Buprenorphine Blocks ϵ- and μ-Opioid Receptor-Mediated Antinociception in the Mouse

  title={Buprenorphine Blocks ϵ- and $\mu$-Opioid Receptor-Mediated Antinociception in the Mouse},
  author={Hirokazu Mizoguchi and Amanda Spaulding and Randy J. Leitermann and Hsiang-En Wu and Hiroshi Nagase and Leon F. Tseng},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={394 - 400}
Antagonistic properties of buprenorphine for ϵ- and μ-opioid receptors were characterized in β-endorphin- and [d-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin (DAMGO)-induced antinociception, respectively, with the tail-flick test in male ICR mice. ϵ-Opioid receptor agonist β-endorphin (0.1–1 μg), μ-opioid receptor agonist DAMGO (0.5–20 ng), or buprenorphine (0.1–20 μg) administered i.c.v. dose dependently produced antinociception. The antinociception induced by 10 μg of buprenorphine given i.c.v. was… Expand
Differential effects of gestational buprenorphine, naloxone, and methadone on mesolimbic mu opioid and ORL1 receptor G protein coupling.
These findings on mu opioid receptor (MOR) GTP-binding regulatory protein (G protein) coupling and its gender dependency are consistent with earlier studies on mu receptor binding adaptation induced by buprenorphine in dams and neonatal rats after in utero treatment regimens, and they extend the gestational effects of this opiate to mu and N/OFQ receptor functionality. Expand
Buprenorphine: a unique drug with complex pharmacology.
Evidence is provided demonstrating that the ORL-1 receptor plays a functional role not only in the antinociceptive effect of buprenorphine but also in other actions of the drug as well. Expand
Antinociceptive effects of intravenous administration of hydromorphone hydrochloride alone or followed by buprenorphine hydrochloride or butorphanol tartrate to healthy conscious cats.
Butorphanol administration decreased the duration of antinociception achieved with hydromorphone administration in cats, and this opioid interaction and its impact on pain management require additional investigation. Expand
Mechanism-Based Pharmacokinetic-Pharmacodynamic Modelling of the Reversal of Buprenorphine-Induced Respiratory Depression by Naloxone
Because of the slow receptor association-dissociation Kinetics of buprenorphine in combination with the fast elimination kinetics of naloxone, nal oxone is best administered as a continuous infusion for reversal of buPrenorphines-induced respiratory depression. Expand
Interaction of μ‐opioid receptor agonists and antagonists with the analgesic effect of buprenorphine in mice
This study investigated the interaction potential with several full μ‐agonists in the tail‐flick test in mice and examined the reversibility of buprenorphine antinociception by different μ‐opioid receptor antagonists. Expand
Rational drug design and synthesis of a selective opioid receptor antagonist on the basis of the accessory site concept.
To newly synthesize a selective opioid receptor antagonist, 17-(cyclopropylmethyl)-4,5 alpha-epoxy-6 beta,21-epoxymethano-3-hydroxy-6,14-endoethenomorphinan-7 alpha-(N-phenethyl)carboxamide was firstExpand
Effects of intravenous patient-controlled analgesia with buprenorphine and morphine alone and in combination during the first 12 postoperative hours: a randomized, double-blind, four-arm trial in adults undergoing abdominal surgery.
In these patients undergoing abdominal surgery, the Buprenorphine + BUP-b regimen controlled postoperative pain as well as did MO-i + MO-b or the combinations of BUP and MO. Expand
Advances in the delivery of buprenorphine for opioid dependence
Clinical trial data for novel buprenorphine delivery systems in the form of subcutaneous depot injections, transdermal patches, and subdermal implants for the treatment of OUD are reviewed and both the clinical efficacy of longer-acting formulations through increasing consistent medication exposure and their potential utility in reducing diversion are discussed. Expand
Endogenous opiates and behavior: 2003
This paper is the 26th consecutive installment of the annual review of research concerning the endogenous opioid system, and summarizes papers published during 2003 that studied the behavioral effects of molecular, pharmacological and genetic manipulation of opioid peptides, opioid receptors, opioid agonists and opioid antagonists. Expand
Effect of transdermal opioids in experimentally induced superficial, deep and hyperalgesic pain
This work has compared the analgesic and anti‐hyperalgesic effects of buprenorphine and fentanyl. Expand


Buprenorphine is a potent κ-opioid receptor antagonist in pigeons and mice
Abstract Buprenorphine was studied for its antagonist activity against the specific κ-opioid agonist U-50,488H in pigeons responding under a multiple schedule of grain presentation and in mice in anExpand
Antagonistic property of buprenorphine for putative ϵ-opioid receptor-mediated G-protein activation by β-endorphin in pons/medulla of the μ-opioid receptor knockout mouse
Abstract β-Endorphin is a non-selective opioid peptide which binds μ-, δ- and putative ϵ (β-endorphin-sensitive non-μ-, non-δ- and non-κ 1 -)-opioid receptors. We have previously reported thatExpand
Antinociceptive effect of buprenorphine in mu1-opioid receptor deficient CXBK mice.
The results support the previous hypothesis that mu1- rather than mu2-, delta- or kappa-opioid receptors are involved in the antinociceptive effects of buprenorphine. Expand
Buprenorphine exerts its antinociceptive activity via mu 1-opioid receptors.
It is suggested that buprenorphine acts selectively at mu1-opioid receptors to induce antinociceptive effects in mice. Expand
β-Endorphin-(1–27) antagonizes β-endorphin- but not morphine-, D-PEN2-D-PEN2-enkephalin- and U50, 488H-induced analgesia in mice
β-Endorphin-(1–27), administered intraventricularly has been previously reported to block the analgesia induced by β-endorphin injected intraventricularly. The present study was to determine if theExpand
The role of spinal opioid receptors in antinociceptive effects produced by intrathecal administration of hydromorphone and buprenorphine in the rat.
It is reported for the first time that intrathecal buprenorphine is approximately 17 times more effective than hydromorphone in inhibiting thermal pain, and bupenorphine produces its antinociceptive effect by acting as an agonist at both mu- and kappa-spinal opioid receptors. Expand
The Role of Spinal Opioid Receptors in Antinociceptive Effects Produced by Intrathecal Administration of Hydromorphone and Buprenorphine in the Rat
Intrathecally-administered hydromorphone and buprenorphine produced a dose- and time-dependent increase in the tail-flick response latency in rats, and naloxone administered intrathecally was effective in preventing the antinociceptive effects of subsequent intrathecal injections of bupenorphine. Expand
Different types of opioid receptors mediating analgesia induced by morphine, DAMGO, DPDPE, DADLE and β-endorphin in mice
  • H. H. Suh, L. Tseng
  • Chemistry, Medicine
  • Naunyn-Schmiedeberg's Archives of Pharmacology
  • 2004
Results indicate that analgesia induced by morphine and DAMGO is mediated by the stimulation of mu-opioid receptors while analgesiainduced by DPDPE ismediated by the stimulating of delta-opIOid receptors. Expand
Involvement of epsilon and kappa opioid receptors in inhibition of the tail-flick response induced by bremazocine in the mouse.
The present studies were designed to determine what types of opioid receptors and neurotransmitters were involved in inhibiting the tail-flick response induced by bremazocine in male ICR mice. Expand
Evidence for ε-opioid receptor-mediated β-endorphin-induced analgesia
Abstract Among the opioid receptors, which have been pharmacologically classified as μ, δ, κ and e, the existence of the e receptor has been controversial, and this receptor is generally notExpand