Thienorphine is a potent long-acting partial opioid agonist: A comparative study with buprenorphine

Journal of Pharmacology and Experimental Therapeutics

Volumn 318, Issue 1, 2006, Pages 282-287

  Yu, Gang ^a   Yue, Yong Juan ^a   Cui, Meng Xun ^a   Gong, Ze Hui ^a  

^a BEIJING INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

BUPRENORPHINE; DELTA OPIATE RECEPTOR; DIPRENORPHINE; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); KAPPA OPIATE RECEPTOR; LONG ACTING DRUG; MORPHINE; MU OPIATE RECEPTOR; OPIATE AGONIST; PARTIAL AGONIST; THIENORPHINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; CHO CELL; COMPARATIVE STUDY; CONTROLLED STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG EFFICACY; DRUG INHIBITION; DRUG POTENCY; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; FEMALE; IN VITRO STUDY; IN VIVO STUDY; LETHALITY; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION;

ANALGESICS, OPIOID; ANIMALS; BUPRENORPHINE; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; MICE; PAIN MEASUREMENT; PROTEIN BINDING; RATS; RECEPTORS, OPIOID; TIME FACTORS;

EID: 33745288804     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.105.099937     Document Type: Article

References (28)

1. Amass L, Bickel WK, Crean JP, Blake J, and Higgins ST (1998) Alternate-day buprenorphine dosing is preferred to daily dosing by opioid-dependent humans. Psychopharmacology 136:217-225.
2. Bartus RT, Emerich DF, Hotz J, Blaustein M, Dean RL, Perdomo B, and Basile AS (2003) Vivitrexs, an injectable, extended-release formulation of naltrexone, provides pharmacokinetic and pharmacodynamic evidence of efficacy for 1 month in rats. Neuropsychopharmacology 28:1973-1982.
3. Bliss CI (1967) Statistics in Biology. McGraw-Hill Book Company, New York.
4. Carreno JE, Alvarez CE, Narciso GI, Bascaran MT, Diaz M, and Bobes J (2003) Maintenance treatment with depot opioid antagonists in subcutaneous implants: an alternative in the treatment of opioid dependence. Addict Biol 8:429-438.
5. Comer SD, Collins ED, Kleber HD, Nuwayser ES, Kerrigan JH, and Fischman MW (2002) Depot naltrexone: long-lasting antagonism of the effects of heroin in humans. Psychopharmacology 159:351-360.
6. Cowan A, Lewis JW, and McFarlane IR (1977) Agonist and antagonist properties of buprenorphine, a new antinociceptive agent. Br J Pharmacol 60:537-545.
7. Davids E and Gastpar M (2004) Buprenorphine in the treatment of opioid dependence. Eur Neuropsychopharmacol 14:209-216.
8. Dum JE and Herz A (1981) In vivo receptor binding of the opiate partial agonist, buprenorphine, correlated with its agonistic and antagonistic actions. Br J Pharmacol 74:627-633.
9. Eddy NB and Leimbach D (1953) Synthetic analgesics. II. Dithienylbutenyl- and dithienylbutylamines. J Pharmacol Exp Ther 107:385-393.
10. Fudala PJ, Jaffe JH, Dax EM, and Johnson RE (1990) Use of buprenorphine in the treatment of opioid addiction. II. Physiologic and behavioral effects of daily and alternate-day administration and abrupt withdrawal. Clin Pharmacol Ther 47:525-534.
11. Heel RC, Brogden RN, Speight TM, and Avery GS (1979) Buprenorphine: a review of its pharmacological properties and therapeutic efficacy. Drugs 17:81-110.
12. Husbands SM, Neilan CL, Broadbear J, Grundt P, Breeden S, Aceto MD, Woods JH, Lewis JW, and Traynor JR (2005) BU74, a complex oripavine derivative with potent kappa opioid receptor agonism and delayed opioid antagonism. Eur J Pharmacol 509:117-125.
13. Johnson RE, Strain EC, and Amass L (2003) Buprenorphine: how to use it right. Drug Alcohol Depend 70:S59-S77.
14. Kreek MJ (1992) Rationale for maintenance pharmacotherapy of opiate dependence, in Addictive States (O'Brien CP and Jaffe JH eds) pp. 205-230, Raven Press, New York.
15. Kreek MJ (1996) Opiates, opioids and addiction. Mol Psychiatry 1:232-254.
16. Kreek MJ and Vocci FJ (2002) History and current status of opioid maintenance treatments: blending conference session. J Subst Abuse Treat 23:93-105.
17. Lewis JW (1985) Buprenorphine. Drug Alcohol Depend 14:363-372.
18. Li J, Huang P, Chen CG, Riel K, Weinstein H, and Liu-Chen LY (2001) Constitutive activation of the μ opioid receptor by mutation of D3.49(164), but not D3.32(147): D3.49(164) is critical for stabilization of the inactive form of the receptor and for its expression. Biochemistry 40:12039-12050.
19. Liu CH, Liu H, Han XY, Wu B, Zhong BH, and Gong ZH (2005) Synthesis and characterization of thienorphine and its glucuronide conjugate. Synth Commun 35:701-710.
20. Lopatko OV, White JM, Huber A, and Ling W (2003) Opioid effects and opioid withdrawal during a 24 h dosing interval inpatients maintained on buprenorphine. Drug Alcohol Depend 69:317-322.
21. Mendelson J, Upton RA, Everhart ET, Jacob P III, and Jones RT (1997) Bioavailability of sublingual buprenorphine. J Clin Pharmcol 37:31-37.
22. Negus SS, Picker MJ, and Dykstra LA (1989) Kappa antagonist properties of buprenorphine in non-tolerant and morphine-tolerant rats. Psychopharmacology 98:141-143.
23. Neilan CL, Husbands SM, Breeden S, Ko MC, Aceto MD, Lewis JW, Woods JH, and Traynor JR (2004) Characterization of the complex morphinan derivative BU72 as a high efficacy, long-lasting mu-opioid receptor agonist. Eur J Pharmacol 499:107-116.
24. Schuh KJ and Johanson CE (1999) Pharmacokinetic comparison of the buprenorphine sublingual liquid and tablet. Drug Alcohol Depend 56:55-60.
25. Sobel BF, Sigmon SC, Walsh SL, Johnson RE, Liebson IA, Nuwayser ES, Kerrigan JH, and Bigelow GE (2004) Open-label trial of an injection depot formulation of buprenorphine in opioid detoxification. Drug Alcohol Depend 73:11-22.
26. Walsh SL, Preston KL, Bigelow GE, and Stitzer MD (1995) Acute administration of buprenorphine in humans: partial agonist and blockage effects. J Pharmacol Exp Ther 274:361-372.
27. Walsh SL, Preston KL, Stitzer MD, Cone EJ, and Bigelow GE (1994) Clinical pharmacology of buprenorphine: ceiling effects as high doses. Clin Pharmacol Ther 55:569-580.
28. Zhao WL, Gong ZH, and Liang JH (2004) A new buprenorphine analogy, thienorphine, inhibits morphine-induced behavioral sensitization in mice. Acta Pharmacol Sin 25:1413-1418.