BAAM exhibits non-specific depressant activity at higher concentrations and is not suitable as an irreversible beta-adrenoreceptor antagonist for in vitro organ bath experiments.
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BAAM should be avoided in cardiac organ bath experiments; leaves open identification of suitable irreversible beta-adrenoceptor antagonists.
The effects of the irreversible beta-adrenoreceptor antagonist bromoacetylalprenololmenthane (BAAM) were studied in isolated cardiac and uterine preparations from guinea-pigs and rats and in guinea-pig ileal preparations. 2. In the presence of BAAM (0.1-10 microM) concentration-effect curves to (-)-isoprenaline were shifted to the right in a concentration-dependent manner in all cardiac and uterine tissues. Maximum responses to (-)-isoprenaline were unaffected by BAAM except in guinea-pig left atrial and in some guinea-pig uterine preparations; however, the reductions in the maximum responses were not concentration-dependent. The mean pKB values for BAAM in guinea-pig left atria, right atria, rat whole atria and rat uterus were 7.26, 7.24, 6.84 and 7.90 respectively. 3. In guinea-pig ileal preparations, BAAM (0.1-30 microM) relaxed contractions induced by K+, histamine and acetylcholine in a non-beta-adrenoreceptor-related manner since relaxant responses were unaffected by propranolol (0.5 microM). In other tissues higher concentrations of BAAM (30-100 microM) elicited atrial standstill and depressed K+-induced contractions in uterine smooth muscle. 4. Treatment of tissues with BAAM (10-100 microM) followed by extensive wash-out increased the EC50 values for (-)-isoprenaline 21- to 83-fold. The maximum response to the catecholamine was unaffected by BAAM except in guinea-pig left atrial preparations following treatment with 100 microM BAAM. At these concentrations BAAM markedly increased the effective refractory period. 5. Concentration-effect curves for the partial agonist, oxymethylene-isoprenaline (OM-ISO) were shifted to the right 12- to 355-fold after pretreatment of tissues with BAAM (10-30 microM) followed by wash-out. The maximum response to OM-ISO was unaltered in guinea-pig and rat uteri and was reduced to a similar degree as observed with (-)-isoprenaline in guinea-pig left atria. 6. In general, the non-selective beta-adrenoreceptor antagonist BAAM depressed maximum responses to beta-adrenoreceptor agonists only in cardiac preparations and at concentrations which elicited depressant activity. On the basis of the present study, BAAM does not appear to be a suitable irreversible beta-adrenoreceptor antagonist for use in organ bath experiments.
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Ng et al. (1989) studied this question.
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