PMID: 7517327Mar 1, 1994Paper

Tachykinin NK1 receptor subtypes in the rat urinary bladder

British Journal of Pharmacology
S MeiniC A Maggi

Abstract

1. Following the recent proposal that the selective agonist septide, ([pGlu6,Pro9]SP(6-11)), acts on a novel tachykinin receptor distinct from the 'classical' NK1 receptor, the aim of the study was to investigate the possible heterogeneity of tachykinin NK1 receptors in the rat urinary bladder. 2. The synthetic tachykinin receptor agonists, septide (pD2 7.87) and [Sar9]substance P (SP) sulphone (pD2 7.64) produced concentration-dependent contractions of the rat isolated urinary bladder. 3. The NK1 receptor antagonists GR82,334, (+/-)-CP96,345, and RP67,580 competitively antagonized (slopes of Schild plot not significantly different from unity) the response to septide with the rank order of potency (pKB values in parentheses): RP 67,580 (7.57) > GR 82,334 (7.01) > (+/-)-CP 96,345 (6.80). The same antagonists were significantly less potent when tested against [Sar9]SP sulphone, while maintaining the same rank order of potency: RP 67,580 (7.00) > GR 82,334 (5.93) > (+/-)-CP 96,345 (< 6). The antagonists did not affect the concentration-response curve to bombesin. 4. To exclude the involvement of the NK2 receptor, a second series of experiments was performed in the presence of the potent nonpeptide NK2 receptor antagonist, SR 48,96...Continue Reading

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Citations

Nov 30, 1993·European Journal of Pharmacology·G R SeabrookJ Longmore
Sep 1, 1995·General Pharmacology·C A Maggi
Jan 29, 1997·European Journal of Pharmacology·J C BeaujouanJ Glowinski
Nov 14, 1997·Trends in Pharmacological Sciences·C A Maggi, T W Schwartz
May 30, 2001·The International Journal of Biochemistry & Cell Biology·S Harrison, P Geppetti
Mar 7, 1998·British Journal of Pharmacology·J MagranerM L Candenas
Jan 12, 2002·British Journal of Pharmacology·Francesca BellucciCarlo Alberto Maggi
Mar 31, 2004·British Journal of Pharmacology·Riccardo PatacchiniCarlo Alberto Maggi
Dec 17, 2009·The American Journal of Pathology·Veronica Sanchez FreireKatia Monastyrskaya
Dec 14, 2004·Life Sciences·Luz CandenasJocelyn N Pennefather
May 12, 2004·Peptides·Jean-Claude BeaujouanJacques Glowinski
Oct 25, 2016·Experimental Neurology·Beatrice GirardMargaret A Vizzard
Mar 1, 2010·Current Protocols in Pharmacology·Stefania Meini, Carlo Alberto Maggi
Sep 12, 2002·American Journal of Physiology. Gastrointestinal and Liver Physiology·Jaimie D NathanRodger A Liddle
Aug 11, 2000·Journal of Neurochemistry·J C BeaujouanJ Glowinski

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