Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide

Journal of Medicinal Chemistry
Remo GuerriniDomenico Regoli

Abstract

Nociceptin (NC) and some of its fragments as well as nociceptin-(1-13)-peptide amide [NC- (1-13)-NH2] and a series of its analogues were prepared and tested in the mouse vas deferens in an attempt to identify the sequences involved in the activation (message) and in the binding (address) of nociceptin to its receptor. The NC receptor that inhibits the electrically evoked twitches of the mouse vas deferens was demonstrated to be distinct from the delta opioid receptor, since naloxone and Dmt-Tic-OH (a selective delta opioid receptor antagonist) block the delta opioid receptor but have no effect on the nociceptin receptor. Results from structure-activity experiments suggest that (a) the entire sequence of NC may not be required for full biological activities, since NC(1-13)-NH2 is as active as NC; (b) fragments of NC have however to be amidated as in NC(1-13)-NH2 in order to be protected from degradation by proteases; (c) cationic residues (as Arg8,12, Lys9,13) appear to play a functional role, since their replacement with Ala in the sequence of NC(1-13)-NH2 leads to inactivity; (d) the N-terminal tetrapeptide Phe-Gly-Gly-Phe is essential for activity: its full length and flexibility appear to be required for NC receptor activati...Continue Reading

References

Nov 5, 1979·Life Sciences·J SawynokF S LaBella
Jan 1, 1992·International Journal of Developmental Neuroscience : the Official Journal of the International Society for Developmental Neuroscience·V Erspamer
Jul 1, 1989·Medicinal Research Reviews·V J Hruby, C A Gehrig
Jan 1, 1985·Peptides·R de Castiglione, A C Rossi
Jun 14, 1996·The Journal of Biological Chemistry·R K ReinscheidO Civelli
Aug 6, 1996·Proceedings of the National Academy of Sciences of the United States of America·H P NothackerO Civelli
Apr 29, 1996·European Journal of Pharmacology·I P Berzetei-GurskeL Toll
Sep 5, 1996·European Journal of Pharmacology·G CalòD Regoli
Nov 1, 1996·Neuroscience·J S MogilD K Grandy

❮ Previous
Next ❯

Citations

Oct 10, 2002·Journal of Peptide Science : an Official Publication of the European Peptide Society·Pietro AmodeoPiero A Temussi
Oct 11, 2008·Intensive Care Medicine·Dickson CarvalhoFelipe Dal-Pizzol
Jun 29, 2007·Naunyn-Schmiedeberg's Archives of Pharmacology·M KitayamaD G Lambert
Sep 23, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Massimo IbbaDavid G Lambert
Feb 3, 2009·Naunyn-Schmiedeberg's Archives of Pharmacology·Valeria CamardaGirolamo Calo
Jul 21, 2012·Bulletin of Experimental Biology and Medicine·E A IvanovaA A Kamensky
Oct 11, 2003·Biochemical and Biophysical Research Communications·Brice Bes, Jean-Claude Meunier
May 17, 2000·FEBS Letters·P AmodeoT Tancredi
Jun 4, 1998·Trends in Neurosciences·T DarlandD K Grandy
Jul 26, 2002·Regulatory Peptides·Florian LipplHans Dieter Allescher
Sep 22, 2000·Peptides·L TereniusT Sakurada
Sep 22, 2000·Peptides·G Calo'D Regoli
Sep 22, 2000·Peptides·C T Dooley, R A Houghten
Apr 29, 2000·European Journal of Medicinal Chemistry·D BarloccoL Toma
Apr 24, 1999·Progress in Neurobiology·T YamamotoS Kimura
Feb 5, 2003·Bioorganic & Medicinal Chemistry Letters·Remo GuerriniSevero Salvadori
Aug 2, 2008·Nature Reviews. Drug Discovery·David G Lambert
Mar 7, 1998·British Journal of Pharmacology·R GuerriniD Regoli
Sep 28, 1999·British Journal of Pharmacology·A SiniscalchiC Bianchi
Apr 1, 2000·British Journal of Pharmacology·G Calo'D Regoli
May 16, 2002·British Journal of Pharmacology·Girolamo CaloDomenico Regoli
Aug 7, 2002·British Journal of Pharmacology·Anna SiniscalchiClementina Bianchi
Apr 25, 2001·British Journal of Clinical Pharmacology·R BigoniD G Lambert
Sep 25, 2001·Neuroreport·A RizziG Calò
May 9, 2013·Doklady Biological Sciences : Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections·E A ChesnokovaN F Myasoedov
Feb 22, 2001·The Journal of Clinical Investigation·V LaudenbachP Gressens

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.