PMID: 7522864Jul 1, 1994Paper

Typical and atypical NK1 tachykinin receptor characteristics in the rabbit isolated iris sphincter

British Journal of Pharmacology
J M HallI K Morton

Abstract

1. A contraction of the rabbit isolated iris sphincter smooth muscle follows activation of either tachykinin NK1 or NK3 receptors. We have here characterized the pharmacological activity profiles of various tachykinin receptor agonists considered to have NK1-receptor-preferring activity in this preparation. 2. Two groups of NK1-receptor-preferring agonists could be distinguished in terms of a common pharmacological profile. The first group (Group 1) included [Glp6,L-Pro9]-SP(6-11) (septide), [Glp6]-SP (6-11), substance P methyl ester, delta-aminovaleryl-[L-Pro9, N-MeLeu10]-SP(7-11) (GR73632), and [Apa9-10]-SP. The second group (Group 2) included [Pro9]-SP, substance P, physalaemin and ranamargarin. 3. Under control conditions, the responses to Group 1 agonists were relatively fast in offset (time for reversal of maximal responses, 11.2-18.2 min), and were antagonized by NK1-receptor-selective antagonists (range of pKB estimates vs various agonists; GR82334, 7.1-8.2; (+/-)-CP-96,345, 8.9-9.5; RP67580, 7.0-7.4). Following incubation of the tissue with phenoxybenzamine (20 microM, 10 min), the affinity of GR82334, tested against the Group 1 agonists, substance P methyl ester and septide, was not significantly different (P < 0.05; ...Continue Reading

References

Nov 1, 1992·Pharmacology & Therapeutics·J M Hall
Apr 29, 1992·European Journal of Pharmacology·R PatacchiniC A Maggi
Feb 6, 1990·European Journal of Pharmacology·J M HallI K Morton
Jan 25, 1991·Science·R M SniderR W Spencer
Apr 30, 1991·Biochemical and Biophysical Research Communications·N RouissiD Regoli
Jul 15, 1991·Biochemical and Biophysical Research Communications·R HåkansonK Folkers
Jun 18, 1991·European Journal of Pharmacology·J M HallI K Morton
Nov 15, 1991·Proceedings of the National Academy of Sciences of the United States of America·C GarretP M Laduron
Jun 24, 1986·European Journal of Pharmacology·S LavielleJ Glowinski
Oct 1, 1993·Trends in Pharmacological Sciences·J M HallS Guard
Feb 1, 1993·Journal of Autonomic Pharmacology·C A MaggiA Giachetti

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Citations

Sep 1, 1995·General Pharmacology·C A Maggi
Nov 14, 1997·Trends in Pharmacological Sciences·C A Maggi, T W Schwartz
Dec 1, 1996·Bioorganic & Medicinal Chemistry·S SaganS Lavielle
Jan 1, 1997·British Journal of Pharmacology·A D MedhurstD W Hay
Apr 1, 1994·British Journal of Pharmacology·Z Y WangR Håkanson

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