Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy

European Journal of Pharmacology

Volumn 616, Issue 1-3, 2009, Pages 101-106

  Able, Sarah L ^a   Ivarsson, Magnus ^a   Fish, Rebecca L ^a   Clarke, Tracey L ^a   McCourt, Clare ^b   Duckworth, Jonathan M ^a   Napier, Carolyn ^a   Katugampola, Sidath D ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b QUEEN'S UNIVERSITY BELFAST   (United Kingdom)

Author keywords

(Rat); CNS; EEG; Melanin concentrating hormone receptor 1; Occupancy

Indexed keywords

4' [[1 (CYCLOPROPYLMETHYL)PIPERIDIN 4 YLIDENE][5 FLUORO 6 (TRIFLUOROMETHYL) 1H BENZIMIDAZOL 2 YL]METHYL]BIPHENYL 3 CARBONITRILE; 6 (4 CHLOROPHENYL) 3 [3 METHOXY 4 [2 (1 PYRROLIDINYL)ETHOXY]PHENYL]THIENOL[3,2 D]PYRIMIDIN 4(3H) ONE; GW 3430; IODINE 125; MELANIN CONCENTRATING HORMONE RECEPTOR 1; MELANIN CONCENTRATING HORMONE RECEPTOR 1 ANTAGONIST; N [3 [1 [[4 (3,4 DIFLUOROPHENOXY)PHENYL]METHYL](4 PIPERIDYL)] 4 METHYLPHENYL] 2 METHYLPROPANAMIDE; SNAP 94847; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BINDING AFFINITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG RECEPTOR BINDING; ELECTROENCEPHALOGRAPHY; MALE; NONHUMAN; PRIORITY JOURNAL; PROTEIN LOCALIZATION; PUTAMEN; RAT; RECEPTOR BLOCKING; SLEEP PARAMETERS; SLEEP PATTERN; SLEEP WAKING CYCLE;

ANIMALS; AUTORADIOGRAPHY; BENZIMIDAZOLES; BINDING, COMPETITIVE; BRAIN; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROENCEPHALOGRAPHY; MALE; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SOMATOSTATIN; SLEEP; SUBSTRATE SPECIFICITY;

EID: 67651098876     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2009.06.009     Document Type: Article

References (29)

1. Adamantidis A., Salvert D., Goutagny R., Lakaye B., Gervasoni D., Grisar T., Luppi P.H., and Fort P. Sleep architecture of the melanin-concentrating hormone receptor 1-knockout mice. Eur. J. Neurosci. 27 (2008) 1793-1800
2. Ahnaou A., Drinkenburg W.H.I.M., Bouwknecht J.A., Alcazar J., Steckler T., and Dautzenberg F.M. Blocking melanin-concentrating hormone MCH1 receptor affects rat sleep-wake architecture. Eur. J. Pharmacol. 579 (2008) 177-188
3. Audinot V., Lahaye C., Suply T., Beauverger P., Rodriguez M., Galizzi J.P., Fauchere J.L., and Boutin J.A. [125I]-S36057: a new and highly potent radioligand for the melanin-concentrating hormone receptor. Br. J. Pharmacol. 133 (2001) 371-378
4. Bittencourt J.C., Presse F., Arias C., Peto C., Vaughan J., Nahon J.L., Vale W., and Sawchenko P.E. The melanin-concentrating hormone system of the rat brain: an immuno- and hybridization histochemical characterization. J. Comp. Neurol. 319 (1992) 218-245
5. Brignol N., McMahon L.M., Luo S., and Tse F.L. High-throughput semi-automated 96-well liquid/liquid extraction and liquid chromatography/mass spectrometric analysis of everolimus (RAD 001) and cyclosporin a (CsA) in whole blood. Rapid. Commun. Mass Spectrom. 15 (2001) 898-907
6. Chambers J., Ames R.S., Bergsma D., Muir A., Fitzgerald L.R., Hervieu G., Dytko G.M., Foley J.J., Martin J., Liu W.S., Park J., Ellis C., Ganguly S., Konchar S., Cluderay J., Leslie R., Wilson S., and Sarau H.M. Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1. Nature 400 (1999) 261-265
7. Chen Y., Hu C., Hsu C.K., Zhang Q., Bi C., Asnicar M., Hsiung H.M., Fox N., Slieker L.J., Yang D.D., Heiman M.L., and Shi Y. Targeted disruption of the melanin-concentrating hormone receptor-1 results in hyperphagia and resistance to diet-induced obesity. Endocrinology 143 (2002) 2469-2477
8. Cheng Y., and Prusoff W.H. Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 percent inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol. 22 (1973) 3099-3108
9. David D.J., Klemenhagan K.C., Holick K.A., Saxe M.D., Mendez I., Santarelli L., Craig D.A., Zhong H., Swanson C.J., Hegde L.G., Ping X.I., Dong D., Marzabadi M.R., Gerald C.P., and Hen R. Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis. J. Pharmacol. Exp. Ther. 321 (2007) 237-248
10. Dumont G.J.H., de Visser S.J., Cohen A.F., and van Gerven J.M.A. Biomarkers for the effects of selective serotonin reuptake inhibitors (SSRIs) in healthy subjects. Br. J. Clin. Pharmacol. 59 (2005) 495-510
11. Dzirasa K., Ribeiro S., Costa R., Santos L.M., Lin S.C., Grosmark A., Sotnikova T.D., Gainetdinov R.R., Caron M.G., and Nicolelis M.A. Dopaminergic control of sleep-wake states. J. Neurosci. 26 (2006) 10577-10589
12. Fong T.M., Guan X.M., Marsh D.J., Shen C.P., Sloan Stribling D., Rosko K.M., Lao J., Yu H., Feng Y., Xiao J.C., Van der Ploeg L.H.T., Goulet M.T., Hagmann W.K., Lin L.S., Lanza T.J., Jewell J.P., Liu P., Shah S.K., Tong H.Q.X., Wang J., Xu S.S., Francis B., Strack A.M., MacIntyre D.E., and Shearman L.P. Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), in rodents. J. Pharmacol. Exp. Ther. 321 (2007) 1013-1022
13. Hervieu G.J., Cluderay J.E., Harrison D., Meakin J., Maycox P., Nasir S., and Leslie R.A. The distribution of the mRNA and protein products of the melanin-concentrating hormone (MCH) receptor gene, slc-1, in the central nervous system of the rat. Eur. J. Neurosci. 12 (2000) 1194-1216
14. Ivarsson M., Paterson L.M., and Hutson P.H. Antidepressants and REM sleep in Wistar-Kyoto and Sprague-Dawley rats. Eur. J. Pharmacol. 522 (2005) 63-71
15. Kantor S., Jakus R., Bodizs R., Halasz P., and Bagdy G. Acute and long-term effects of the 5-HT receptor antagonist 2 ritanserin on EEG power spectra, motor activity, and sleep: changes at the light-dark phase shift. Brain Res. 943 (2002) 105-111
16. Kawauchi H., Kawazoe I., Tsubokawa M., Kishida M., and Baker B.I. Characterization of melanin-concentrating hormone in chum salmon pituitaries. Nature 305 (1983) 321-323
17. Li Y.W., Hill G., Wong H., Kelly N., Ward K., Pierdomenico M., Ren S., Gilligan P., Grossman S., Trainor G., Taub R., McElroy J., and Zazcek R. Receptor occupancy of nonpeptide corticotropin-releasing factor 1 antagonist DMP696: correlation with drug exposure and anxiolytic efficacy. J. Pharmacol. Exp. Ther. 305 (2003) 86-96
18. Marsh D.J., Weingarth D.T., Novi D.E., Chen H.Y., Trumbauer M.E., Chen A.S., Guan X.M., Jiang M.M., Feng Y., Camacho R.E., Shen Z., Frazier E.G., Yu H., Metzger J.M., Kuca S.J., Shearman L.P., Gopal-Truter S., MacNeil D.J., Strack A.M., MacIntyre D.E., Van der Ploeg L.H.T., and Qian S. Proc. Natl. Acad. Sci. U. S. A. 99 (2002) 3240-3245
19. Mashiko S., Ishihara A., Gomori A., Moriya R., Ito M., Iwaasa H., Matsuda M., Feng Y., Shen Z., Marsh D.J., Bednarek M.A., MacNeil D.J., and Kanatani A. Antiobesity effect of a melanin-concentrating hormone 1 receptor antagonist in diet-induced obese mice. Endocrinology 146 (2005) 3080-3086
20. McBriar M.D., Guzik H., Shapiro S., Paruchova J., Xu R., Palani A., Clader J.W., Cox K., Greenlee W.J., Hawes B.E., Kowalski T.J., O'Neill K., Spar B.D., Weig B., Weston D.J., Farley C., and Cook J. Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J. Med. Chem. 49 (2006) 2294-2310
21. 1 muscarinic acetylcholine receptor agonism alters sleep without affecting memory consolidation. J. Cogn. Neurosci. 18 (2006) 1799-1807
22. Qu D., Ludwig D.S., Gammeltoft S., Piper M., Pelleymounter M.A., Cullen M.J., Mathes W.F., Przypek R., Kanarek R., and Maratos-Flier E. A role for melanin-concentrating hormone in the central regulation of feeding behaviour. Nature 380 (1996) 243-247
23. Sailer A.W., Sano H., Zeng Z., McDonald T.P., Pan J., Pong S.S., Feighner S.D., Tan C.P., Fukami T., Iwaasa H., Hreniuk D.L., Morin N.R., Sadowski S.J., Ito M., Bansali A., Ky B., Figueroa D.J., Jiang Q., Austin C.P., MacNeil D.J., Ishihara A., Ihara M., Kanatani A., Van der Ploeg L.H.T., Howard A.D., and Liu Q. Identification and characterization of a second melanin concentrating hormone receptor, MCH-2R. Proc. Natl. Acad. Sci. U. S. A. 98 (2001) 7564-7569
24. Shearman L.P., Camacho R.E., Stribling D.S., Zhou D., Bednarek M.A., Hreniuk D.L., Feighner S.D., Tan C.P., Howard A.D., Van der Ploeg L.H.T., MacIntyre D.E., Hickey G.J., and Strack A.M. Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats. Eur. J. Pharmacol. 475 (2003) 37-47
25. Smith D.G., Jarvis R.J., Rorick-Kehn L., Morin M., Witkin J.M., McKinzie D.L., Nomikos G.G., and Gehlert D.R. Melanin-concentrating hormone-1 receptor modulates neuroendocrine, behavioral, and corticolimbic neurochemical stress responses in mice. Neuropsychopharmacology 31 (2006) 1135-1145
26. Tan C.P., Sano H., Iwaasa H., Pan J., Sailer A.W., Hreniuk D.L., Feighner S.D., Palyha O.C., Pong S.S., Figueroa D.J., Austin C.P., Jiang M.M., Yu H., Ito J., Ito M., Ito M., Guan X.M., MacNeil D.J., Kanatani A., Van der Ploeg L.H.T., and Howard A.D. Melanin-concentrating hormone receptor subtypes 1 and 2: species-specific gene expression. Genomics 79 (2002) 785-792
27. Verret L., Goutagny R., Fort P., Cagnon L., Salvert D., Léger L., Boissard R., Salin P., Peyron P., and Luppi P.H. A role of melanin-concentrating hormone producing neurons in the central regulation of paradoxical sleep. BMC Neurosci. 9 (2003) 4-19
28. Wagner J.A. Strategic approach to fit-for-purpose biomarkers in drug development. Ann. Rev. Pharmacol. Toxicol. 48 (2008) 631-651
29. Wu W.L., Burnett D.A., Caplen M.A., Domalski M.S., Bennett C., Greenlee W.J., Hawes B.E., O'Neill K., Weig B., Weston D., Spar B., and Kowalski T. Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists. Bioorg. Med. Chem. Lett. 16 (2006) 3674-3678