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

Reid, Larry D.; Glick, Stanley D.; Menkens, Kent A.; French, Edward D.; Bilsky, Edward J.; Porreca, Frank

doi:10.1097/00001756-199507100-00012

Cited by 57 publications

(42 citation statements)

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“…The NAcc data are consistent with previous reports that DOR antagonism can significantly attenuate responding for cocaine (Reid et al 1995), although this effect had been characterized as modest (Negus et al 1995;Martin et al 2000) and inconsistent (Negus et al 1995). The present findings are most similar to Martin et al (2000), who reported that i.c.v.…”

supporting

confidence: 93%

Microinjection of the δ-opioid receptor selective antagonist naltrindole 5′-isothiocyanate site specifically affects cocaine self-administration in rats responding under a progressive ratio schedule of reinforcement

Ward

Roberts

2007

Behavioural Brain Research

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Whether the δ -opioid receptor (DOR) system can modulate behavioral effects of cocaine remains equivocal. We examined whether site-and subtype-selective blockade of DORs within the rat mesocorticolimbic system affects cocaine self-administration. The DOR antagonist naltrindole 5′-isothiocyanate (5′-NTII; 5 nmol) was microinjected into the nucleus accumbens (NAcc), ventral tegmental area (VTA), or amygdala (AMYG) in rats self-administering 1.5 mg/kg cocaine under a progressive ratio (PR)schedule. Intra-NAcc 5′-NTII significantly decreased cocaine selfadministration, while 5′-NTII administration into the VTA significantly increased cocainemaintained responding. 5′-NTII adminsitration into the AMYG produced no effect. These data support a site-specific role of DORs in cocaine's behavioral effects.Whereas the initial sites of action governing cocaine reinforcement are thought to be dopamine (DA) transporters within the mesocorticolimbic system (see Koob et al.1998 for review), a number of other neurotransmitter systems co-localized within the mesocorticolimbic system can modulate the reinforcing effects of cocaine, including the endogenous opioid system. For example, non-selective opioid receptor blockade with naloxone or naltrexone can decrease cocaine self-administration in both non-human primates (Mello et al 1990) and rodents (Carroll et al 1986;De Vry et al 1989;Corrigall and Coen 1991;Ramsey and Van Ree 1991;Ramsey et al 1999). The relative contributions of μ, δ, and κ opioid receptor subtype-specific antagonism by these compounds on decreased cocaine self-administration remain equivocal. For example, our laboratory reported that site specific microinjections of the μ-opioid receptor (MOR) selective antagonist beta-funaltrexamine (β-FNA) attenuated responding for cocaine under a progressive ratio (PR) schedule of reinforcement in rats (Ward et al 2003). However, MOR blockade has been shown by others to be ineffective in altering cocaine's reinforcing effects (Martin et al 1998;Corrigall et al 1999). Similarly, Kuzmin et al (1998) reported that κ-opioid antagonism decreased cocaine self-administration in rats, while others have reported no effect of κ-opioid antagonism on cocaine self-administration in rats and rhesus monkeys (Negus et al 1997).Corresponding author: Dr. Sara Jane Ward, Ph.D., Temple University School of Pharmacy, 3307 North Broad Street, Philadelphia, PA 19140, Phone: (215) 707-1005, Fax: (215) 707-3678, Email address: saraward@temple.edu Publisher's Disclaimer: This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final citable form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. (1995) reported that only a high dose of naltrindole ...

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supporting

confidence: 93%

Microinjection of the δ-opioid receptor selective antagonist naltrindole 5′-isothiocyanate site specifically affects cocaine self-administration in rats responding under a progressive ratio schedule of reinforcement

Ward

Roberts

2007

Behavioural Brain Research

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“…Competing IC 50 values for other compounds ranged from 50 to 100 n M . Taken together, in ␦ h CHO cell membrane fractions, agonist-like direct stimulatory effects of the peptides were not detected, while (2S,3R)DIMCP and (2S,3R)DIMCPamide analogs were able to antagonize the agonist action produced by Ile 5,6 deltorphin-II in these preparations. …”

Section: S]gtp ␥ S-binding Competition Assaysmentioning

confidence: 81%

“…Activating potency (EC 50 values) and effi cacy (% maximal stimulation) of the peptide analogs were measured and compared to those of prototype peptide agonist ligands, such as the ␦ -agonist Ile 5,6 deltorphin-II [20] and the -receptor-selective DAMGO [31] . Both in rat brain membrane preparations and in ␦ h CHO cell membranes stably expressing the human ␦ -opioid receptors, Ile 5,6 deltorphin-II caused a concentration-dependent increase in the binding of [ …”

Section: S]gtp ␥ S-binding Experimentsmentioning

confidence: 99%

“…Delta ( ␦ ) opioid ligands are especially important ligands in the study of narcotic addiction, since ␦ -receptor activation is not accompanied by severe signs of dependence in animal models [2,3] . Selective ligands for ␦ -opioid receptors may also have therapeutic potential as immunosuppressants [4] , and they offer a putative new approach to treat cocaine or alcohol addiction [5,6] . A number of ␦ -receptor-selective antagonists have been described with diverse chemical structures, among them are peptide derivatives, modifi ed epoxymorphinan alkaloid compounds, and others [7,8] .…”

mentioning

confidence: 99%

“…Unlabeled DAMGO was purchased from Bachem (Bubendorf, Switzerland). Ile 5,6 -deltorphin II and the TIPP analogs were synthesized in the BRC Radiolab or in the Department of Organic Chemistry of the Free University of Brussels (Belgium). [24] .…”

mentioning

confidence: 99%

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Opioid Receptor Binding Characteristics and Structure-Activity Studies of Novel Tetrapeptides in the TIPP (Tyr-Tic-Phe-Phe) Series

et al. 2005

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The development of the prototype synthetic δ-opioid receptor antagonist peptides TIPP [(H-Tyr-Tic-Phe- Phe-OH); Tic: tetrahydroisoquinoline-3-carboxylic acid] and TIPPψ (H-Tyr-ψTic-Phe-Phe-OH) by Schiller and coworkers was followed by extensive structure-activity relationship studies, leading to the emergence of numerous analogs that are of pharmacological interest. Eight novel diastereomeric compounds in this peptide family were designed, prepared, and tested biologically to gain structure-activity relationship information. The new multisubstituted tetrapeptide analogs contain both a 2′,6′-dimethyltyrosine residue at the N-terminus and β-methyl-cyclohexylalanine at the third position as replacements for the original first tyrosine and the third phenylalanine, respectively. These derivatives wear either free acidic (–COOH) or amidated (–CONH₂) C-terminal. The potency and δ- versus µ-opioid receptor selectivity were evaluated by in vitro radioreceptor-binding assays, while the intrinsic G-protein-activating efficacy of these analogs was tested in [³⁵S]GTPγS-binding assays using rat brain membranes or Chinese hamster ovary cells stably expressing µ- or δ-opioid receptors. The analogs showed δ-antagonist selectivity with differences regarding their isomeric forms, and these analogs containing a C-terminal carboxamide group displayed a mixed µ-agonist/δ-antagonist profile, thus they are expected to be safer analgesics with a low propensity to produce tolerance and physical dependence. These results constitute further examples of the influence of β-methyl substitution and C-terminal amidation on potency, selectivity, and signal transduction properties of TIPP-related peptides as well as they represent valuable pharmacological tools for opioid research.

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The TIPP opioid peptide family: Development of ? antagonists, ? agonists, and mixed ? agonist/? antagonists

et al. 1999

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

Cited by 57 publications

References 0 publications

Microinjection of the δ-opioid receptor selective antagonist naltrindole 5′-isothiocyanate site specifically affects cocaine self-administration in rats responding under a progressive ratio schedule of reinforcement

Microinjection of the δ-opioid receptor selective antagonist naltrindole 5′-isothiocyanate site specifically affects cocaine self-administration in rats responding under a progressive ratio schedule of reinforcement

Opioid Receptor Binding Characteristics and Structure-Activity Studies of Novel Tetrapeptides in the TIPP (Tyr-Tic-Phe-Phe) Series

The TIPP opioid peptide family: Development of ? antagonists, ? agonists, and mixed ? agonist/? antagonists

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