IN VITRO RESPONSE OF TRACHEAL SMOOTH MUSCLE FROM HYPERRESPONSIVE GUINEA PIGS TO CELIPROLOL
Abstract
Background: The use of -blockers is limited by adverse effects such as bronchospasm in asthmatics.Third generation -blockers such as celiprolol may show better respiratory tolerability because theylack -blocker induced broncho-constriction. Method: Effect of celiprolol on the histamine inducedcontraction of tracheal muscle strips prepared from ovalbumin-sensitised guinea pigs was studied.Using oxygenated Krebs-Henseleit solution as the nutrient medium, the trachealis muscle activity wasmeasured with isometric force displacement transducer and recorded on 4-channel Oscillograph.Result: Celiprolol 10-4 M shifted the concentration-response curve of histamine downwards and to theright. Mean of amplitude of contraction, percent responses and deviations when compared with thecontrol group were significantly different (p<0.05). Conclusion: Celiprolol antagonised histamineinduced contractions of tracheal muscle of guinea pigs. So it may be considered safe in patients withasthma. However, further clinical evaluation and exploratory work is required.Keywords: Celiprolol, Histamine, Chronic Obstructive Airway Disease (COAD), Tracheal muscleReferences
Limmroth, Michel MC. The prevention of migraine: a critical
review with special emphasis on beta-adrenoceptor blockers. Br J
Clin Pharmacol 2001;52:237–43.
Ochi S, Nakazawa M, Kimura T, Nakagawa Y, Imai S.
Partial agonist activity of celiprolol, a cardioselective β-
antagonist. Eur J Pharmacol 2002;194(1):171–6.
Cazzola M, Noschese P, Amato MD, Amato GD. Comparison of
the effects of single oral doses of nebivolol and celiprolol on
airways in patients with mild asthma. Chest 2000;118:1322–6.
Brink C, Duncan PG, Douglas JS. The response and sensitivity to
histamine of respiratory tissue from normal to ovalbumin sensitized
guinea pigs: effects of cyclooxygenase and lipoxegenase inhibition.
J Pharmacol Exp Ther 1981;217:592–601.
Gilani AH, Khan A, Raoof M, Ghayur MN, Siddiqui BS,
Vohra W, et al. Gastrointestinal, selective airway and urinary
bladder relaxant effect of Hyoscyamus niger are mediated
through dual blockade of muscarinic receptors and Calcium
channels. Fundam Clin Pharmacol 2008;22:87–99.
Liao Y, Asakura M, Takashima S, Ogai A, Asano Y, Shintani
Y, et al. Celiprolol, A vasodilatory β blocker inhibits
pressure overload induced cardiac hypertrophy and prevents
transition to heart failure via NO dependent mechanism in
mice. Circulation 2004; 110:692–699.
Wheeldon NM, McDevitt DG, Lipworth BJ. Selectivity of
antagonist and partial agonist activity of celiprolol in normal
subjects. Br J Clin Pharmacol 1992;34:337–43.
Hauck RW, Schulz EHP, Bohm M. Pharmacological actions of
selective and non selective beta adrenoceptor antagonists
celiprolol, bisoprolol and propranolol on human bronchi. Br J
Pharmacol 1994;113:1043–9.
Doshan DH, Brown R, Rosenthal RR, Slutsky A, Aplin WJ and
Caruso FS. Celiprolol, atenolol and propranolol: a comparison of
pulmonary effects in asthmatic patients. J Cardiovasc Pharmacol
;8(4):105–8.
Toda N. Vasodilating β-adrenoceptor blockers as
cardiovascular therapeutics. Pharmacol Ther
;100(3):215–34.
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