![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
A Mattia, SC Farmer, AE Takemori, M Sultana, PS Portoghese, HI Mosberg, WD Bowen and F Porreca
Department of Pharmacology, University of Arizona Health Sciences Center, Tucson.
Previous studies from our laboratory have indicated that i.c.v. pretreatment of mice with the novel, selective opioid delta receptor antagonists, [D-Ala2,Leu5,Cys6]enkephalin (DALCE) and naltrindole-5'- isothiocyanate (5'-NTII), differentially antagonized the direct antinociceptive effects of [D-Pen2,D-Pen5]enkephalin (DPDPE) and [D- Ala2]deltorphin II (DELT). These findings, and others, suggested the existence of subtypes of opioid delta receptors which could be classified as activated by DPDPE and DALCE sensitive (delta 1 receptor), or selectively activated by DELT and 5'-NTII sensitive (delta 2 receptor). The present study has extended these observations to the characterization of delta-mediated antinociception effects of DPDPE and DELT after i.t. administration in mice using pretreatment with DALCE and 5'-NTII in order to selectively antagonize the delta subtypes. Additionally, the acute antinociceptive actions of DALCE itself were studied to ensure activity of this compound at the spinal level. The respective antinociceptive A50 value (95% CL) for i.t. DPDPE, DELT and DALCE were 19.0 (12.9-28.1), 19.3 (16.1-23.1) and 2.0 (1.4-3.0) nmol. The delta antagonist, N,N-diallyl-Try-Aib-Aib-Phe-Leu- OH (ICI 174,864) (where Aib is alpha-aminoisobutyric acid) blocked the antinociceptive effects of DPDPE and DELT, but not those of i.t. morphine or [D-Ala2,NMPhe4,Gly-ol5]enkephalin (DAMGO), indicating that the observed antinociceptive effects of DPDPE and DELT were delta mediated. Pretreatment 24 hr before testing with graded doses of i.t. 5'-NTII blocked the i.t. antinociceptive effects of DPDPE and DELT, although at least a 10-fold higher dose of 5'-NTII was needed to produce equivalent antagonism of DPDPE.(ABSTRACT TRUNCATED AT 250 WORDS)
This article has been cited by other articles:
|
|
 |
|
  A. Morinville, C. M. Cahill, M. J. Esdaile, H. Aibak, B. Collier, B. L. Kieffer, and A. Beaudet Regulation of {delta}-Opioid Receptor Trafficking via {micro}-Opioid Receptor Stimulation: Evidence from {micro}-Opioid Receptor Knock-Out Mice J. Neurosci., June 15, 2003; 23(12): 4888 - 4898. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. C. Broom, J. F. Nitsche, J. E. Pintar, K. C. Rice, J. H. Woods, and J. R. Traynor Comparison of Receptor Mechanisms and Efficacy Requirements for delta -Agonist-Induced Convulsive Activity and Antinociception in Mice J. Pharmacol. Exp. Ther., November 1, 2002; 303(2): 723 - 729. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. J. Bilsky, X. Qian, V. J. Hruby, and F. Porreca Antinociceptive Activity of [beta -Methyl-2',6'-dimethyltyrosine1]-Substituted Cyclic [D-Pen2,D-Pen5]Enkephalin and [D-Ala2,Asp4]Deltorphin Analogs J. Pharmacol. Exp. Ther., April 1, 2000; 293(1): 151 - 158. [Abstract] [Full Text]
|
|
|
|
|
|
C. G. Acosta and H. S. Lopez delta Opioid Receptor Modulation of Several Voltage-Dependent Ca2+ Currents in Rat Sensory Neurons J. Neurosci., October 1, 1999; 19(19): 8337 - 8348. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. W. Hurley, T. S. Grabow, R. J. Tallarida, and D. L. Hammond Interaction Between Medullary and Spinal delta 1 and delta 2 Opioid Receptors in the Production of Antinociception in the Rat J. Pharmacol. Exp. Ther., May 1, 1999; 289(2): 993 - 999. [Abstract] [Full Text]
|
|
|
|
|
|
L. He and N. M. Lee Delta Opioid Receptor Enhancement of Mu Opioid Receptor-Induced Antinociception in Spinal Cord J. Pharmacol. Exp. Ther., June 1, 1998; 285(3): 1181 - 1186. [Abstract] [Full Text]
|
|
|
|
|
|
D. L. Hammond, H. Wang, N. Nakashima, and A. I. Basbaum Differential Effects of Intrathecally Administered Delta and Mu Opioid Receptor Agonists on Formalin-Evoked Nociception and on the Expression of Fos-like Immunoreactivity in the Spinal Cord of the Rat J. Pharmacol. Exp. Ther., January 1, 1998; 284(1): 378 - 387. [Abstract] [Full Text]
|
|
|
|
|
|
S. N. Thorat and D. L. Hammond Modulation of Nociception by Microinjection of Delta-1 and Delta-2 Opioid Receptor Ligands in the Ventromedial Medulla of the Rat J. Pharmacol. Exp. Ther., December 1, 1997; 283(3): 1185 - 1192. [Abstract] [Full Text]
|
|
|
|
|
|
P. G. Szekeres and J. R. Traynor Delta Opioid Modulation of the Binding of Guanosine-5'-O-(3-[35S]thio)triphosphate to NG108-15 Cell Membranes: Characterization of Agonist and Inverse Agonist Effects J. Pharmacol. Exp. Ther., December 1, 1997; 283(3): 1276 - 1284. [Abstract] [Full Text]
|
|
|
|
 |
|
 C. Evans, D. Keith Jr, H Morrison, K Magendzo, and R. Edwards Cloning of a delta opioid receptor by functional expression Science, December 18, 1992; 258(5090): 1952 - 1955. [Abstract] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
