Activity of SR 142801 at peripheral tachykinin receptors

European Journal of Pharmacology
R PatacchiniC A Maggi

Abstract

The pharmacological profile of the novel tachykinin NK3 receptor antagonist SR 142801, ((S)-(N)-(1-(3-(1-benzoyl-3-(3,4-dichlorophenyl) piperidin-3-yl) propyl)-4-phenylpiperidin-4-yl)-N-methylacetamide), was studied at tachykinin NK1, NK2 and NK3 receptors, in several in vitro bioassays. In the guinea-pig isolated ileum longitudinal muscle preparation, SR 142801 (10 nM-1 microM) caused an insurmountable antagonism of tachykinin NK3 receptor-mediated contractions produced by senktide (apparent pKB = 9.27). The blockade induced by SR 142801 was essentially irreversible, since it was not removed by washout (up to 2 h) and was increased by prolonging the incubation from 15 to 120 min. SR 142801 showed similar antagonist potency at rat tachykinin NK3 receptors (portal vein) and rabbit tachykinin NK2 receptors (pulmonary artery) (pKB = 7.49 and 7.66, respectively), whereas it was distinctly less potent at hamster tachykinin NK2 receptors (trachea; pKB = 6.84) and inactive at guinea-pig tachykinin NK1 receptors (ileum, longitudinal muscle). In the guinea-pig whole ileum SR 142801 (100 nM) did not affect the contraction produced by capsaicin (1 microM). The combined SR 142801 pretreatment and tachyphylaxis of neuronal CGRP (calcitonin ...Continue Reading

References

Oct 1, 1978·Naunyn-Schmiedeberg's Archives of Pharmacology·L Barthó, J Szolcsányi
May 15, 1992·Biochemical and Biophysical Research Communications·C AdvenierD Regoli
Nov 13, 1990·European Journal of Biochemistry·K TsuchidaS Nakanishi
Jan 25, 1991·Science·R M SniderR W Spencer
Feb 1, 1991·Trends in Pharmacological Sciences·D H Jenkinson
Jul 1, 1990·British Journal of Pharmacology·C A MaggiA Meli
Nov 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·R LauferZ Selinger
May 5, 1986·FEBS Letters·J M ConlonL Thim
Jul 1, 1987·Neuropeptides·G DrapeauD Regoli
Dec 15, 1987·European Journal of Pharmacology·S Guard, S P Watson
Oct 23, 1989·Neuroscience Letters·M Takaki, S Nakayama
Jul 7, 1988·European Journal of Pharmacology·J C BeaujouanJ Glowinski
Feb 24, 1987·European Journal of Pharmacology·D MastrangeloD Regoli
Mar 31, 1987·European Journal of Pharmacology·L BarthóP Holzer
Oct 16, 1987·Neuroscience Letters·L BarthóJ Szolcsányi
Jun 1, 1982·Naunyn-Schmiedeberg's Archives of Pharmacology·L A Chahl
Feb 26, 1993·Biochemical and Biophysical Research Communications·F PetitetJ Glowinski
Feb 1, 1993·Journal of Autonomic Pharmacology·C A MaggiA Giachetti
Mar 30, 1993·European Journal of Pharmacology·C A MaggiA Giachetti
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

❮ Previous
Next ❯

Citations

Dec 6, 2005·Naunyn-Schmiedeberg's Archives of Pharmacology·Christian GeberHeinz Kilbinger
May 4, 1995·Regulatory Peptides·U Holzer-Petsche
Jan 29, 1997·European Journal of Pharmacology·J C BeaujouanJ Glowinski
May 20, 1998·European Journal of Pharmacology·P G McLeanL Buéno
Dec 1, 1998·European Journal of Pharmacology·J E ThorbøllE Skadhauge
Dec 29, 1998·European Journal of Pharmacology·M A Coudoré-CivialeJ Fialip
Aug 10, 1999·European Journal of Pharmacology·N MoodleyL Fisher
Jan 1, 1997·Pharmacology & Therapeutics·P Holzer, U Holzer-Petsche
Apr 30, 1997·Regulatory Peptides·C A MaggiP Santicioli
Jan 1, 1997·British Journal of Pharmacology·A D MedhurstD W Hay
Mar 4, 1998·British Journal of Pharmacology·R M CataliotoC A Maggi
Jan 12, 2002·British Journal of Pharmacology·Francesca BellucciCarlo Alberto Maggi
Dec 6, 2002·British Journal of Pharmacology·Eva PatakMargot E Story
Sep 28, 1999·Clinical and Experimental Pharmacology & Physiology·L Fisher, J N Pennefather
Nov 9, 2000·Clinical and Experimental Pharmacology & Physiology·K P Kerr
May 2, 2009·American Journal of Physiology. Gastrointestinal and Liver Physiology·Rachel M Gwynne, Joel C Bornstein
Jul 9, 1998·American Journal of Respiratory and Critical Care Medicine·S DaouiC Advenier
May 20, 1999·The Journal of Physiology·M NeunlistM Schemann
Jan 16, 2008·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·J G de ManP A Pelckmans
Sep 19, 2006·European Journal of Pharmacology·Cecilia CialdaiCarlo Alberto Maggi
Oct 27, 2004·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·T T KungR W Chapman
Feb 28, 2002·The Journal of Pharmacology and Experimental Therapeutics·Kalina VenkovaB Greenwood-Van Meerveld
Mar 1, 2010·Current Protocols in Pharmacology·Stefania Meini, Carlo Alberto Maggi

❮ 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.