Possible Pharmacotherapy of the Opioid κ Receptor Agonist for Drug Dependence

Background: Efficient maternal pain relief after cesarean delivery remains challenging, but it is important to improve outcomes for the mother and the newborn during the puerperium. We compared the analgesic effect of nalbuphine (a κ receptor agonist/μ receptor antagonistic) with that of sufentanil (a µ-receptor agonist) in patient-controlled intravenous analgesia (PCIA) after cesarean section.Methods: We enrolled 84 patients scheduled for elective cesarean sections with spinal anesthesia and randomized them into either nalbuphine or sufentanil groups (42 patients each). Pain scores, PCIA drug consumptions, degree of satisfaction, and adverse events were recorded as outcome measures.Results: The pain scores at rest and uterine cramping pain scores in the nalbuphine group were lower than those in the sufentanil group at 6, 12, and 24 h after the operation. Also, the pain scores while switching to a seated position were lower in the nalbuphine group than in the sufentanil group at 6 and 12 h after the operation (p < 0.05). We found no significant differences in the PCIA drug consumption between the two groups. The degree of satisfaction in patients in the nalbuphine group was higher than that of patients in the sufentanil group (p = 0.01). Adverse events did not differ in the two groups.Conclusion: PCIA with nalbuphine provides better analgesia and higher patient satisfaction than sufentanil after cesarean section.

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dextro- and levo-morphine attenuate opioid δ and κ receptor agonist produced analgesia in μ-opioid receptor knockout mice

European Journal of Pharmacology ◽

10.1016/j.ejphar.2005.12.012 ◽

2006 ◽

Vol 531 (1-3) ◽

pp. 103-107 ◽

Cited By ~ 14

Author(s):

Hsiang-en Wu ◽

Han-Sen Sun ◽

Maia Terashivili ◽

Emma Schwasinger ◽

Ichiro Sora ◽

...

Keyword(s):

Opioid Receptor ◽

Knockout Mice ◽

Receptor Agonist ◽

Μ Opioid Receptor ◽

Κ Receptor

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Essential Structure of Opioid κ Receptor Agonist Nalfurafine for Binding to κ Receptor 1: Synthesis of Decahydroisoquinoline Derivatives and Their Pharmacologies

Chemical and Pharmaceutical Bulletin ◽

10.1248/cpb.c12-00336 ◽

2012 ◽

Vol 60 (8) ◽

pp. 945-948 ◽

Cited By ~ 12

Author(s):

Hiroshi Nagase ◽

Satomi Imaide ◽

Takaaki Yamada ◽

Shigeto Hirayama ◽

Toru Nemoto ◽

...

Keyword(s):

Receptor Agonist ◽

Κ Receptor

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Analgesic Efficacy of the κ-Receptor Agonist, Enadoline, in Dental Surgery Pain

Clinical Neuropharmacology ◽

10.1097/00002826-199619010-00009 ◽

1996 ◽

Vol 19 (1) ◽

pp. 92-97 ◽

Cited By ~ 47

Author(s):

Atul C. Pande ◽

Robert E. Pyke ◽

Martha Greiner ◽

Stephen A. Cooper ◽

Ronald Benjamin ◽

...

Keyword(s):

Receptor Agonist ◽

Analgesic Efficacy ◽

Dental Surgery ◽

Κ Receptor

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Suppression of cAMP by phosphoinositol/Ca2+ pathway in the cardiac κ-opioid receptor

AJP Cell Physiology ◽

10.1152/ajpcell.1998.274.1.c82 ◽

1998 ◽

Vol 274 (1) ◽

pp. C82-C87 ◽

Cited By ~ 25

Author(s):

Wei-Min Zhang ◽

Tak-Ming Wong

Keyword(s):

Receptor Agonist ◽

Ventricular Myocytes ◽

Tetraacetic Acid ◽

Acetoxymethyl Ester ◽

Receptor Stimulation ◽

Camp Pathway ◽

A 23187 ◽

Intracellular Ca ◽

First Time ◽

Κ Receptor

To determine whether the phosphoinositol/Ca2+ pathway interacts with the adenylate cyclase/adenosine 3′,5′-cyclic monophosphate (cAMP) pathway in the cardiac κ-receptor, the effects of U-50488, a specific κ-receptor agonist, on the intracellular Ca2+ concentration ([Ca2+]i) and forskolin-induced accumulation of cAMP in rat ventricular myocytes were determined after interference of the phosphoinositol/Ca2+ pathway. U-50488 suppressed the forskolin-induced accumulation of cAMP and elevated [Ca2+]i, which were blocked by norbinaltorphimine, a specific κ-receptor antagonist, and pertussis toxin. The effects of U-50488 were qualitatively similar to those of A-23187, a Ca2+ ionophore, but opposite to those of 1,2-bis(2-aminophenoxy)ethane- N, N, N′, N′-tetraacetic acid (BAPTA)-acetoxymethyl ester (AM), a [Ca2+]ichelator. Abolition of U-50488-induced elevation of [Ca2+]iby BAPTA-AM also abolished the effect of U-50488 on forskolin-induced accumulation of cAMP. Inhibition of the phospholipase C by specific inhibitors, U-73122 and neomycin, abolished the effects of U-50488 on both [Ca2+]iand forskolin-induced accumulation of cAMP. The results showed for the first time that κ-receptor stimulation may suppress cAMP accumulation via activation of the phosphoinositol/Ca2+ pathway in the rat heart.

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