PMID: 8358572Jul 1, 1993

Effects of rolipram and siguazodan on the human isolated bronchus and their interaction with isoprenaline and sodium nitroprusside

British Journal of Pharmacology
Y QianCharles Advenier

Abstract

1 The effects of the selective inhibitors of cyclic AMP phosphodiesterase type IV (rolipram) and type III (siguazodan) and their interactions with isoprenaline and sodium nitroprusside have been studied in the human isolated bronchus. 2 On bronchi under resting tone rolipram was, in terms of potency (pD2 = 7.77 +/- 0.14, n = 8), very similar to isoprenaline (pD2 = 7.31 +/- 0.12, n = 12) and salbutamol (pD2 = 7.12 +/- 0.17, n = 10) and approximately 10 fold more potent than siguazodan (pD2 = 6.80 +/- 0.12, n = 6). In terms of efficacy (Emax, expressed as percentage of maximal effect induced by theophylline 3 mM), both rolipram and siguazodan were less efficient (Emax = 74 +/- 6.7%, n = 8 and 66 +/- 7.5%, n = 6, respectively) than isoprenaline (Emax = 98 +/- 0.4%, n = 12) and salbutamol (Emax = 83 +/- 2.4%, n = 10). 3 During precontraction induced by methacholine (3 x 10(-7) M) or acetylcholine (10(-3) M), concentration-response curves to rolipram and siguazodan were shifted to the right and maximal effects reduced. Rolipram was more potent than siguazodan and, in terms of efficacy, it was less active. 4. Rolipram 10(-8) and 10(-7) M but not siguazodan potentiated the effects of isoprenaline as shown by the shift to the left of t...Continue Reading

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Citations

Oct 1, 1994·Trends in Pharmacological Sciences·T J Torphy
Jan 1, 1995·The International Journal of Biochemistry & Cell Biology·D Raeburn, Charles Advenier
May 7, 1998·European Journal of Pharmacology·J M PlanquoisS G Dahl
Mar 11, 1998·Clinical and Experimental Pharmacology & Physiology·M TanizawaK Takagi
Aug 1, 1995·Thorax·A J Knox, A E Tattersfield
Aug 2, 2000·Respiratory Medicine·S Thirstrup
May 14, 2016·British Journal of Pharmacology·R Venkatasamy, D Spina
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Nov 5, 2020·Fundamental & Clinical Pharmacology·Hélène SalvatorPhilippe Devillier

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