GRAC), 5th edn. Br. J. Pharmacol 164 (Suppl. 1): S1-S324.
2. Arrang JM, Garbarg M, Schwartz JC, (1983). Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature 302: 832-837. (Pubitemid 13125123)
3. Arrang JM, Garbarg M, Lancelot JC, Lecomte JM, Pollard H, Robba M, et al,. (1987). Highly potent and selective ligands for histamine H3-receptors. Nature 327: 117-123. (Pubitemid 17062756)
4. Arrang JM, Morisset S, Gbahou F, (2007). Constitutive activity of the histamine H3 receptor. Trends Pharmacol Sci 28: 350-357.
5. Baldi E, Bucherelli C, Schunack W, Cenni G, Blandina P, Passani MB, (2005). The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology 48: 246-251. (Pubitemid 40208260)
6. Barrett P, Ross AW, Balik A, Littlewood PA, Mercer JG, Moar KM, et al,. (2005). Photoperiodic regulation of histamine H3 receptor and VGF messenger ribonucleic acid in the arcuate nucleus of the Siberian hamster. Endocrinology 146: 1930-1939. (Pubitemid 40396902)
7. Borg MA, Sherwin RS, Borg WP, Tamborlane WV, Shulman GI, (1997). Local ventromedial hypothalamus glucose perfusion blocks counterregulation during systemic hypoglycemia in awake rats. J Clin Invest 99: 361-365. (Pubitemid 27053991)
8. Chiba S, Itateyama E, Sakata T, Yoshimatsu H, (2009). Acute central administration of immepip, a histamine H3 receptor agonist, suppresses hypothalamic histamine release and elicits feeding behavior in rats. Brain Res Bull 79: 37-40.
9. Dhillon H, Zigman JM, Ye C, Lee CE, McGovern RA, Tang V, et al,. (2006). Leptin directly activates SF1 neurons in the VMH, and this action by leptin is required for normal body-weight homeostasis. Neuron 49: 191-203. (Pubitemid 43089637)
10. Dodd GT, Mancini G, Lutz B, Luckman SM, (2010). The peptide hemopressin acts through CB1 cannabinoid receptors to reduce food intake in rats and mice. J Neurosci 30: 7369-7376.
11. Dupre C, Lovett-Barron M, Pfaff DW, Kow LM, (2010). Histaminergic responses by hypothalamic neurons that regulate lordosis and their modulation by estradiol. Proc Natl Acad Sci USA 107: 12311-12316.
12. Fox GB, Pan JB, Esbenshade TA, Bitner RS, Nikkel AL, Miller T, et al,. (2002). Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model. Pharmacol Biochem Behav 72: 741-750. (Pubitemid 34450873)
13. Fukagawa K, Sakata T, Shiraishi T, Yoshimatsu H, Fujimoto K, Ookuma K, et al,. (1989). Neuronal histamine modulates feeding behavior through H1-receptor in rat hypothalamus. Am J Physiol 256: R605-R611.
14. Garbarg M, Arrang JM, Rouleau A, Ligneau X, Tuong MD, Schwartz JC, et al,. (1992). S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agaonist. J Pharmacol Exp Ther 263: 304-310.
15. Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin JS, et al,. (2003). Protean agonism at histamine H3 receptors in vitro and in vivo. Proc Natl Acad Sci U S A 100: 11086-11091. (Pubitemid 37140156)
16. Haas HL, Sergeeva OA, Selbach O, (2008). Histamine in the nervous system. Physiol Rev 88: 1183-1241.
17. Hancock AA, Brune ME, (2005). Assessment of pharmacology and potential anti-obesity properties of H3 receptor antagonists/inverse agonists. Expert Opin Investig Drugs 14: 223-241. (Pubitemid 40520963)
18. Hancock AA, Bennani YL, Bush EN, Esbenshade TA, Faghih R, Fox GB, et al,. (2004). Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. Eur J Pharmacol 487: 183-197. (Pubitemid 38368996)
19. Hancock AA, Diehl MS, Fey TA, Bush EN, Faghih R, Miller TR, et al,. (2005). Antiobesity evaluation of histamine H3 receptor (H3R) antagonist analogs of A-331440 with improved safety and efficacy. Inflamm Res 54 (Suppl. 1): S27-S29. (Pubitemid 40880777)
20. Hawke Z, Ivanov TR, Bechtold DA, Dhillon H, Lowell BB, Luckman SM, (2009). PACAP neurons in the hypothalamic ventromedial nucleus are targets of central leptin signaling. J Neurosci 29: 14828-14835.
21. Henry MB, Zheng S, Duan C, Patel B, Vassileva G, Sondey C, et al,. (2011). Antidiabetic properties of the histamine H3 receptor protean agonist proxyfan. Endocrinology 152: 828-835.
22. Ishizuka T, Hatano K, Murotani T, Yamatodani A, (2008). Comparison of the effect of an H(3)-inverse agonist on energy intake and hypothalamic histamine release in normal mice and leptin resistant mice with high fat diet-induced obesity. Behav Brain Res 188: 250-254.
23. Itoh E, Fujimiya M, Inui A, (1998). Thioperamide, a histamine H3 receptor antagonist, suppresses NPY-but not dynorphin A-induced feeding in rats. Regul Pept 75-76: 373-376. (Pubitemid 28477549)
24. Itoh Y, Oishi R, Saeki K, (1991). Feeding-induced increase in the extracellular concentration of histamine in rat hypothalamus as measured by in vivo microdialysis. Neurosci Lett 125: 235-237.
25. Jang IS, Rhee JS, Watanabe T, Akaike N, Akaike N, (2001). Histaminergic modulation of GABAergic transmission in rat ventromedial hypothalamic neurones. J Physiol 534: 791-803. (Pubitemid 32700876)
26. Jethwa PH, Barrett P, Turnbull Y, Enright RA, Warner A, Murphy M, et al,. (2009). The role of histamine 3 receptors in the control of food intake in a seasonal model of obesity: the Siberian hamster. Behav Pharmacol 20: 155-165.
27. Kent P, Plamondon H, Merali Z, (1997). Pharmaco-ontogeny of bombesin's suppression of food intake and its attenuation by histamine H3 receptor agonists. Brain Res Dev Brain Res 102: 87-95. (Pubitemid 27376769)
28. King BM, (2006). The rise, fall, and resurrection of the ventromedial hypothalamus in the regulation of feeding behavior and body weight. Physiol Behav 87: 221-244. (Pubitemid 43188818)
29. Kow LM, Easton A, Pfaff DW, (2005). Acute estrogen potentiates excitatory responses of neurons in rat hypothalamic ventromedial nucleus. Brain Res 1043: 124-131. (Pubitemid 40603379)
30. Lawrence CB, Ellacott KL, Luckman SM, (2002). PRL-releasing peptide reduces food intake and may mediate satiety signaling. Endocrinology 143: 360-367. (Pubitemid 34107187)
31. Lecklin A, Tuomisto L, (1998). The blockade of H1 receptors attenuates the suppression of feeding and diuresis induced by inhibition of histamine catabolism. Pharmacol Biochem Behav 59: 753-758. (Pubitemid 28144220)
32. Lecklin A, Etu-Seppala P, Stark H, Tuomisto L, (1998). Effects of intracerebroventricularly infused histamine and selective H1, H2 and H3 agonists on food and water intake and urine flow in Wistar rats. Brain Res 793: 279-288. (Pubitemid 28294095)
33. Leurs R, Bakker RA, Timmerman H, de Esch IJ, (2005). The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov 4: 107-120. (Pubitemid 40277492)
34. 3 receptors. J Pharmacol Exp Ther 271: 452-459.
35. Lovenberg TW, Roland BL, Wilson SJ, Jiang X, Pyati J, Huvar A, et al,. (1999). Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol 55: 1101-1107. (Pubitemid 29252378)
36. Malmlof K, Zaragoza F, Golozoubova V, Refsgaard HH, Cremers T, Raun K, et al,. (2005). Influence of a selective histamine H3 receptor antagonist on hypothalamic neural activity, food intake and body weight. Int J Obes (Lond) 29: 1402-1412. (Pubitemid 41622218)
37. Malmlof K, Golozoubova V, Peschke B, Wulff BS, Refsgaard HH, Johansen PB, et al,. (2006). Increase of neuronal histamine in obese rats is associated with decreases in body weight and plasma triglycerides. Obesity (Silver Spring) 14: 2154-2162. (Pubitemid 46121970)
38. Malmlof K, Hastrup S, Wulff BS, Hansen BC, Peschke B, Jeppesen CB, et al,. (2007). Antagonistic targeting of the histamine H3 receptor decreases caloric intake in higher mammalian species. Biochem Pharmacol 73: 1237-1242. (Pubitemid 46413184)
39. McGrath J, Drummond G, McLachlan E, Kilkenny C, Wainwright C, (2010). Guidelines for reporting experiments involving animals: the ARRIVE guidelines. Br J Pharmacol 160: 1573-1576.
40. Merali Z, Banks K, (1994). Does the histaminergic system mediate bombesin/GRP-induced suppression of food intake? Am J Physiol 267: R1589-R1595.
41. Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, et al,. (2000). High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature 408: 860-864. (Pubitemid 32016096)
42. Ookuma K, Sakata T, Fukagawa K, Yoshimatsu H, Kurokawa M, Machidori H, et al,. (1993). Neuronal histamine in the hypothalamus suppresses food intake in rats. Brain Res 628: 235-242. (Pubitemid 2012693)
43. Orthen-Gambill N, Salomon M, (1992). FMH-induced decrease in central histamine levels produces increased feeding and body weight in rats. Physiol Behav 51: 891-893.
44. Passani MB, Blandina P, Torrealba F, (2011). The histamine H3 receptor and eating behavior. J Pharmacol Exp Ther 336: 24-29.
45. Paxinos G, Watson C, (1986). The Rat Brain in Stereotaxic Coordinates. Academic Press: San Diego.
46. Pillot C, Heron A, Cochois V, Tardivel-Lacombe J, Ligneau X, Schwartz JC, et al,. (2002). A detailed mapping of the histamine H(3) receptor and its gene transcripts in rat brain. Neuroscience 114: 173-193. (Pubitemid 35247499)
47. Poole SL, Lewis DI, Deuchars SA, (2008). Histamine depolarizes neurons in the dorsal vagal complex. Neurosci Lett 432: 19-24.
48. Sakata T, Ookuma K, Fukagawa K, Fujimoto K, Yoshimatsu H, Shiraishi T, et al,. (1988). Blockade of the histamine H1-receptor in the rat ventromedial hypothalamus and feeding elicitation. Brain Res 441: 403-407. (Pubitemid 18059993)
49. Sakata T, Fukagawa K, Ookuma K, Fujimoto K, Yoshimatsu H, Yamatodani A, et al,. (1990). Hypothalamic neuronal histamine modulates ad libitum feeding by rats. Brain Res 537: 303-306.
50. Scott V, Kimura N, Stark JA, Luckman SM, (2005). Intravenous peptide YY3-36 and Y2 receptor antagonism in the rat: effects on feeding behaviour. J Neuroendocrinol 17: 452-457. (Pubitemid 40873282)
51. Sheiner JB, Morris P, Anderson GH, (1985). Food intake suppression by histidine. Pharmacol Biochem Behav 23: 721-726. (Pubitemid 16201066)
52. Sindelar DK, Shepperd ML, Pickard RT, Alexander-Chacko J, Dill MJ, Cramer JW, et al,. (2004). Central H3R activation by thioperamide does not affect energy balance. Pharmacol Biochem Behav 78: 275-283. (Pubitemid 38829363)
53. Takahashi K, Suwa H, Ishikawa T, Kotani H, (2002). Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110: 1791-1799. (Pubitemid 36076486)
54. Tong Q, Ye C, McCrimmon RJ, Dhillon H, Choi B, Kramer MD, et al,. (2007). Synaptic glutamate release by ventromedial hypothalamic neurons is part of the neurocircuitry that prevents hypoglycemia. Cell Metab 5: 383-393. (Pubitemid 46667758)
55. Unger TJ, Calderon GA, Bradley LC, Sena-Esteves M, Rios M, (2007). Selective deletion of Bdnf in the ventromedial and dorsomedial hypothalamus of adult mice results in hyperphagic behavior and obesity. J Neurosci 27: 14265-14274.
56. Wulff BS, Hastrup S, Rimvall K, (2002). Characteristics of recombinantly expressed rat and human histamine H3 receptors. Eur J Pharmacol 453: 33-41. (Pubitemid 35232452)
57. Yoshimoto R, Miyamoto Y, Shimamura K, Ishihara A, Takahashi K, Kotani H, et al,. (2006). Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Proc Natl Acad Sci USA 103: 13866-13871. (Pubitemid 44413999)
58. Yoshimoto R, Kanatani A, Tokita S, (2008). Distinctive role of central histamine H3 receptor in various orexigenic pathways. Eur J Pharmacol 579: 229-232.
59. Zhou J, Lee AW, Devidze N, Zhang Q, Kow LM, Pfaff DW, (2007). Histamine-induced excitatory responses in mouse ventromedial hypothalamic neurons: ionic mechanisms and estrogenic regulation. J Neurophysiol 98: 3143-3152.