Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: Synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies

2012 ◽  
Vol 22 (24) ◽  
pp. 7711-7714 ◽  
Author(s):  
Hideaki Fujii ◽  
Satomi Imaide ◽  
Shigeto Hirayama ◽  
Toru Nemoto ◽  
Hiroaki Gouda ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Oxygen Functionality ◽  
Κ Receptor

scholarly journals Analgesic Effect Comparison Between Nalbuphine and Sufentanil for Patient-Controlled Intravenous Analgesia After Cesarean Section

2020 ◽  
Vol 11 ◽  
Author(s):  
Shen Sun ◽  
Yundong Guo ◽  
Tingting Wang ◽  
Shaoqiang Huang
Keyword(s):  
Adverse Events ◽  
Cesarean Section ◽  
Analgesic Effect ◽  
Receptor Agonist ◽  
Cesarean Sections ◽  
Pain Scores ◽  
Intravenous Analgesia ◽  
Degree Of Satisfaction ◽  
Elective Cesarean ◽  
Κ Receptor

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.

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

2006 ◽  
Vol 531 (1-3) ◽  
pp. 103-107 ◽  
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

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

2012 ◽  
Vol 60 (8) ◽  
pp. 945-948 ◽  
Author(s):  
Hiroshi Nagase ◽  
Satomi Imaide ◽  
Takaaki Yamada ◽  
Shigeto Hirayama ◽  
Toru Nemoto ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Κ Receptor

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

1996 ◽  
Vol 19 (1) ◽  
pp. 92-97 ◽  
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

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

1998 ◽  
Vol 274 (1) ◽  
pp. C82-C87 ◽  
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.

scholarly journals Antipruritic effects of opioid κ receptor agonist TRK-820

2000 ◽  
Vol 82 ◽  
pp. 229
Author(s):  
Yuko Togashi ◽  
Yoshitaka Yoshizawa ◽  
Toshiyuki Honda ◽  
Hideo Umeuchi ◽  
Toshiaki Tanaka ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Κ Receptor

scholarly journals Novel Molecular Targets of Dezocine and Their Clinical Implications

2014 ◽  
Vol 120 (3) ◽  
pp. 714-723 ◽  
Author(s):  
Renyu Liu ◽  
Xi-Ping Huang ◽  
Alexei Yeliseev ◽  
Jin Xi ◽  
Bryan L. Roth
Keyword(s):  
Opioid Receptor ◽  
Serotonin Transporter ◽  
Receptor Agonist ◽  
Molecular Targets ◽  
Norepinephrine Transporter ◽  
Clinical Implications ◽  
Protein Activation ◽  
G Protein Activation ◽  
Κ Receptor ◽  
Μ Receptor

Abstract Background: Although dezocine is a partial μ-opioid receptor agonist, it is not a controlled substance. Thus, the characterization of the molecular targets of dezocine is critical for scientific and clinical implications. The goal of this study is to characterize molecular targets for dezocine and determine their implications. Methods: A binding screen for dezocine was performed on 44 available receptors and transporter proteins. Functional assays for the novel targets were performed along with computation calculations to locate the binding site. A G protein activation study was performed for the human κ opioid receptor to determine whether dezocine is a κ-antagonist. Data are presented as mean ± standard error. Results: The affinities for dezocine were 3.7 ± 0.7 nM for the μ receptor, 527 ± 70 nM for the δ-receptor, and 31.9 ± 1.9 nM for the κ-receptor. Dezocine failed to induce G protein activation with κ-opioid receptor and concentration dependently inhibited κ-agonist (salvinorin A and nalbuphine)–induced receptor activation, indicating that dezocine is a κ-antagonist. Two novel molecular targets (norepinephrine transporter and serotonin transporter) were identified. Dezocine concentration-dependently inhibited norepinephrine and serotonin reuptake in vitro. The half maximal inhibitory concentrations (expressed as pIC50) were 5.68 ± 0.11 for norepinephrine transporter and 5.86 ± 0.17 for serotonin transporter. Dezocine occupied the binding site for known norepinephrine transporter and serotonin transporter inhibitors. Conclusions: The unique molecular pharmacological profile of dezocine as a partial μ-receptor agonist, a κ-receptor antagonist, and a norepinephrine and serotonin reuptake inhibitor (via norepinephrine transporter and serotonin transporter) was revealed. These discoveries reveal potentially important novel clinical implications and drug interactions of dezocine.

Possible Pharmacotherapy of the Opioid κ Receptor Agonist for Drug Dependence

2004 ◽  
Vol 1025 (1) ◽  
pp. 404-413 ◽  
Author(s):  
KO HASEBE ◽  
KOJI KAWAI ◽  
TOMOHIKO SUZUKI ◽  
KUNIAKI KAWAMURA ◽  
TOSHIAKI TANAKA ◽  
...  
Keyword(s):  
Drug Dependence ◽  
Receptor Agonist ◽  
Κ Receptor
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