Regulation of ingestive behaviors in the rat by GSK1521498, a novel μ-opioid receptor-selective inverse agonist

Journal of Pharmacology and Experimental Therapeutics

Volumn 339, Issue 1, 2011, Pages 24-34

  Ignar, Diane M ^a   Goetz, Aaron S ^a   Noble, Kimberly Nichols ^a   Carballo, Luz Helena ^a   Stroup, Andrea E ^a   Fisher, Julie C ^a   Boucheron, Joyce A ^a   Brainard, Tracy A ^a   Larkin, Andrew L ^a   Epperly, Andrea H ^a   Shearer, Todd W ^a   Sorensen, Scott D ^a   Speake, Jason D ^a   Hommel, Jonathan D ^a,b  

^a GLAXOSMITHKLINE   (United States)

^b University of Texas Medical Branch School of Medicine   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DELTA OPIATE RECEPTOR; GSK 1521498; KAPPA OPIATE RECEPTOR; MU OPIATE RECEPTOR AGONIST; N [[3,5 DIFLUORO 3' (1H 1,2,4 TRIAZOL 3 YL) 4 BIPHENYLYL]METHYL] 2,3 DIHYDRO 1H INDEN 2 AMINE; NALTREXONE; SUCROSE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; BRAIN SLICE; CONTROLLED STUDY; CORRELATION ANALYSIS; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG SELECTIVITY; FEEDING BEHAVIOR; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR OCCUPANCY; SATIETY; SINGLE DRUG DOSE; WEIGHT REDUCTION;

ADIPOSITY; ANIMALS; ANTI-OBESITY AGENTS; BODY WEIGHT; BRAIN; CALIBRATION; CONDITIONING, OPERANT; DATA INTERPRETATION, STATISTICAL; DRINKING BEHAVIOR; FEEDING BEHAVIOR; FOOD PREFERENCES; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); INDANS; INJECTIONS, INTRAVENOUS; MALE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID, DELTA; RECEPTORS, OPIOID, KAPPA; RECEPTORS, OPIOID, MU; SATIETY RESPONSE; TRIAZOLES; WEIGHT LOSS;

EID: 80053164213     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.180943     Document Type: Article

References (40)

1. Atkinson RL, Berke LK, Drake CR, Bibbs ML, Williams FL, and Kaiser DL (1985) Effects of long-term therapy with naltrexone on body weight in obesity. Clin Pharmacol Ther 38:419-422. (Pubitemid 16250316)
2. Barnes MJ, Holmes G, Primeaux SD, York DA, and Bray GA (2006) Increased expression of mu opioid receptors in animals susceptible to diet-induced obesity. Peptides 27:3292-3298. (Pubitemid 44738177)
3. Bolaños CA, Barrot M, Berton O, Wallace-Black D, and Nestler EJ (2003) Methylphenidate treatment during pre- and periadolescence alters behavioral responses to emotional stimuli at adulthood. Biol Psychiatry 54:1317-1329. (Pubitemid 37522155)
4. Chen G, Jayawikreme C, Way J, Armour S, Queen K, Watson C, Ignar D, Chen WJ, and Kenakin T (1999) Constitutive receptor systems for drug discovery. J Pharmacol Toxicol 42:199-206.
5. Condreay JP, Witherspoon SM, Clay WC, and Kost TA (1999) Transient and stable gene expression in mammalian cells transduced with a recombinant baculovirus vector. Proc Natl Acad Sci USA 96:127-132. (Pubitemid 29036064)
6. Cowan DJ (2010) Identification of novel potent opioid inverse agonists. Abstracts of Papers, 239th ACS National Meeting; 2010 Mar 21-25; San Francisco, CA. American Chemical Society, Washington, DC.
7. Drewnowski A (1997) Taste preferences and food intake. Annu Rev Nutr 17:237-253.
8. 3H]-LY255582 binding sites in mouse brain: comparison with the distribution of mu, delta and kappa binding sites. Neuropeptides 39:559-567.
9. Gavériaux-Ruff C and Kieffer BL (2002) Opioid receptor genes inactivated in mice: the highlights. Neuropeptides 36:62-71.
10. Hill JO (2006) Understanding and addressing the epidemic of obesity: an energy balance perspective. Endocr Rev 27:750-761.
11. Hommel JD, Trinko R, Sears RM, Georgescu D, Liu ZW, Gao XB, Thurmon JJ, Marinelli M, and DiLeone RJ (2006) Leptin receptor signaling in midbrain dopamine neurons regulates feeding. Neuron 51:801-810. (Pubitemid 44374908)
12. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed. Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington DC.
13. Kelley AE and Berridge KC (2002) The neuroscience of natural rewards: relevance to addictive drugs. J Neurosci 22:3306-3311. (Pubitemid 37465733)
14. Kenakin T (1995) The physiological significance of constitutive receptor activity. Trends Pharmacol Sci 26:603-605.
15. Levine AS and Billington CJ (1997) Why do we eat? A neural systems approach. Annu Rev Nutr 17:597-619. (Pubitemid 27328814)
16. Maccioni P, Pes D, Carai MA, Gessa GL, and Colombo G (2008) Suppression by the cannabinoid CB1 receptor antagonist, rimonabant, of the reinforcing and motivational properties of a chocolate-flavoured beverage in rats. Behav Pharmacol 19:197-209. (Pubitemid 351670400)
17. Malcolm R, O'Neil PM, Sexauer JD, Riddle FE, Currey HS, and Counts C (1985) A controlled trial of naltrexone in obese humans. Int J Obes 9:347-353. (Pubitemid 16201361)
18. Mansour A, Hoversten MT, Taylor LP, Watson SJ, and Akil H (1995) The cloned -, δ and κ receptors and their endogenous ligands: evidence for two opioid peptide recognition cores. Brain Res 700:89-98.
19. Martin WR, Wikler A, Eades CG, and Pescor FT (1963) Tolerance to and physical dependence on morphine in rats. Psychopharmacologia 4:247-260.
20. Mitch CH, Leander JD, Mendelsohn LG, Shaw WN, Wong DT, Cantrell BE, Johnson BG, Reel JK, Snoddy JD, and Takemori AE (1993) 3,4-Dimethyl-4-(3- hydroxyphenyl) piperidines: opioid antagonists with potent anorectant activity. J Med Chem 36:2842-2850. (Pubitemid 23315386)
21. Morton GJ, Cummings DE, Baskin DG, Barsh GS, and Schwartz MW (2006) Central nervous system control of food intake and body weight. Nature 443:289-295. (Pubitemid 44435142)
22. Mucha RF and Iversen SD (1986) Increased food intake after opioid microinjections into nucleus accumbens and ventral tegmental area of rat. Brain Res 397:214-224. (Pubitemid 17185811)
23. Nair SG, Golden SA, and Shaham Y (2008) Differential effects of the hypocretin 1 receptor antagonist SB 334867 on high-fat food self-administration and reinstatement of food seeking in rats. Br J Pharmacol 154:406-416. (Pubitemid 351670600)
24. Nathan PJ, O'Neill BV, Bush MA, Koch A, Tao WX, Maltby K, Napolitano A, Brooke AC, Skeggs AL, Herman CS, et al. (2011) Opioid receptor modulation of hedonic taste preference and food intake: a single dose safety, pharmacokinetic and pharmacodynamic investigation with GSK1521498, a novel mu-opioid receptor inverse agonist. J Clin Pharmacol doi:10.1177/0091270011399577.
25. Ogden CL, Carroll MD, Curtin LR, McDowell MA, Tabak CJ, and Flegal KM (2006) Prevalence of overweight and obesity in the United States, 1999-2004. JAMA 295:1549-1555.
26. Papaleo F, Kieffer BL, Tabarin A, and Contarino A (2007) Decreased motivation to eat in μ-opioid receptor-deficient mice. Eur J Neurosci 25:3398-3405. (Pubitemid 46872779)
27. Peciña S and Berridge KC (2000) Opioid site in nucleus accumbens shell mediates eating and hedonic 'liking' for food: map based on microinjection Fos plumes. Brain Res 863:71-86. (Pubitemid 30201586)
28. Poisnel G, Quentin T, Barré L, Coquerel A, and Debruyne D (2006) Competitive displacement binding assay on rat brain sections and using a β-imager: application to μ-opioid ligands. J Neurosci Methods 154:60-67. (Pubitemid 43949057)
29. Rabiner EA, Beaver J, Makwana A, Searle G, Long C, Nathan PJ, Newbould RD, Howard J, Miller SR, Bush MA, et al. (2011). Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans. Mol Psychiatry 16: 826-835.
30. Rolls ET (2007) Understanding the mechanisms of food intake and obesity. Obes Rev 8 (Suppl 1):67-72.
31. Shaw WN (1993) Long-term treatment of obese Zucker rats with LY255582 and other appetite suppressants. Pharmacol Biochem Behav 46:653-659.
32. Smith KS and Berridge KC (2007) Opioid limbic circuit for reward: interaction between hedonic hotspots of nucleus accumbens and ventral pallidum. J Neurosci 27:1594-1605. (Pubitemid 46280077)
33. Smith SL, Harrold JA, and Williams G (2002) Diet-induced obesity increases mu opioid receptor binding in specific regions of the rat brain. Brain Res 953:215-222. (Pubitemid 35217823)
34. Statnick MA, Tinsley FC, Eastwood BJ, Suter TM, Mitch CH, and Heiman ML (2003) Peptides that regulate food intake: antagonism of opioid receptors reduces body fat in obese rats by decreasing food intake and stimulating lipid utilization. Am J Physiol Regul Integr Comp Physiol 284:R1399-R1408. (Pubitemid 36617478)
35. Tabarin A, Diz-Chaves Y, Chaves YD, Carmona Mdel C, Catargi B, Zorrilla EP, Roberts AJ, Coscina DV, Rousset S, Redonnet A, et al. (2005) Resistance to diet-induced obesity in μ-opioid receptor-deficient mice: evidence for a "thrifty gene." Diabetes 54:3510-3516. (Pubitemid 43334343)
36. Will MJ, Franzblau EB, and Kelley AE (2003) Nucleus accumbens μ-opioids regulate intake of a high-fat diet via activation of a distributed brain network. J Neurosci 23:2882-2888. (Pubitemid 36418624)
37. Xu L, Zhang F, Zhang DD, Chen XD, Lu M, Lin RY, Wen H, Jin L, and Wang XF (2009) OPRM1 gene is associated with BMI in Uyghur population. Obesity 17:121-125. (Pubitemid 50331905)
38. Zhang M, Gosnell BA, and Kelley AE (1998) Intake of high-fat food is selectively enhanced by mu opioid receptor stimulation within the nucleus accumbens. J Pharmacol Exp Ther 285:908-914. (Pubitemid 28237478)
39. Zhang M and Kelley AE (1997) Opiate agonists microinjected into the nucleus accumbens enhance sucrose drinking in rats. Psychopharmacology (Berl) 132:350-360. (Pubitemid 27373476)
40. Zhang M and Kelley AE (2000) Enhanced intake of high-fat food following striatal mu-opioid stimulation: microinjection mapping and fos expression. Neuroscience 99:267-277. (Pubitemid 30628414)