The depolarizing action of 5-hydroxytryptamine on rabbit vagal afferent and sympathetic neurones in vitro and its selective blockade by ICS 205-930

British Journal of Pharmacology
A Round, D I Wallis

Abstract

Depolarizing responses to 5-hydroxytryptamine (5-HT) were recorded from rabbit nodose (NG) and superior cervical (SCG) ganglia using the sucrose-gap technique. The antagonist potency and selectivity of ICS 205-930 ([3 alpha-tropanyl]-1H-indole-3-carboxylic acid ester) were investigated. In NG, 5-HT (5 to 80 nmol) evoked depolarizations of graded amplitude. The ED50 was 18.2 (10.9-30.5) nmol (geometric mean, 95% confidence limits). Responses were blocked surmountably by ICS 205-930, 10(-11) and 10(-10) M, the threshold for blockade being below 10(-11) M. Parallel, rightward shifts in dose-response curves were seen with these concentrations of antagonist, but at higher concentrations (10(-9) and 10(-8) M) there was a further rightward shift with reduction in slope and maximum of the curves. In SCG, where 5-HT (20 to 320 nmol) evoked depolarizations of graded amplitude and the ED50 was 55.8 (22.3-139.6) nmol (geometric mean, 95% confidence limits), ICS 205-930 had a similar inhibitory effect to that observed in NG. The apparent pA2 values for the surmountable blockade produced by ICS 205-930 at concentrations of 10(-11) and 10(-10) M were 10.2 +/- 0.2 for NG and 10.4 +/- 0.1 for SCG (means +/- s.e. mean). ICS 205-930 was selective...Continue Reading

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Citations

Dec 1, 1988·Naunyn-Schmiedeberg's Archives of Pharmacology·P Elliott, D I Wallis
Oct 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·D HoyerJ M Palacios
Mar 21, 1989·European Journal of Pharmacology·N R Newberry, M J Gilbert
Sep 22, 1989·European Journal of Pharmacology·L M PinkusJ C Gordon
Feb 3, 1994·European Journal of Pharmacology·A MoránL San Román
Jul 1, 1993·Journal of the Autonomic Nervous System·B J Undem, D Weinreich
Jul 1, 1996·International Journal of Pediatric Otorhinolaryngology·C D LawhornR Shirey
Jan 1, 1996·Progress in Neurobiology·A J Lawrence, B Jarrott
Mar 1, 1987·Brain Research Bulletin·M A Hashim, D Bieger
Jan 1, 1988·Baillière's Clinical Gastroenterology·P L Andrews, J Hawthorn
Mar 5, 1997·European Journal of Pharmacology·M MinamiK Hagihara
Jun 5, 1997·European Journal of Pharmacology·A J LawrenceB Jarrott
Jul 4, 1998·European Journal of Pharmacology·E KrstewA J Lawrence
Dec 28, 2002·Progress in Neuro-psychopharmacology & Biological Psychiatry·Carlos A BolañosDenise Jackson
Feb 1, 1997·British Journal of Pharmacology·M Ashworth-PreeceA J Lawrence
Jan 5, 2001·British Journal of Pharmacology·B R TuladharR J Naylor
Jan 1, 1994·Anaesthesia·R J Naylor, F C Inall
Jun 1, 1993·Journal of Autonomic Pharmacology·G P Connolly, T W Stone
Nov 1, 1990·British Journal of Pharmacology·G J BirrellB D Grubb
Apr 1, 1995·British Journal of Pharmacology·A J LawrenceB Jarrott
Aug 7, 2004·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Masaru MinamiMasahiko Hirafuji
Nov 28, 2009·European Journal of Pharmacology·Seetha CheboluNissar A Darmani

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