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Volumn 15, Issue 11-12, 2010, Pages 411-415

How inverse can a neutral antagonist be? Strategic questions after the rimonabant issue

Author keywords

[No Author keywords available]

Indexed keywords

CANNABINOID 1 RECEPTOR; G PROTEIN COUPLED RECEPTOR; RIMONABANT;

EID: 77954814265     PISSN: 13596446     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.drudis.2010.04.004     Document Type: Short Survey
Times cited : (20)

References (31)
  • 1
    • 17144382751 scopus 로고    scopus 로고
    • Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study
    • Van Gaal L.F., et al. Effects of the cannabinoid-1 receptor blocker rimonabant on weight reduction and cardiovascular risk factors in overweight patients: 1-year experience from the RIO-Europe study. Lancet 2005, 365:1389-1397.
    • (2005) Lancet , vol.365 , pp. 1389-1397
    • Van Gaal, L.F.1
  • 2
    • 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
    • Pi-Sunyer F.X., et al. 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. J. Am. Med. Assoc. 2006, 295:761-775.
    • (2006) J. Am. Med. Assoc. , vol.295 , pp. 761-775
    • Pi-Sunyer, F.X.1
  • 3
    • 27844463517 scopus 로고    scopus 로고
    • Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia
    • Despres J.P., et al. Effects of rimonabant on metabolic risk factors in overweight patients with dyslipidemia. N. Engl. J. Med. 2005, 353:2121-2134.
    • (2005) N. Engl. J. Med. , vol.353 , pp. 2121-2134
    • Despres, J.P.1
  • 4
    • 33751001942 scopus 로고    scopus 로고
    • Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study
    • Scheen A.J., et al. Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study. Lancet 2006, 368:1660-1672.
    • (2006) Lancet , vol.368 , pp. 1660-1672
    • Scheen, A.J.1
  • 5
    • 36048995288 scopus 로고    scopus 로고
    • Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials
    • Christensen R., et al. Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials. Lancet 2007, 370:1706-1713.
    • (2007) Lancet , vol.370 , pp. 1706-1713
    • Christensen, R.1
  • 6
    • 36049006465 scopus 로고    scopus 로고
    • Depression and anxiety with rimonabant
    • Mitchell P.B., Morris M.J. Depression and anxiety with rimonabant. Lancet 2007, 370:1671-1672.
    • (2007) Lancet , vol.370 , pp. 1671-1672
    • Mitchell, P.B.1    Morris, M.J.2
  • 7
    • 40749089483 scopus 로고    scopus 로고
    • Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties
    • Bergman J., et al. Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties. Physiol. Behav. 2008, 93:666-670.
    • (2008) Physiol. Behav. , vol.93 , pp. 666-670
    • Bergman, J.1
  • 8
    • 57049102251 scopus 로고    scopus 로고
    • End of the line for cannabinoid receptor 1 as an anti-obesity target?
    • Jones D. End of the line for cannabinoid receptor 1 as an anti-obesity target?. Nat. Rev. Drug Discov. 2008, 7:961-962.
    • (2008) Nat. Rev. Drug Discov. , vol.7 , pp. 961-962
    • Jones, D.1
  • 9
    • 33846026023 scopus 로고    scopus 로고
    • Assessing receptor affinity for inverse agonists: Schild and Cheng-Prusoff methods revisited
    • Giraldo J., et al. Assessing receptor affinity for inverse agonists: Schild and Cheng-Prusoff methods revisited. Curr. Drug Targets 2007, 8:197-202.
    • (2007) Curr. Drug Targets , vol.8 , pp. 197-202
    • Giraldo, J.1
  • 10
    • 0001169515 scopus 로고
    • Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins
    • Costa T., Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. U.S.A. 1989, 86:7321-7325.
    • (1989) Proc. Natl. Acad. Sci. U.S.A. , vol.86 , pp. 7321-7325
    • Costa, T.1    Herz, A.2
  • 11
    • 1642495639 scopus 로고    scopus 로고
    • Efficacy as a vector: the relative prevalence and paucity of inverse agonism
    • Kenakin T. Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol. Pharmacol. 2004, 65:2-11.
    • (2004) Mol. Pharmacol. , vol.65 , pp. 2-11
    • Kenakin, T.1
  • 12
    • 34347336422 scopus 로고    scopus 로고
    • Cannabinoid CB1 receptor inverse agonists and neutral antagonists: effects on food intake, food-reinforced behavior and food aversions
    • Salamone J.D., et al. Cannabinoid CB1 receptor inverse agonists and neutral antagonists: effects on food intake, food-reinforced behavior and food aversions. Physiol. Behav. 2007, 91:383-388.
    • (2007) Physiol. Behav. , vol.91 , pp. 383-388
    • Salamone, J.D.1
  • 13
    • 54849141400 scopus 로고    scopus 로고
    • Play an ADAGIO with a STRADIVARIUS: the right patient for CB1 receptor antagonists?
    • Di Marzo V. Play an ADAGIO with a STRADIVARIUS: the right patient for CB1 receptor antagonists?. Nat. Clin. Pract. Cardiovasc. Med. 2008, 5:610-612.
    • (2008) Nat. Clin. Pract. Cardiovasc. Med. , vol.5 , pp. 610-612
    • Di Marzo, V.1
  • 14
    • 70350347327 scopus 로고    scopus 로고
    • CB1 antagonists for obesity-what lessons have we learned from rimonabant?
    • Di Marzo V., Despres J.P. CB1 antagonists for obesity-what lessons have we learned from rimonabant?. Nat. Rev. Endocrinol. 2009, 5:633-638.
    • (2009) Nat. Rev. Endocrinol. , vol.5 , pp. 633-638
    • Di Marzo, V.1    Despres, J.P.2
  • 15
    • 70349128141 scopus 로고    scopus 로고
    • Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions
    • Fong T.M., Heymsfield S.B. Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions. Int. J. Obes. (Lond.) 2009, 33:947-955.
    • (2009) Int. J. Obes. (Lond.) , vol.33 , pp. 947-955
    • Fong, T.M.1    Heymsfield, S.B.2
  • 16
    • 58149138840 scopus 로고    scopus 로고
    • Should peripheral CB(1) cannabinoid receptors be selectively targeted for therapeutic gain?
    • Kunos G., et al. Should peripheral CB(1) cannabinoid receptors be selectively targeted for therapeutic gain?. Trends Pharmacol. Sci. 2009, 30:1-7.
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 1-7
    • Kunos, G.1
  • 17
    • 48149101434 scopus 로고    scopus 로고
    • The endocannabinoid system in obesity and type 2 diabetes
    • Di Marzo V. The endocannabinoid system in obesity and type 2 diabetes. Diabetologia 2008, 51:1356-1367.
    • (2008) Diabetologia , vol.51 , pp. 1356-1367
    • Di Marzo, V.1
  • 18
    • 75749126604 scopus 로고    scopus 로고
    • Signal transduction of the CB1 cannabinoid receptor
    • Turu G., Hunyady L. Signal transduction of the CB1 cannabinoid receptor. J. Mol. Endocrinol. 2010, 44:75-85.
    • (2010) J. Mol. Endocrinol. , vol.44 , pp. 75-85
    • Turu, G.1    Hunyady, L.2
  • 19
    • 68949209293 scopus 로고    scopus 로고
    • The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as anti-obesity agents
    • Lee H.K., et al. The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as anti-obesity agents. Curr. Top. Med. Chem. 2009, 9:482-503.
    • (2009) Curr. Top. Med. Chem. , vol.9 , pp. 482-503
    • Lee, H.K.1
  • 20
    • 24044539957 scopus 로고    scopus 로고
    • Allosteric modulation of the cannabinoid CB1 receptor
    • Price M.R., et al. Allosteric modulation of the cannabinoid CB1 receptor. Mol. Pharmacol. 2005, 68:1484-1495.
    • (2005) Mol. Pharmacol. , vol.68 , pp. 1484-1495
    • Price, M.R.1
  • 21
    • 33745127060 scopus 로고    scopus 로고
    • The two-state dimer receptor model: a general model for receptor dimers
    • Franco R., et al. The two-state dimer receptor model: a general model for receptor dimers. Mol. Pharmacol. 2006, 69:1905-1912.
    • (2006) Mol. Pharmacol. , vol.69 , pp. 1905-1912
    • Franco, R.1
  • 22
    • 73049085563 scopus 로고    scopus 로고
    • The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways
    • Rovira X., et al. The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways. Trends Pharmacol. Sci. 2010, 31:15-21.
    • (2010) Trends Pharmacol. Sci. , vol.31 , pp. 15-21
    • Rovira, X.1
  • 23
    • 36148944785 scopus 로고    scopus 로고
    • When a G protein-coupled receptor does not couple to a G protein
    • Sun Y., et al. When a G protein-coupled receptor does not couple to a G protein. Mol. Biosyst. 2007, 3:849-854.
    • (2007) Mol. Biosyst. , vol.3 , pp. 849-854
    • Sun, Y.1
  • 24
    • 66849093630 scopus 로고    scopus 로고
    • Evidence for distinct antagonist-revealed functional states of 5-hydroxytryptamine(2A) receptor homodimers
    • Brea J., et al. Evidence for distinct antagonist-revealed functional states of 5-hydroxytryptamine(2A) receptor homodimers. Mol. Pharmacol. 2009, 75:1380-1391.
    • (2009) Mol. Pharmacol. , vol.75 , pp. 1380-1391
    • Brea, J.1
  • 25
    • 69649097791 scopus 로고    scopus 로고
    • '7TM receptor allostery: putting numbers to shapeshifting proteins
    • Kenakin T.P. '7TM receptor allostery: putting numbers to shapeshifting proteins. Trends Pharmacol. Sci. 2009, 30:460-469.
    • (2009) Trends Pharmacol. Sci. , vol.30 , pp. 460-469
    • Kenakin, T.P.1
  • 26
    • 68249113457 scopus 로고    scopus 로고
    • Cellular assays as portals to seven-transmembrane receptor-based drug discovery
    • Kenakin T.P. Cellular assays as portals to seven-transmembrane receptor-based drug discovery. Nat. Rev. Drug Discov. 2009, 8:617-626.
    • (2009) Nat. Rev. Drug Discov. , vol.8 , pp. 617-626
    • Kenakin, T.P.1
  • 27
    • 0028950255 scopus 로고
    • The two-state model of receptor activation
    • Leff P. The two-state model of receptor activation. Trends Pharmacol. Sci. 1995, 16:89-97.
    • (1995) Trends Pharmacol. Sci. , vol.16 , pp. 89-97
    • Leff, P.1
  • 28
    • 55849117700 scopus 로고    scopus 로고
    • CB(1) receptor antagonism: biological basis for metabolic effects
    • Di Marzo V. CB(1) receptor antagonism: biological basis for metabolic effects. Drug Discov. Today 2008, 13:1026-1041.
    • (2008) Drug Discov. Today , vol.13 , pp. 1026-1041
    • Di Marzo, V.1
  • 29
    • 77649234756 scopus 로고    scopus 로고
    • How to improve R&D productivity: the pharmaceutical industry's grand challenge
    • Paul S.M., et al. How to improve R&D productivity: the pharmaceutical industry's grand challenge. Nat. Rev. Drug Discov. 2010, 9:203-214.
    • (2010) Nat. Rev. Drug Discov. , vol.9 , pp. 203-214
    • Paul, S.M.1
  • 30
    • 0347985770 scopus 로고    scopus 로고
    • Agonist induction, conformational selection, and mutant receptors
    • Giraldo J. Agonist induction, conformational selection, and mutant receptors. FEBS Lett. 2004, 556:13-18.
    • (2004) FEBS Lett. , vol.556 , pp. 13-18
    • Giraldo, J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.