Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats - PubMed (original) (raw)
Comparative Study
Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats
H J Schliep et al. Eur J Pharmacol. 1986.
Abstract
The beta-adrenoceptor antagonistic activity of i.v. administered bisoprolol ((+/-)-1-[4-(2-isopropoxyethoxymethyl)-phenoxy] -3-isopropylamino-2-propanol, hemifumarate) was studied under two different sets of experimental conditions in anaesthetized cats and compared to the activity of atenolol and propranolol. The responses of several target organs to beta 2-adrenoceptor stimulation were used: inhibition of isoprenaline effects on diastolic blood pressure, hindlimb perfusion pressure, soleus muscle contractility and histamine aerosol-induced bronchoconstriction. The inhibition of isoprenaline-induced tachycardia served as indicator of beta 1-antagonism. The slopes of agonist dose ratio vs. antagonist dose effect were close to unity for propranolol but deviated from unity for atenolol and even more so for bisoprolol. In spite of the ensuing difficulty of comparisons, bisoprolol showed the most pronounced selectivity indices (10-20), followed by atenolol (1-7.5) and propranolol (0.3-1.6). Thus, bisoprolol exhibited a higher degree of beta 1-selectivity in the cat than did atenolol, regardless of the parameter used for measurement of beta 2-antagonism. Propranolol proved to be non-selective or even had a somewhat higher affinity for beta 2- than for beta 1-adrenoceptors.
Similar articles
- Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and guinea pigs.
Schliep HJ, Harting J. Schliep HJ, et al. J Cardiovasc Pharmacol. 1984 Nov-Dec;6(6):1156-60. J Cardiovasc Pharmacol. 1984. PMID: 6084774 - The selectivity of beta-adrenoceptor antagonists on isoprenaline-induced changes in heart rate, blood pressure, soleus muscle contractility and airways function in anaesthetized cats.
Letts LG, Richardson DP, Temple DM, Williams LR. Letts LG, et al. Br J Pharmacol. 1983 Oct;80(2):323-34. doi: 10.1111/j.1476-5381.1983.tb10037.x. Br J Pharmacol. 1983. PMID: 6140058 Free PMC article. - Beta-adrenoceptor blockade by atenolol, metoprolol and propranolol in the anaesthetized cat.
Lundgren B, Carlsson E, Herrmann I. Lundgren B, et al. Eur J Pharmacol. 1979 May 1;55(3):263-8. doi: 10.1016/0014-2999(79)90193-6. Eur J Pharmacol. 1979. PMID: 37096 - Bisoprolol: a new beta-adrenoceptor blocking drug.
Prichard BN. Prichard BN. Eur Heart J. 1987 Dec;8 Suppl M:121-9. doi: 10.1093/eurheartj/8.suppl_m.121. Eur Heart J. 1987. PMID: 2897295 Review. - Clinical pharmacology of vasodilatory beta-blocking drugs.
Shanks RG. Shanks RG. Am Heart J. 1991 Mar;121(3 Pt 2):1006-11. doi: 10.1016/0002-8703(91)90612-l. Am Heart J. 1991. PMID: 1671724 Review.
Cited by
- Efficacy and tolerability of a β-1 selective β blocker, bisoprolol, as a first-line antihypertensive in Indian patients diagnosed with essential hypertension (BRIGHT): an open-label, multicentric observational study.
Channaraya V, Marya RK, Somasundaram M, Mitra D, Tibrewala KD; BRIGHT investigators. Channaraya V, et al. BMJ Open. 2012 May 14;2(3):e000683. doi: 10.1136/bmjopen-2011-000683. Print 2012. BMJ Open. 2012. PMID: 22586283 Free PMC article. - Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris.
Lancaster SG, Sorkin EM. Lancaster SG, et al. Drugs. 1988 Sep;36(3):256-85. doi: 10.2165/00003495-198836030-00002. Drugs. 1988. PMID: 2903820 Review. - Bisoprolol improves perfusion of ischaemic myocardium in anaesthetized pigs.
Sassen LM, den Boer MO, Rensen RJ, Saxena PR, Verdouw PD. Sassen LM, et al. Br J Pharmacol. 1988 Oct;95(2):361-70. doi: 10.1111/j.1476-5381.1988.tb11654.x. Br J Pharmacol. 1988. PMID: 2976288 Free PMC article.
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Miscellaneous