메뉴 건너뛰기




Volumn 10, Issue , 2010, Pages

Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) Receptor Antagonist

Author keywords

[No Author keywords available]

Indexed keywords

1 [7 (2 CHLOROPHENYL) 8 (4 CHLOROPHENYL) 2 METHYLPYRAZOLO[1,5 A][1,3,5]TRIAZIN 4 YL] 3 ETHYLAMINOAZETIDINE 3 CARBOXYLIC ACID HYDROCHLORIDE; CANNABINOID 1 RECEPTOR AGONIST; CARBOHYDRATE; CE 178253; FAT; UNCLASSIFIED DRUG; ANOREXIGENIC AGENT; AZETIDINE DERIVATIVE; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR; CE-178253; TRIAZINE DERIVATIVE;

EID: 77955528474     PISSN: None     EISSN: 14712210     Source Type: Journal    
DOI: 10.1186/1471-2210-10-9     Document Type: Article
Times cited : (13)

References (35)
  • 6
    • 0030738512 scopus 로고    scopus 로고
    • Selective inhibition of sucrose and ethanol intake by SR 141716, an antagonist of central cannabinoid (CB1) receptors
    • 10.1007/s002130050326, 9272766
    • Arnone M, Maruani J, Chaperon F, Thiebot M-H, Poncelet M, Soubrie P, Le Fur G. Selective inhibition of sucrose and ethanol intake by SR 141716, an antagonist of central cannabinoid (CB1) receptors. Psychopharmacology 1997, 132(1):104-106. 10.1007/s002130050326, 9272766.
    • (1997) Psychopharmacology , vol.132 , Issue.1 , pp. 104-106
    • Arnone, M.1    Maruani, J.2    Chaperon, F.3    Thiebot, M.-.H.4    Poncelet, M.5    Soubrie, P.6    Le Fur, G.7
  • 8
    • 66649085214 scopus 로고    scopus 로고
    • Minireview: Endocannabinoids and Their Receptors as Targets for Obesity Therapy
    • de Kloet AD, Woods SC. Minireview: Endocannabinoids and Their Receptors as Targets for Obesity Therapy. Endocrinol 2009, 50(6):2531-2536.
    • (2009) Endocrinol , vol.50 , Issue.6 , pp. 2531-2536
    • de Kloet, A.D.1    Woods, S.C.2
  • 9
    • 57749119549 scopus 로고    scopus 로고
    • Endocannabinoids and the Control of Energy Homeostasis
    • 10.1074/jbc.R800012200, 2586261, 18694938
    • Kunos G, Osei-Hyiaman D, Liu J, Godlewski G, Batkai S. Endocannabinoids and the Control of Energy Homeostasis. J Biol Chem 2008, 283(48):33021-33025. 10.1074/jbc.R800012200, 2586261, 18694938.
    • (2008) J Biol Chem , vol.283 , Issue.48 , pp. 33021-33025
    • Kunos, G.1    Osei-Hyiaman, D.2    Liu, J.3    Godlewski, G.4    Batkai, S.5
  • 10
    • 32444440208 scopus 로고    scopus 로고
    • The emerging role of the endocannabinoid system in endocrine regulation and energy balance
    • 10.1210/er.2005-0009, 16306385
    • Pagotto U, Marsicano G, Cota D, Lutz B, Pasquali R. The emerging role of the endocannabinoid system in endocrine regulation and energy balance. Endocr Rev 2006, 27:73-100. 10.1210/er.2005-0009, 16306385.
    • (2006) Endocr Rev , vol.27 , pp. 73-100
    • Pagotto, U.1    Marsicano, G.2    Cota, D.3    Lutz, B.4    Pasquali, R.5
  • 13
    • 60549088559 scopus 로고    scopus 로고
    • Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-Yl]-4-ethylaminopiperidine-4-carboxylic Acid Amine Hydrochloride (CP-945,598), a Novel, Potent and Selective Cannabinoid CB1 Receptor Antagonist
    • 10.1021/jm8012932, 19102698
    • Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL, Landis MS, O'Connor RE, Scott DO. Discovery of 1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-Yl]-4-ethylaminopiperidine-4-carboxylic Acid Amine Hydrochloride (CP-945,598), a Novel, Potent and Selective Cannabinoid CB1 Receptor Antagonist. J Med Chem 2009, 52:234-237. 10.1021/jm8012932, 19102698.
    • (2009) J Med Chem , vol.52 , pp. 234-237
    • Griffith, D.A.1    Hadcock, J.R.2    Black, S.C.3    Iredale, P.A.4    Carpino, P.A.5    DaSilva-Jardine, P.6    Day, R.7    DiBrino, J.8    Dow, R.L.9    Landis, M.S.10    O'Connor, R.E.11    Scott, D.O.12
  • 14
    • 34548848043 scopus 로고    scopus 로고
    • Blockade of cannabinoid type 1 receptors augments the antiparkinsonian action of levodopa without affecting dyskinesias in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated rhesus monkeys
    • 10.1124/jpet.107.125666, 17630359
    • Cao X, Liang L, Hadcock JR, Iredale PA, Griffith DA, Menniti FS, Factor S, Greenamyre JT, Papa SM. Blockade of cannabinoid type 1 receptors augments the antiparkinsonian action of levodopa without affecting dyskinesias in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated rhesus monkeys. J Pharmacol Exp Ther 2007, 323(1):318-326. 10.1124/jpet.107.125666, 17630359.
    • (2007) J Pharmacol Exp Ther , vol.323 , Issue.1 , pp. 318-326
    • Cao, X.1    Liang, L.2    Hadcock, J.R.3    Iredale, P.A.4    Griffith, D.A.5    Menniti, F.S.6    Factor, S.7    Greenamyre, J.T.8    Papa, S.M.9
  • 16
    • 0029859983 scopus 로고    scopus 로고
    • Identification and characterization of novel somatostatin antagonists
    • Bass R, Strnad J, Price LA, Pausch MH, Hadcock JR. Identification and characterization of novel somatostatin antagonists. Mol Pharm 1996, 50:709-715.
    • (1996) Mol Pharm , vol.50 , pp. 709-715
    • Bass, R.1    Strnad, J.2    Price, L.A.3    Pausch, M.H.4    Hadcock, J.R.5
  • 17
    • 11144290156 scopus 로고    scopus 로고
    • Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice
    • 10.1124/dmd.104.001222, 15502010
    • Maurer TS, Debartolo DB, Tess DA, Scott DO. Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug metabolism and disposition: the biological fate of chemicals 2005, 33(1):175-81. 10.1124/dmd.104.001222, 15502010.
    • (2005) Drug metabolism and disposition: the biological fate of chemicals , vol.33 , Issue.1 , pp. 175-181
    • Maurer, T.S.1    Debartolo, D.B.2    Tess, D.A.3    Scott, D.O.4
  • 18
    • 0030853692 scopus 로고    scopus 로고
    • SR-141716 is an inverse agonist at the human cannabinoid CB1 receptor
    • 10.1016/S0014-2999(97)01160-6, 9346339
    • Landsman RS, Burkey TH, Consroe P, Roeske WR, Yamamura HI. SR-141716 is an inverse agonist at the human cannabinoid CB1 receptor. Eur J Pharmacol 1997, 334:R1-R2. 10.1016/S0014-2999(97)01160-6, 9346339.
    • (1997) Eur J Pharmacol , vol.334
    • Landsman, R.S.1    Burkey, T.H.2    Consroe, P.3    Roeske, W.R.4    Yamamura, H.I.5
  • 19
    • 61349143694 scopus 로고    scopus 로고
    • The enigmatic pharmacology of GPR55
    • Roth RA. The enigmatic pharmacology of GPR55. Trends Pharmacol Sci 2005, 30(3):156-163.
    • (2005) Trends Pharmacol Sci , vol.30 , Issue.3 , pp. 156-163
    • Roth, R.A.1
  • 20
    • 0035918311 scopus 로고    scopus 로고
    • The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism
    • 10.1074/jbc.M008555200, 11278420
    • De Petrocellis L, Bisogno T, Maccarrone M, Davis JB, Finazzi-Agro A, Di Marzo V. The activity of anandamide at vanilloid VR1 receptors requires facilitated transport across the cell membrane and is limited by intracellular metabolism. J Biol Chem 2001, 276(16):12856-63. 10.1074/jbc.M008555200, 11278420.
    • (2001) J Biol Chem , vol.276 , Issue.16 , pp. 12856-12863
    • De Petrocellis, L.1    Bisogno, T.2    Maccarrone, M.3    Davis, J.B.4    Finazzi-Agro, A.5    Di Marzo, V.6
  • 21
    • 34247523747 scopus 로고    scopus 로고
    • Regulation of transient receptor potential channels of melastatin type 8 (TRPM8): effect of cAMP, cannabinoid CB(1) receptors and endovanilloids
    • 10.1016/j.yexcr.2007.01.008, 17428469
    • De Petrocellis L, Starowicz K, Moriello AS, Vivese MM, Orlando P, Di Marzo V. Regulation of transient receptor potential channels of melastatin type 8 (TRPM8): effect of cAMP, cannabinoid CB(1) receptors and endovanilloids. Experimental Cell Research 2007, 313(9):1911-20. 10.1016/j.yexcr.2007.01.008, 17428469.
    • (2007) Experimental Cell Research , vol.313 , Issue.9 , pp. 1911-1920
    • De Petrocellis, L.1    Starowicz, K.2    Moriello, A.S.3    Vivese, M.M.4    Orlando, P.5    Di Marzo, V.6
  • 22
    • 0036874825 scopus 로고    scopus 로고
    • Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery
    • Kalvass JC, Maurer SM. Influence of nonspecific brain and plasma binding on CNS exposure: implications for rational drug discovery. Biopharmaceutics & Drug Disposition 2002, 23(8):327-338.
    • (2002) Biopharmaceutics & Drug Disposition , vol.23 , Issue.8 , pp. 327-338
    • Kalvass, J.C.1    Maurer, S.M.2
  • 23
    • 11144290156 scopus 로고    scopus 로고
    • Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice
    • 10.1124/dmd.104.001222, 15502010
    • Maurer TS, DeBartolo DB, Tess DA, Scott DO. Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug Metab Dispos 2005, 33:175-81. 10.1124/dmd.104.001222, 15502010.
    • (2005) Drug Metab Dispos , vol.33 , pp. 175-181
    • Maurer, T.S.1    DeBartolo, D.B.2    Tess, D.A.3    Scott, D.O.4
  • 25
    • 26044461277 scopus 로고    scopus 로고
    • Endocannabinoids in the regulation of appetite and body weight
    • 10.1097/00008877-200509000-00004, 16148436
    • Kirkham TC. Endocannabinoids in the regulation of appetite and body weight. Behav Pharmacol 2005, 16:297-313. 10.1097/00008877-200509000-00004, 16148436.
    • (2005) Behav Pharmacol , vol.16 , pp. 297-313
    • Kirkham, T.C.1
  • 27
    • 32644441249 scopus 로고    scopus 로고
    • Effect of rimonabant, a cannabinoid-1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients: RIO-North America: a randomized controlled trial
    • 10.1001/jama.295.7.761, 16478899
    • Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J. Effect of rimonabant, a cannabinoid-1 receptor blocker, on weight and cardiometabolic risk factors in overweight or obese patients: RIO-North America: a randomized controlled trial. JAMA 2006, 295:761-775. 10.1001/jama.295.7.761, 16478899.
    • (2006) JAMA , vol.295 , pp. 761-775
    • Pi-Sunyer, F.X.1    Aronne, L.J.2    Heshmati, H.M.3    Devin, J.4    Rosenstock, J.5
  • 28
    • 0035984946 scopus 로고    scopus 로고
    • Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2-arachidonoyl glycerol
    • 10.1038/sj.bjp.0704767, 1573386, 12055133
    • Kirkham TC, Williams CM, Fezza F, Di Marzo V. Endocannabinoid levels in rat limbic forebrain and hypothalamus in relation to fasting, feeding and satiation: stimulation of eating by 2-arachidonoyl glycerol. Br J Pharmacol 2002, 136:550-557. 10.1038/sj.bjp.0704767, 1573386, 12055133.
    • (2002) Br J Pharmacol , vol.136 , pp. 550-557
    • Kirkham, T.C.1    Williams, C.M.2    Fezza, F.3    Di Marzo, V.4
  • 29
    • 0032541111 scopus 로고    scopus 로고
    • Appetite suppression and weight loss after the cannabinoid antagonist SR141716
    • 10.1016/S0024-3205(98)00322-1, 9718088
    • Colombo G, Agabio R, Diaz G, Lobina C, Reali R, Gessa GL. Appetite suppression and weight loss after the cannabinoid antagonist SR141716. Life Sci 1998, 63(8):PL113-PL117. 10.1016/S0024-3205(98)00322-1, 9718088.
    • (1998) Life Sci , vol.63 , Issue.8
    • Colombo, G.1    Agabio, R.2    Diaz, G.3    Lobina, C.4    Reali, R.5    Gessa, G.L.6
  • 30
    • 0037304290 scopus 로고    scopus 로고
    • Keane, Peter, Maffrand, J-P, Soubrie, Philippe. Anti-obesity effect of SR-141716, a CB1 receptor antagonist, in diet-induced obese mice
    • Ravinet C, Arnone M, Delgorge C, Gonalons N. Keane, Peter, Maffrand, J-P, Soubrie, Philippe. Anti-obesity effect of SR-141716, a CB1 receptor antagonist, in diet-induced obese mice. Am J Physiol Regul Integr Comp Physiol 2003, 284(2):R345-353.
    • (2003) Am J Physiol Regul Integr Comp Physiol , vol.284 , Issue.2
    • Ravinet, C.1    Arnone, M.2    Delgorge, C.3    Gonalons, N.4
  • 31
    • 0038070321 scopus 로고    scopus 로고
    • Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats
    • Vickers SP, Webster LJ, Wyatt A, Dourish CT, Kennett GA. Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology 2003, 167(1):103-111.
    • (2003) Psychopharmacology , vol.167 , Issue.1 , pp. 103-111
    • Vickers, S.P.1    Webster, L.J.2    Wyatt, A.3    Dourish, C.T.4    Kennett, G.A.5
  • 32
    • 0037458690 scopus 로고    scopus 로고
    • Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice
    • 10.1016/S0014-2999(03)01343-8, 12591104
    • Hildebrandt AL, Kelly-Sullivan DM, Black SC. Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice. Eur J Pharmacol 2003, 462(1-3):125-132. 10.1016/S0014-2999(03)01343-8, 12591104.
    • (2003) Eur J Pharmacol , vol.462 , Issue.1-3 , pp. 125-132
    • Hildebrandt, A.L.1    Kelly-Sullivan, D.M.2    Black, S.C.3
  • 34
    • 58149138840 scopus 로고    scopus 로고
    • Should peripheral CB1 cannabinoid receptors be selectively targeted for therapeutic gain?
    • 10.1016/j.tips.2008.10.001, 2748782, 19042036
    • Kunos G, Osei-Hyiaman D, Bátkai S, Sharkey KA, Makriyannis A. Should peripheral CB1 cannabinoid receptors be selectively targeted for therapeutic gain?. Trends Pharmacol Sci 2009, 30(1):1-7. 10.1016/j.tips.2008.10.001, 2748782, 19042036.
    • (2009) Trends Pharmacol Sci , vol.30 , Issue.1 , pp. 1-7
    • Kunos, G.1    Osei-Hyiaman, D.2    Bátkai, S.3    Sharkey, K.A.4    Makriyannis, A.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.