OPIOID DELTA SUBTYPES--CORRELATION IN VITRO AND IN VIVO

阿片类药物 Delta 亚型——体外和体内的相关性

• 批准号: 2377332
• 负责人: Frank Porreca
• 金额: $ 9.93万
• 依托单位: UNIVERSITY OF ARIZONA
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-03-01 至 1998-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2377332
• 关键词: adenylate cyclase; brain; computer program /software; cyclic AMP; drug interactions; drug tolerance; genetic strain; guanine nucleotide binding protein; high performance liquid chromatography; hippocampus; inhibitor /antagonist; laboratory mouse; ligands; microinjections; opioid receptor; pertussis toxin; radiotracer; receptor binding; receptor sensitivity; stimulant /agonist; tissue /cell culture

The specific goals of the proposed work are to (a) directly identify opioid delta receptor subtypes in brain and other tissues using radioligand binding techniques in wholebrain control membranes, in membranes pretreated with selective and irreversible ligands, in membranes from different strains of mice which have been reported to show differences in populations of opioid receptors (e.g., the mu-receptor deficient CXBK mouse), and in membranes from specific brain regions; (b) investigate possible differences in the regulation of interactions of the receptor subtypes with their respective effector systems by evaluation of radioligand binding in the presence of guanine nucleotides, cations (or both), or following pretreatment with pertussis toxin in vitro or in vivo; (c) use radioligand binding techniques to evaluate possible mechanism of tolerance and supersensitivity following repeated/continuous exposure of the brain to compounds with selectivity for the opioid delta receptor subtypes, and (d) use some of the above approaches in an effector system by measuring adenylyl cyclase activity in NG 108-15 cells. Such approaches will provide insights into opioid delta subtypes, and their mechanisms which may correlate with substantial data accumulated in vivo, and may be important in establishing the potential therapeutic utility of delta subtype selective drugs.

拟议工作的具体目标是：(a)直接确定

项目成果

Antinociceptive profile of biphalin, a dimeric enkephalin analog.

• 发表时间: 1993-06
• 期刊: The Journal of pharmacology and experimental therapeutics
• 作者: Peter J. Horan;A. Mattia;E. Bilsky;S. J. Weber;T. Davis;H. Yamamura;E. Malatyńska;S. Appleyard;J. Slaninová;A. Misicka

Effects of naloxone and D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 and the protein kinase inhibitors H7 and H8 on acute morphine dependence and antinociceptive tolerance in mice.

• 发表时间: 1996-04
• 期刊: The Journal of pharmacology and experimental therapeutics
• 作者: E. Bilsky;R. N. Bernstein;Z. Wang;W. Sadee;F. Porreca

Cocaine self-administration and naltrindole, a delta-selective opioid antagonist.

可卡因自我给药和纳曲吲哚（一种 δ 选择性阿片拮抗剂）。

• DOI: 10.1097/00001756-199507100-00012
• 发表时间: 1995
• 期刊: Neuroreport
• 影响因子: 1.7
• 作者: Reid,LD;Glick,SD;Menkens,KA;French,ED;Bilsky,EJ;Porreca,F
• 通讯作者: Porreca,F

Differential antagonism of bremazocine- and U69,593-induced antinociception by quadazocine: further functional evidence of opioid kappa receptor multiplicity in the mouse.

四唑辛对布马佐辛和 U69,593 诱导的抗伤害作用的差异拮抗作用：小鼠中阿片类药物 kappa 受体多样性的进一步功能证据。

• 发表时间: 1993
• 期刊: The Journal of pharmacology and experimental therapeutics
• 作者: Horan,PJ;deCosta,BR;Rice,K;Haaseth,RC;Hruby,VJ;Porreca,F
• 通讯作者: Porreca,F

Increased expression of opioid delta receptors by deoxy conformation heme proteins in NG108-15 cells.

NG108-15 细胞中脱氧构象血红素蛋白增加阿片 δ 受体的表达。

• DOI: 10.1016/0006-8993(95)00089-9
• 发表时间: 1995
• 期刊: Brain research
• 影响因子: 2.9
• 作者: Mayfield,KP;Horvath,R;Lai,J;Porreca,F
• 通讯作者: Porreca,F