PMID: 7518302May 1, 1994Paper

Comparison of tachykinin NK1 and NK2 receptors in the circular muscle of the guinea-pig ileum and proximal colon

British Journal of Pharmacology
C A MaggiA Giachetti

Abstract

1. The aim of this study was the pharmacological characterization of tachykinin NK1 and NK2 receptors mediating contraction in the circular muscle of the guinea-pig ileum and proximal colon. The action of substance P (SP), neurokinin A (NKA) and of the synthetic agonists [Sar9]SP sulphone, [Glp6,Pro9]SP(6-11) (septide) and [beta Ala8]NKA(4-10) was investigated. The affinities of various peptide and nonpeptide antagonists for the NK1 and NK2 receptor was estimated by use of receptor selective agonists. 2. The natural agonists, SP and NKA, produced concentration-dependent contraction in both preparations. EC50 values were 100 pM and 5 nM for SP, 1.2 nM and 19 nM for NKA in the ileum and colon, respectively. The action of SP and NKA was not significantly modified by peptidase inhibitors (bestatin, captopril and thiorphan, 1 microM each). 3. Synthetic NK1 and NK2 receptor agonists produced concentration-dependent contraction of the circular muscle of the ileum and proximal colon. EC50 values were 83 pM, 36 pM and 10 nM in the ileum, 8 nM, 0.7 nM and 12 nM in the colon for [Sar9]SP sulphone, septide and [beta Ala8]NKA-(4-10), respectively. The pseudopeptide derivative of NKA(4-10), MDL 28,564 behaved as a full or near-to-full agonis...Continue Reading

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Citations

Apr 14, 1995·Regulatory Peptides·C W Shuttleworth, K D Keef
May 4, 1995·Regulatory Peptides·U Holzer-Petsche
Sep 1, 1995·General Pharmacology·C A Maggi
Jun 23, 2000·European Journal of Pharmacology·R PatacchiniC A Maggi
Dec 1, 1998·European Journal of Pharmacology·J E ThorbøllE Skadhauge
Jan 9, 1999·European Journal of Pharmacology·J Goldhill, I Angel
Jan 1, 1997·Pharmacology & Therapeutics·P Holzer, U Holzer-Petsche
Nov 14, 1997·Trends in Pharmacological Sciences·C A Maggi, T W Schwartz
Apr 30, 1997·Regulatory Peptides·C A MaggiP Santicioli
Dec 1, 1996·Bioorganic & Medicinal Chemistry·S SaganS Lavielle
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Jul 1, 1997·Equine Veterinary Journal·I M SoneaN E Robinson
Mar 1, 1995·Medicinal Research Reviews·L QuartaraC A Maggi
Jun 8, 2011·European Journal of Pharmacology·Annemie DeiterenJoris G De Man
Jun 28, 2008·Neuropeptides·Frankie H M ChengJohn A Rudd
Mar 22, 2005·British Journal of Pharmacology·Maria Grazia ZizzoRosa Serio
Oct 21, 1999·The Journal of Pharmacy and Pharmacology·J GoldhillN Selve
Nov 28, 2001·The American Journal of Gastroenterology·A M O'RiordanA W Baird
Sep 28, 2005·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·A M HarringtonB R Southwell
Feb 28, 2002·The Journal of Pharmacology and Experimental Therapeutics·Kalina VenkovaB Greenwood-Van Meerveld
Jan 26, 2006·The Journal of Pharmacology and Experimental Therapeutics·Hugh T AbeyThomas M Cocks
Apr 16, 2004·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Thomas E ScholzenJohn C Ansel

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