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Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes.
J Pharmacol Exp Ther. 1991 Jun; 257(3):1069-75.JP

Abstract

The present study has investigated the direct opioid delta receptor-mediated antinociception produced by i.c.v. administration of the highly selective delta agonists, [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2]deltorphin II, as well as that of the less delta-selective [D-Ser2,Leu5,Thr6]enkephalin (DSLET), by using two novel nonequilibrium opioid antagonists, [D-Ala2,Leu5,Cys6] enkephalin (DALCE) and naltrindole 5'-isothiocyanate (5'-NTII). At times ranging from 8 to 48 hr after a single i.c.v. pretreatment of mice with 5'-NTII, the antinociceptive effects of [D-Ala2] deltorphin II were significantly antagonized. In contrast, 5'-NTII pretreatment at times between 10 min and 24 hr failed to antagonize the antinociceptive effects of DPDPE. Previous studies have shown that pretreatment with i.c.v. DALCE produces a dose- and time-related antagonism of DPDPE, but not morphine, antinociception. However, pretreatment with i.c.v. DALCE failed to antagonize the antinociceptive effects of [D-Ala2]deltorphin II. Similarly, i.c.v. administration of DSLET produced time- and dose-related antinociception which was partially antagonized by either beta-funaltrexamine (beta-FNA) or by ICI 174,864 (N,N-dialyl-Tyr-Aib-Aib-Phe-Leu-OH), suggesting mixed activity at mu and delta receptors. ICI 174,864 produced essentially complete antagonism of DSLET antinociception in beta-FNA-pretreated mice. Pretreatment with 5'-NTII (at -8 to -48 hr), blocked the antinociception produced by DSLET in control or in beta-FNA-pretreated mice. In contrast, pretreatment with DALCE failed to antagonize the antinociception produced by i.c.v. DSLET in either control or in beta-FNA-pretreated mice.(ABSTRACT TRUNCATED AT 250 WORDS)

Authors+Show Affiliations

Department of Pharmacology, University of Arizona Health Sciences Center, Tucson.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

1646319

Citation

Jiang, Q, et al. "Differential Antagonism of Opioid Delta Antinociception By [D-Ala2,Leu5,Cys6]enkephalin and Naltrindole 5'-isothiocyanate: Evidence for Delta Receptor Subtypes." The Journal of Pharmacology and Experimental Therapeutics, vol. 257, no. 3, 1991, pp. 1069-75.
Jiang Q, Takemori AE, Sultana M, et al. Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes. J Pharmacol Exp Ther. 1991;257(3):1069-75.
Jiang, Q., Takemori, A. E., Sultana, M., Portoghese, P. S., Bowen, W. D., Mosberg, H. I., & Porreca, F. (1991). Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes. The Journal of Pharmacology and Experimental Therapeutics, 257(3), 1069-75.
Jiang Q, et al. Differential Antagonism of Opioid Delta Antinociception By [D-Ala2,Leu5,Cys6]enkephalin and Naltrindole 5'-isothiocyanate: Evidence for Delta Receptor Subtypes. J Pharmacol Exp Ther. 1991;257(3):1069-75. PubMed PMID: 1646319.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Differential antagonism of opioid delta antinociception by [D-Ala2,Leu5,Cys6]enkephalin and naltrindole 5'-isothiocyanate: evidence for delta receptor subtypes. AU - Jiang,Q, AU - Takemori,A E, AU - Sultana,M, AU - Portoghese,P S, AU - Bowen,W D, AU - Mosberg,H I, AU - Porreca,F, PY - 1991/6/1/pubmed PY - 1991/6/1/medline PY - 1991/6/1/entrez SP - 1069 EP - 75 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 257 IS - 3 N2 - The present study has investigated the direct opioid delta receptor-mediated antinociception produced by i.c.v. administration of the highly selective delta agonists, [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D-Ala2]deltorphin II, as well as that of the less delta-selective [D-Ser2,Leu5,Thr6]enkephalin (DSLET), by using two novel nonequilibrium opioid antagonists, [D-Ala2,Leu5,Cys6] enkephalin (DALCE) and naltrindole 5'-isothiocyanate (5'-NTII). At times ranging from 8 to 48 hr after a single i.c.v. pretreatment of mice with 5'-NTII, the antinociceptive effects of [D-Ala2] deltorphin II were significantly antagonized. In contrast, 5'-NTII pretreatment at times between 10 min and 24 hr failed to antagonize the antinociceptive effects of DPDPE. Previous studies have shown that pretreatment with i.c.v. DALCE produces a dose- and time-related antagonism of DPDPE, but not morphine, antinociception. However, pretreatment with i.c.v. DALCE failed to antagonize the antinociceptive effects of [D-Ala2]deltorphin II. Similarly, i.c.v. administration of DSLET produced time- and dose-related antinociception which was partially antagonized by either beta-funaltrexamine (beta-FNA) or by ICI 174,864 (N,N-dialyl-Tyr-Aib-Aib-Phe-Leu-OH), suggesting mixed activity at mu and delta receptors. ICI 174,864 produced essentially complete antagonism of DSLET antinociception in beta-FNA-pretreated mice. Pretreatment with 5'-NTII (at -8 to -48 hr), blocked the antinociception produced by DSLET in control or in beta-FNA-pretreated mice. In contrast, pretreatment with DALCE failed to antagonize the antinociception produced by i.c.v. DSLET in either control or in beta-FNA-pretreated mice.(ABSTRACT TRUNCATED AT 250 WORDS) SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/1646319/Differential_antagonism_of_opioid_delta_antinociception_by_[D_Ala2Leu5Cys6]enkephalin_and_naltrindole_5'_isothiocyanate:_evidence_for_delta_receptor_subtypes_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=1646319 DB - PRIME DP - Unbound Medicine ER -