Receptors, Opioid - Antagonists & inhibitors
Research News and Information

Monday, November 23, 2009

Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.

8 Sep 2009 To improve the structure-activity studies of the lead delta opioid agonist H-Dmt-Tic-Asp*-Bid, we synthesized and pharmacologically characterized a series of analogues in which the side chain next to 1H-benzimidazole-2-yl (Bid) was substituted by ... Read more...

Methylnaltrexone, a peripherally acting opioid receptor antagonist, enhances tumoricidal effects of 5-Fu on human carcinoma cells.

30 Jul 2009 BACKGROUND: Methylnaltrexone, a novel peripherally acting opioid receptor antagonist, is used to treat opiate-induced constipation in cancer patients. Its effects on the activities of chemotherapeutic agents, however, have not been evaluated. In ... Read more...

Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.

21 Jul 2009 Our efforts to optimize prototype opioid receptor-like 1 (ORL1) antagonist 1 led to the discovery of ... Read more...

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

These are the very latest articles for this heading:

• Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore. 8 Sep 2009
• Methylnaltrexone, a peripherally acting opioid receptor antagonist, enhances tumoricidal effects of 5-Fu on human carcinoma cells. 30 Jul 2009
• Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate. 21 Jul 2009
• Distinct opioid circuits determine the palatability and the desirability of rewarding events. 11 Jul 2009
• Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure. 29 Jun 2009
• Local antinociception induced by endothelin-1 in the hairy skin of the rat's back. 29 Jun 2009
• Hypoglycemia-associated autonomic failure is prevented by opioid receptor blockade. 28 Jun 2009
• Acute and chronic fentanyl administration causes hyperalgesia independently of opioid receptor activity in mice. 22 Jun 2009
• Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. 15 Jun 2009
• Involvement of the Nociceptin/Orphanin FQ-NOP receptor system in the ventrolateral periaqueductal gray following mechanical allodynia in chronic pain. 9 Jun 2009
• In vitro and in vivo characterization of opioid activities of C-terminal esterified endomorphin-2 analogs. 7 Jun 2009
• Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain. 3 Jun 2009
• Retrograde opioid signaling regulates glutamatergic transmission in the hypothalamus. Jun 2009
• Structure-activity studies on the nociceptin/orphanin FQ receptor antagonist 1-benzyl-N-{3-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl} pyrrolidine-2-carboxamide. 31 May 2009
• [Significance of opioid receptors in regulation of cardiac tolerance in pathogenic impact of long-term ischemia-reperfusion in vivo] 30 May 2009
• Morphine-6beta-glucuronide rapidly increases pain sensitivity independently of opioid receptor activity in mice and humans. 30 May 2009
• Opioid receptor antagonist promotes angiogenesis in bile duct ligated rats. 24 May 2009
• Alteration in male reproductive system in experimental cholestasis: roles for opioids and nitric oxide overproduction. 11 May 2009
• Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24. 10 May 2009
• The relative potency of inverse opioid agonists and a neutral opioid antagonist in precipitated withdrawal and antagonism of analgesia and toxicity. 10 May 2009

See a longer list of these articles.

Technical information about 'Receptors, Opioid'

Definition: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.

Registry Number: 0

Descriptor UI: D011957

Alternative terms: Receptors, Opioid; Opiate Receptors; Opioid Receptor; Receptor, Opioid; Opioid Receptors; Opiate Receptor; Receptor, Opiate; Receptors, Opiate; Receptors, Normorphine; Normorphine Receptors; Receptors, Narcotic; Narcotic Receptors; Enkephalin Receptor; Receptor, Enkephalin; Receptors, Enkephalin; Enkephalin Receptors; beta-Endorphin Receptor; Receptor, beta-Endorphin; beta Endorphin Receptor; Receptors, beta-Endorphin; Receptors, beta Endorphin; beta-Endorphin Receptors; Receptors, Endorphin; Endorphin Receptor; Receptor, Endorphin; Endorphin Receptors;

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; D12.776.543.750.720.600.610; D12.776.543.750.750.555.610;

Online Note: use RECEPTORS, OPIOID to search RECEPTORS, ENDORPHIN 1980-93 & RECEPTORS, NARCOTIC 1977-79

History Note: 94; was RECEPTORS, ENDORPHIN 1980-93; was RECEPTORS, NARCOTIC 1977-79

Technical Notes: coord IM with specific opioid (IM); DF: RECEPT OPIOID