Studies of tolerance and dependence with the delta-opioid agonist SNC80 in rhesus monkeys responding under a schedule of food presentation.
作者： K C Rice , S S Negus , M S Furness , M R Brandt , B D Fischer
DOI:
关键词:
摘要: Tolerance and dependence after acute or chronic administration of the selective delta-opioid agonist SNC80 were assessed in rhesus monkeys (Macaca mulatta) responding under a schedule food presentation. dose dependently decreased response rates. These effects waned 5 h. When administered as an 24-h pretreatment, (1.0-10.0 mg/kg) produced tolerance evidenced by dose-dependent rightward shifts dose-effect curve. Pretreatments 3.2 10.0 mg/kg increased ED50 4- 25-fold, respectively. to was also time-dependent values when 5-h (14-fold), (25-fold), 3-day (11-fold) pretreatment. The curve similar control 7-day delta-antagonist naltrindole (1.0 partially blocked SNC80. Chronic mg/kg/day) more effective than producing tolerance. Moreover, slowly Acute (10.0 cross-tolerance rate-decreasing other delta-agonists (SNC162 SNC243A) but not mu- (morphine) kappa (U-50,488)-agonists. Changes rates behavioral signs withdrawal observed opioid antagonists (i.e., naltrexone) treated with data suggest that pharmacologically develops both little no dependence.
参考文章(41)
L A Dykstra, D E Gmerek, J H Woods, Kappa opioids in rhesus monkeys. III. Dependence associated with chronic administration. Journal of Pharmacology and Experimental Therapeutics. ,vol. 242, pp. 428- 436 ,(1987)
Ann E. Remmers, Mary J. Clark, Fedor Medzihradsky, Xiang Yang Liu, Delta Opioid Receptor Down-Regulation Is Independent of Functional G Protein yet Is Dependent on Agonist Efficacy Journal of Pharmacology and Experimental Therapeutics. ,vol. 287, pp. 625- 632 ,(1998)
J H Woods, F Medzihradsky, T F Burke, S S Negus, Effects of opioid agonists selective for mu, kappa and delta opioid receptors on schedule-controlled responding in rhesus monkeys: antagonism by quadazocine. Journal of Pharmacology and Experimental Therapeutics. ,vol. 267, pp. 896- 903 ,(1993)
L R Gerak, Behavioral effects of 6-methylene naltrexone (nalmefene) in rhesus monkeys. Journal of Pharmacology and Experimental Therapeutics. ,vol. 270, pp. 992- 999 ,(1994)
W H Morse, Pharmacological characterization of supersensitivity to naltrexone in squirrel monkeys Journal of Pharmacology and Experimental Therapeutics. ,vol. 250, pp. 928- 936 ,(1989)
A Herz, C Stein, T S Shippenberg, K Peter, M J Millan, Peripheral opioid receptors mediating antinociception in inflammation. Evidence for involvement of mu, delta and kappa receptors. Journal of Pharmacology and Experimental Therapeutics. ,vol. 248, pp. 1269- 1275 ,(1989)
Silvia N. Calderon, Kenner C. Rice, Richard B. Rothman, Frank Porreca, Judith L. Flippen-Anderson, Heng Xu, Karen Becketts, Larren E. Smith, Edward J. Bilsky, Peg Davis, Robert Horvath, Probes for narcotic receptor mediated phenomena. 23.1 Synthesis, opioid receptor binding, and bioassay of the highly selective δ agonist (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC 80) and related novel nonpeptide δ opioid receptor ligands Journal of Medicinal Chemistry. ,vol. 40, pp. 695- 704 ,(1997) , 10.1021/JM960319N
Smriti Iyengar, Helen S. Kim, Paul L. Wood, μ-, δ-, κ- and ϵ-Opioid receptor modulation of the hypothalamic-pituitary-adrenocortical (HPA) axis: subchronic tolerance studies of endogenous opioid peptides Brain Research. ,vol. 435, pp. 220- 226 ,(1987) , 10.1016/0006-8993(87)91604-0
Jill U. Adams, Stephen G. Holtzman, Naltrexone-sensitizing effects of centrally administered morphine and opioid peptides. European Journal of Pharmacology. ,vol. 193, pp. 67- 73 ,(1991) , 10.1016/0014-2999(91)90201-Z
Mitchell J. Picker, Jill Yarbrough, Cross-tolerance and enhanced sensitivity to the response rate-decreasing effects of opioids with varying degrees of efficacy at the mu receptor. Psychopharmacology. ,vol. 105, pp. 459- 466 ,(1991) , 10.1007/BF02244364