Receptors, Opioid, kappa - Antagonists & inhibitors
Research News and Information

Sunday, November 22, 2009

Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.

16 Jul 2009 Based on an established 3D pharmacophore, a series of quinoline derivatives were synthesized. The opioidergic properties of these compounds were determined by a competitive binding assay using (125)I-Dynorphine, (3)H-DAMGO and (125)I-DADLE for ... Read more...

Acute and chronic fentanyl administration causes hyperalgesia independently of opioid receptor activity in mice.

22 Jun 2009 Although mu-receptor opioids are clinically important analgesics, they can also paradoxically cause hyperalgesia independently of opioid receptor activity, presumably via the action of neuroexcitatory glucoronide metabolites. However, it is unknown ... Read more...

Inhibitory effect of lidocaine on pain and itch using formalin-induced nociception and 5'-guanidinonaltrindole-induced scratching models in mice: behavioral and neuroanatomical evidence.

19 Jun 2009 The aim of this study was to establish the effect of lidocaine, a local anesthetic, on pain and itch using formalin-induced nociception and kappa opioid antagonist-induced scratching models in mice. We investigated if local intradermal pretreatment ... Read more...

Latest indexed articles for 'Receptors, Opioid, kappa - Antagonists & inhibitors'

These are the very latest articles for this heading:

• Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence. 16 Jul 2009
• Acute and chronic fentanyl administration causes hyperalgesia independently of opioid receptor activity in mice. 22 Jun 2009
• Inhibitory effect of lidocaine on pain and itch using formalin-induced nociception and 5'-guanidinonaltrindole-induced scratching models in mice: behavioral and neuroanatomical evidence. 19 Jun 2009
• Kappa-opioid ligands in the study and treatment of mood disorders. 31 May 2009
• Morphine-6beta-glucuronide rapidly increases pain sensitivity independently of opioid receptor activity in mice and humans. 30 May 2009
• Peptide kappa opioid receptor ligands: potential for drug development. 7 May 2009
• Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. May 2009
• The effects of repeated opioid administration on locomotor activity: I. Opposing actions of mu and kappa receptors. 27 Apr 2009
• [Intracellular mechanisms of opioidergic regulation of the myocardial function during normoxia and postischemic reperfusion] 30 Mar 2009
• Blockade of central kappa-opioid receptors inhibits the antidipsogenic effect of interleukin-1beta. 11 Feb 2009
• Chemical function-based pharmacophore generation of selective kappa-opioid receptor agonists by catalyst and phase. 9 Feb 2009
• Synthesis of cyclic tetrapeptide CJ 15,208: a novel kappa opioid receptor antagonist. 30 Dec 2008
• Design and synthesis of cyclic arodyn analogues by ring-closing metathesis (RCM) for kappa opioid receptor (KOP) antagonists. 30 Dec 2008
• Comparison with naloxone of two dynorphin A analogues with K- and delta-opioid antagonist activity. 30 Dec 2008
• Protection conferred by Corticotropin-releasing hormone in rat primary cortical neurons against chemical ischemia involves opioid receptor activation. 28 Dec 2008
• Dynorphin inhibits NEP activity in R1.1 mouse thymoma cells. 29 Nov 2008
• Synthesis of novel twin drug consisting of 8-oxaendoethanotetrahydromorphides with a 1,4-dioxane spacer and its pharmacological activities: mu, kappa, and putative epsilon opioid receptor antagonists. 16 Nov 2008
• Kappa opioids promote the proliferation of astrocytes via Gbetagamma and beta-arrestin 2-dependent MAPK-mediated pathways. 8 Nov 2008
• Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates. 6 Oct 2008
• Lack of tolerance and morphine-induced cross-tolerance to the analgesia of chimeric peptide of Met-enkephalin and FMRFa. 24 Sep 2008

See a longer list of these articles.

Technical information about 'Receptors, Opioid, kappa'

Definition: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.

Registry Number: 0

Descriptor UI: D017473

Alternative terms: Receptors, Opioid, kappa; Opioid Receptors, kappa; kappa Opioid Receptors; Receptors, kappa Opioid; Receptors, kappa; kappa Receptor; Receptor, kappa; kappa Receptors; kappa Opioid Receptor; Opioid Receptor, kappa; Receptor, kappa Opioid;

Allowable Qualifiers: administration & dosage; analysis; antagonists & inhibitors; biosynthesis; blood; classification; deficiency; drug effects; genetics; history; immunology; isolation & purification; metabolism; physiology; radiation effects; therapeutic use; ultrastructure; chemistry; agonists;

Tree Number: D12.776.543.750.100.620.400; D12.776.543.750.720.600.610.400; D12.776.543.750.750.555.610.400;

Online Note: use RECEPTORS, OPIOID, KAPPA to search RECEPTORS, KAPPA 1993; use RECEPTORS, OPIOID, KAPPA (NM) to search KAPPA RECEPTOR 1980-92

History Note: 94; was RECEPTORS, KAPPA 1993; was KAPPA RECEPTOR (NM) 1980-92

Technical Notes: opioid receptors found in the anterior pituitary & substantia nigra; DF: RECEPT KAPPA