메뉴 건너뛰기




Volumn 155, Issue 9, 2014, Pages 1829-1835

Biased agonism of the l-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

Author keywords

Biased ligand; Clinical trial; Morphine; Mu Opioid receptor; Postoperative pain

Indexed keywords

ANALGESIC AGENT; MORPHINE; MORPHINE 6 GLUCURONIDE; MU OPIATE RECEPTOR AGONIST; PLACEBO; TRV 130; UNCLASSIFIED DRUG; ((3-METHOXYTHIOPHEN-2-YL)METHYL)((2-(9-(PYRIDIN-2-YL)-6-OXASPIRO(4.5)DECAN-9-YL)ETHYL))AMINE; NARCOTIC ANALGESIC AGENT; SPIRO COMPOUND; THIOPHENE DERIVATIVE;

EID: 84926407374     PISSN: 03043959     EISSN: 18726623     Source Type: Journal    
DOI: 10.1016/j.pain.2014.06.011     Document Type: Article
Times cited : (229)

References (33)
  • 2
    • 0041846747 scopus 로고    scopus 로고
    • Postoperative pain experience: Results from a national survey suggest postoperative pain continues to be undermanaged
    • Apfelbaum JL, Chen C, Mehta SS, Gan TJ. Postoperative pain experience: results from a national survey suggest postoperative pain continues to be undermanaged. Anesth Analg 2003;97:534-40.
    • (2003) Anesth Analg , vol.97 , pp. 534-540
    • Apfelbaum, J.L.1    Chen, C.2    Mehta, S.S.3    Gan, T.J.4
  • 5
    • 84886532899 scopus 로고    scopus 로고
    • Structure-activity relationships and discovery of a G protein biased mu opioid receptor ligand (3-methoxythiophen-2-yl)methyl ({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4 5] decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain
    • Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS. Structure-activity relationships and discovery of a G protein biased mu opioid receptor ligand (3-methoxythiophen-2-yl)methyl ({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5] decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. J Med Chem 2013;56(20):8019-31.
    • (2013) J Med Chem , vol.56 , Issue.20 , pp. 8019-8031
    • Chen, X.T.1    Pitis, P.2    Liu, G.3    Yuan, C.4    Gotchev, D.5    Cowan, C.L.6    Rominger, D.H.7    Koblish, M.8    Dewire, S.M.9    Crombie, A.L.10    Violin, J.D.11    Yamashita, D.S.12
  • 6
    • 0037301393 scopus 로고    scopus 로고
    • Buprenorphine: New pharmacological aspects
    • discussion 23-24
    • Cowan A. Buprenorphine: new pharmacological aspects. Int J Clin Pract Suppl 2003:3-8. discussion 23-24.
    • (2003) Int J Clin Pract Suppl , pp. 3-8
    • Cowan, A.1
  • 9
    • 0021839098 scopus 로고
    • A modified cold stimulation technique for the evaluation of analgesic activity in human volunteers
    • Garcia de Jalon PD, Harrison FJ, Johnson KI, Kozma C, Schnelle K. A modified cold stimulation technique for the evaluation of analgesic activity in human volunteers. PAIN 1985;22:183-9.
    • (1985) PAIN , vol.22 , pp. 183-189
    • Garcia De Jalon, P.D.1    Harrison, F.J.2    Johnson, K.I.3    Kozma, C.4    Schnelle, K.5
  • 10
    • 0036781281 scopus 로고    scopus 로고
    • Molecular mechanisms of analgesia induced by opioids and ethanol: Is the GIRK channel one of the keys
    • Ikeda K, Kobayashi T, Kumanishi T, Yano R, Sora I, Niki H. Molecular mechanisms of analgesia induced by opioids and ethanol: Is the GIRK channel one of the keys? Neurosci Res 2002;44:121-31.
    • (2002) Neurosci Res , vol.44 , pp. 121-131
    • Ikeda, K.1    Kobayashi, T.2    Kumanishi, T.3    Yano, R.4    Sora, I.5    Niki, H.6
  • 12
    • 36348946976 scopus 로고    scopus 로고
    • Functional selectivity through protean and biased agonism: Who steers the ship
    • Kenakin T. Functional selectivity through protean and biased agonism: Who steers the ship? Mol Pharmacol 2007;72:1393-401.
    • (2007) Mol Pharmacol , vol.72 , pp. 1393-1401
    • Kenakin, T.1
  • 13
    • 0033013383 scopus 로고    scopus 로고
    • Opioids: First lessons from knockout mice
    • Kieffer BL. Opioids: First lessons from knockout mice. Trends Pharmacol Sci 1999;20:19-26.
    • (1999) Trends Pharmacol Sci , vol.20 , pp. 19-26
    • Kieffer, B.L.1
  • 14
    • 33751307912 scopus 로고    scopus 로고
    • Differential sensitivity of three experimental pain models in detecting the analgesic effects of transdermal fentanyl and buprenorphine
    • Koltzenburg M, Pokorny R, Gasser UE, Richarz U. Differential sensitivity of three experimental pain models in detecting the analgesic effects of transdermal fentanyl and buprenorphine. PAIN 2006;126:165-74.
    • (2006) PAIN , vol.126 , pp. 165-174
    • Koltzenburg, M.1    Pokorny, R.2    Gasser, U.E.3    Richarz, U.4
  • 15
    • 63449097594 scopus 로고    scopus 로고
    • Improvement of morphinemediated analgesia by inhibition of beta-arrestin 2 expression in mice periaqueductal gray matter
    • Li Y, Liu X, Liu C, Kang J, Yang J, Pei G, Wu C. Improvement of morphinemediated analgesia by inhibition of beta-arrestin 2 expression in mice periaqueductal gray matter. Int J Mol Sci 2009;10:954-63.
    • (2009) Int J Mol Sci , vol.10 , pp. 954-963
    • Li, Y.1    Liu, X.2    Liu, C.3    Kang, J.4    Yang, J.5    Pei, G.6    Wu, C.7
  • 19
    • 33846006524 scopus 로고    scopus 로고
    • The partial 5-hydroxytryptamine1A receptor agonist buspirone does not antagonize morphine-induced respiratory depression in humans
    • Oertel BG, Schneider A, Rohrbacher M, Schmidt H, Tegeder I, Geisslinger G, Lotsch J. The partial 5-hydroxytryptamine1A receptor agonist buspirone does not antagonize morphine-induced respiratory depression in humans. Clin Pharmacol Ther 2007;81:59-68.
    • (2007) Clin Pharmacol Ther , vol.81 , pp. 59-68
    • Oertel, B.G.1    Schneider, A.2    Rohrbacher, M.3    Schmidt, H.4    Tegeder, I.5    Geisslinger, G.6    Lotsch, J.7
  • 20
    • 84864602546 scopus 로고    scopus 로고
    • Relationship between potential opioid-related adverse effects and hospital length of stay in patients receiving opioids after orthopedic surgery
    • Pizzi LT, Toner R, Foley K, Thomson E, Chow W, Kim M, Couto J, Royo M, Viscusi E. Relationship between potential opioid-related adverse effects and hospital length of stay in patients receiving opioids after orthopedic surgery. Pharmacotherapy 2012;32:502-14.
    • (2012) Pharmacotherapy , vol.32 , pp. 502-514
    • Pizzi, L.T.1    Toner, R.2    Foley, K.3    Thomson, E.4    Chow, W.5    Kim, M.6    Couto, J.7    Royo, M.8    Viscusi, E.9
  • 21
    • 23944485741 scopus 로고    scopus 로고
    • Morphine side effects in beta-arrestin 2 knockout mice
    • Raehal KM, Walker JK, Bohn LM. Morphine side effects in beta-arrestin 2 knockout mice. J Pharmacol Exp Ther 2005;314:1195-201.
    • (2005) J Pharmacol Exp Ther , vol.314 , pp. 1195-1201
    • Raehal, K.M.1    Walker, J.K.2    Bohn, L.M.3
  • 22
    • 0016233155 scopus 로고
    • A clinical method for assessing the ventilatory response to hypoxia
    • Rebuck AS, Campbell EJ. A clinical method for assessing the ventilatory response to hypoxia. Am Rev Respir Dis 1974;109:345-50.
    • (1974) Am Rev Respir Dis , vol.109 , pp. 345-350
    • Rebuck, A.S.1    Campbell, E.J.2
  • 23
    • 77956056189 scopus 로고    scopus 로고
    • Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain
    • Schroder W, Vry JD, Tzschentke TM, Jahnel U, Christoph T. Differential contribution of opioid and noradrenergic mechanisms of tapentadol in rat models of nociceptive and neuropathic pain. Eur J Pain 2010;14:814-21.
    • (2010) Eur J Pain , vol.14 , pp. 814-821
    • Schroder, W.1    Vry, J.D.2    Tzschentke, T.M.3    Jahnel, U.4    Christoph, T.5
  • 24
    • 27744457116 scopus 로고    scopus 로고
    • The frequency and timing of respiratory depression in 1524 postoperative patients treated with systemic or neuraxial morphine
    • Shapiro A, Zohar E, Zaslansky R, Hoppenstein D, Shabat S, Fredman B. The frequency and timing of respiratory depression in 1524 postoperative patients treated with systemic or neuraxial morphine. J Clin Anesth 2005;17:537-42.
    • (2005) J Clin Anesth , vol.17 , pp. 537-542
    • Shapiro, A.1    Zohar, E.2    Zaslansky, R.3    Hoppenstein, D.4    Shabat, S.5    Fredman, B.6
  • 26
    • 4944240062 scopus 로고    scopus 로고
    • Experimental human pain models: A review of standardised methods for preclinical testing of analgesics
    • Staahl C, Drewes AM. Experimental human pain models: A review of standardised methods for preclinical testing of analgesics. Basic Clin Pharmacol Toxicol 2004;95:97-111.
    • (2004) Basic Clin Pharmacol Toxicol , vol.95 , pp. 97-111
    • Staahl, C.1    Drewes, A.M.2
  • 30
    • 34447649922 scopus 로고    scopus 로고
    • Beta-arrestin-biased ligands at seven-transmembrane receptors
    • Violin JD, Lefkowitz RJ. Beta-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol Sci 2007;28:416-22.
    • (2007) Trends Pharmacol Sci , vol.28 , pp. 416-422
    • Violin, J.D.1    Lefkowitz, R.J.2
  • 31
    • 0016859569 scopus 로고
    • Diminished ventilatory response to hypoxia and hypercapnia after morphine in normal man
    • Weil JV, McCullough RE, Kline JS, Sodal IE. Diminished ventilatory response to hypoxia and hypercapnia after morphine in normal man. N Engl J Med 1975;292:1103-6.
    • (1975) N Engl J Med , vol.292 , pp. 1103-1106
    • Weil, J.V.1    McCullough, R.E.2    Kline, J.S.3    Sodal, I.E.4
  • 32
    • 0036086324 scopus 로고    scopus 로고
    • Adverse events associated with postoperative opioid analgesia: A systematic review
    • Wheeler M, Oderda GM, Ashburn MA, Lipman AG. Adverse events associated with postoperative opioid analgesia: a systematic review. J Pain 2002;3:159-80.
    • (2002) J Pain , vol.3 , pp. 159-180
    • Wheeler, M.1    Oderda, G.M.2    Ashburn, M.A.3    Lipman, A.G.4
  • 33
    • 0001128427 scopus 로고
    • Studies on Pain. Observations on pain due to local cooling and on factors involved in the ''cold pressor'' effect
    • Wolf S, Hardy JD. Studies on Pain. Observations on pain due to local cooling and on factors involved in the ''cold pressor'' effect. J Clin Invest 1941;20:521-33.
    • (1941) J Clin Invest , vol.20 , pp. 521-533
    • Wolf, S.1    Hardy, J.D.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.