TH-030418: A potent long-acting opioid analgesic with low dependence liability

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 384, Issue 2, 2011, Pages 125-131

  Yu, Gang ^a   Yan, Ling Di ^a   Li, Yu Lei ^a   Wen, Quan ^a   Dong, Hua Jin ^a   Gong, Ze Hui ^a  

^a BEIJING INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY   (China)

Author keywords

Dependence; Long acting opioid analgesic; ORL1; TH 030418; Thienorphine

Indexed keywords

[7 ALPHA [1 HYDROXY 1 METHYL 3 (THIEN 3 YL)PROPYL] 6,14 ENDO ETHANOTETRAHYDROORIPAVINE]; ACETIC ACID; DELTA OPIATE RECEPTOR; DIHYDROETORPHINE; KAPPA OPIATE RECEPTOR; MORPHINE; MORPHINE DERIVATIVE; MU OPIATE RECEPTOR; NALOXONE; NARCOTIC ANALGESIC AGENT; OPIATE RECEPTOR; OPIOID RECEPTOR LIKE 1; TH 030418; THIENORPHINE; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANIMAL CELL; ANIMAL CELL CULTURE; ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; CHINESE HAMSTER; CONTROLLED STUDY; DRUG DOSE INCREASE; DRUG POTENCY; DRUG STRUCTURE; FEMALE; HOT PLATE TEST; MALE; MOUSE; NONHUMAN; OVARY CELL; PLACE PREFERENCE; RADIOASSAY; WRITHING TEST;

ANALGESICS, OPIOID; ANIMALS; BEHAVIOR, ANIMAL; CELL CULTURE TECHNIQUES; CHO CELLS; CONDITIONING, CLASSICAL; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; ETORPHINE; FEMALE; INJECTIONS, SUBCUTANEOUS; LIGANDS; MALE; MICE; MICE, INBRED STRAINS; MOLECULAR STRUCTURE; OPIOID-RELATED DISORDERS; PAIN; PROTEIN BINDING; RADIOLIGAND ASSAY; RECEPTORS, OPIOID; TIME FACTORS; TRANSFECTION;

EID: 79961173347     PISSN: 00281298     EISSN: 14321912     Source Type: Journal    
DOI: 10.1007/s00210-011-0652-8     Document Type: Article

References (25)

1. MT Bardo JK Rowlett MJ Harris 1995 Conditioned place preference using opiate and stimulant drugs: a meta-analysis Neurosci Biobehav Rev 19 39 51 7770196 10.1016/0149-7634(94)00021-R 1:CAS:528:DyaK2MXktl2jsr0%3D
2. KW Bentley DG Hardy 1967 Novel analgesics and molecular rearrangements in the morphine-thebaine group. III. Alcohols of the 6,14-endo- ethenotetrahydrooripavine series and derived analogs of N-allylnormorphine and -norcodeine J Am Chem Soc 89 3281 3292 6042764 10.1021/ja00989a032 1:CAS:528:DyaF2sXks1Cmurg%3D
3. C Contet BL Kieffer K Befort 2004 Mu opioid receptor: a gateway to drug addiction Curr Opin Neurobiol 14 370 378 15194118 10.1016/j.conb.2004.05.005 1:CAS:528:DC%2BD2cXkvV2ns74%3D (Pubitemid 38759868)
4. MP Davis D Walsh R Lagman SB LeGrand 2005 Controversies in pharmacotherapy of pain management Lancet Oncol 6 696 704 16129370 10.1016/S1470-2045(05)70317-X 1:CAS:528:DC%2BD2MXpslynsrs%3D (Pubitemid 41222760)
5. Ellison NM (1993) Opioid analgesics for cancer pain: toxicities and their treatments. In: Patt RB (ed) cancer pain. Lippincott, Philadelphia, pp 185-194
6. M Huang BY Qin 1982 Physical dependence of dihydroetorphine in mice and monkeys Acta Pharmacol Sin 3 81 84 1:CAS:528:DyaL38XltVekt7g%3D (Pubitemid 12059905)
7. TV Khroyan NT Zaveri WE Polgar J Orduna C Olsen F Jiang L Toll 2007 SR 16435 [1-(1-(bicyclo[3.3.1]nonan-9-yl)piperidin-4-yl)indolin-2-one], a novel mixed nociceptin/orphanin FQ/mu-opioid receptor partial agonist: analgesic and rewarding properties in mice J Pharmacol Exp Ther 320 934 943 17132815 10.1124/jpet.106.111997 1:CAS:528:DC%2BD2sXhs1WrsLo%3D (Pubitemid 46147978)
8. R Lattanzi L Negri E Giannini H Schmidhammer J Schutz G Improta 2001 HS-599: a novel long acting opioid analgesic does not induce place-preference in rats Br J Pharmacol 134 441 447 11564664 10.1038/sj.bjp.0704280 1:CAS:528:DC%2BD3MXnsV2gsrc%3D (Pubitemid 32989143)
9. JW Lewis KW Bentley A Cowan 1971 Narcotic analgesics and antagonists Annu Rev Pharmacol 11 241 270 4948499 10.1146/annurev.pa.11.040171.001325 1:STN:280:DyaE383gslOmsA%3D%3D
10. JX Li GL Becker JR Traynor ZH Gong CP France 2007 Thienorphine: receptor binding and behavioral effects in rhesus monkeys J Pharmacol Exp Ther 321 227 236 17220427 10.1124/jpet.106.113290 1:CAS:528:DC%2BD2sXktVSksbY%3D (Pubitemid 46456954)
11. CH Liu H Liu XY Han B Wu BH Zhong ZH Gong 2005 Synthesis and characterization of thienorphine and its glucuronide conjugate Synth Commun 35 701 710 10.1081/SCC-200050367 1:CAS:528:DC%2BD2MXivFGjt74%3D (Pubitemid 40389511)
12. TJ Martin SA Kim LS Harris JE Smith 1997 Potent reinforcing effects of dihydroetorphine in rats Eur J Pharmacol 324 141 145 9145764 10.1016/S0014-2999(97)00074-5 1:CAS:528:DyaK2sXisVemt7Y%3D (Pubitemid 27174598)
13. HW Matthes R Maldonado F Simonin O Valverde S Slowe I Kitchen K Befort A Dierich M Le Meur P Dolle, et al. 1996 Loss of morphine-induced analgesia, reward effect and withdrawal symptoms in mice lacking the mu-opioid-receptor gene Nature 383 819 823 8893006 10.1038/383819a0 1:CAS:528:DyaK28Xms1Sjtbw%3D
14. Maul C, Buschmann H, Sundermann B (2002) Synthetic opioids. In: Buschmann H, Christoph T, Friderichs E, Maul C, Sundermann B (eds) Analgesics: from chemistry and pharmacology to clinical application. Wiley-VCH, Weinheim, pp 159-169
15. NP Murphy Y Lee NT Maidment 1999 Orphanin FQ/nociceptin blocks acquisition of morphine place preference Brain Res 832 168 170 10375664 10.1016/S0006-8993(99)01425-0 1:CAS:528:DyaK1MXjs1SjsLw%3D (Pubitemid 29336175)
16. S Ohmori L Fang M Kawase S Saito Y Morimoto 2001 Tolerance to analgesia and dependence liability by topical application of dihydroetorphine Eur J Pharmacol 423 157 166 11448480 10.1016/S0014-2999(01)01098-6 1:CAS:528:DC%2BD3MXltVGjs70%3D (Pubitemid 32614153)
17. S Ohmori T Hayashi M Kawase S Saito Y Morimoto 2001 Pharmacokinetic and pharmacodynamic evaluations of a potent analgesic dihydroetorphine in hairless rats J Pharmacol Exp Ther 296 528 536 11160640 1:CAS:528:DC%2BD3MXoslejtA%3D%3D (Pubitemid 32112482)
18. JR Shoblock J Wichmann NT Maidment 2005 The effect of a systemically active ORL-1 agonist, Ro 64-6198, on the acquisition, expression, extinction, and reinstatement of morphine conditioned place preference Neuropharmacology 49 439 446 15919100 10.1016/j.neuropharm.2005.04.008 1:CAS:528:DC%2BD2MXosVCrt78%3D (Pubitemid 41169968)
19. S Tokuyama M Takahashi H Kaneto 1993 Antinociceptive effect of dihydroetorphine and its tolerance/dependence liability in mice Biol Pharm Bull 16 774 777 8220323 1:CAS:528:DyaK2cXpsFGhtA%3D%3D (Pubitemid 23288168)
20. S Tokuyama F Nakamura M Takahashi H Kaneto 1996 Antinociceptive effect of dihydroetorphine following various routes of administration: a comparative study with morphine Biol Pharm Bull 19 477 479 8924922 1:CAS:528: DyaK28XhvV2qtLY%3D (Pubitemid 26099907)
21. DX Wang XQ Lu BY Qin 1995 Dihydroetorphine is a μ-receptor-selective ligand J Pharm Pharmacol 47 669 673 8583370 10.1111/j.2042-7158.1995.tb05857.x 1:CAS:528:DyaK2MXotlWls7Y%3D
22. G Yu YJ Yue MX Cui ZH Gong 2006 Thienorphine is a potent long-acting partial opioid agonist: a comparative study with buprenorphine J Pharmacol Exp Ther 318 282 287 16569757 10.1124/jpet.105.099937 1:CAS:528:DC%2BD28XmsFymt7w%3D
23. NT Zaveri F Jiang CM Olsen JR Deschamps D Parrish W Polgar L Toll 2004 A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor J Med Chem 47 2973 2976 15163178 10.1021/jm034249d 1:CAS:528:DC%2BD2cXjs1Sjs7s%3D (Pubitemid 38702693)
24. WL Zhao ZH Gong JH Liang 2004 A new buprenorphine analogy, thienorphine, inhibits morphine-induced behavioral sensitization in mice Acta Pharmacol Sin 25 1413 1418 15525461 1:CAS:528:DC%2BD2cXpvVCjtrs%3D
25. 35S]GTPγS binding to membranes: determination of potencies and efficacies of ligands J Pharmacol Exp Ther 282 676 684 9262330 1:CAS:528:DyaK2sXltlSnt7c%3D (Pubitemid 27340167)