Abstract
The actions of alkylating pindolol ( N 8-bromoacetyl- N 1-3′-(4-indolyloxy)-2′-hydroxypropyl-[ z]-1,8-diamino- p-menthane; BIM) have been examined on β-adrenoceptors in guinea-pig left atria and trachea. In organ bath experiments, addition of BIM (⩾0.1μM), followed by washout, produced concentration-dependent rightward shifts of the dose-response curve to cumulative additions of (−)-isoprenaline and oxymethylene-isoprenaline and reductions in the maximal response. The “apparent” p A 2; value for BIM was 9.23 ± 0.20 (slope = 0.98 ± 0.20). Changes in the maximal density of β-adrenoceptor binding sites were determined in guinea-pig left atrial membranes using [ 125I]-cyanopindolol. BIM (0.1, 1.0 and 10 μM) produced 14, 23 and 41% reductions in B max with no change in K D . The binding of [ 125I]-BIM to guinea-pig left atrial membranes had a high non-specific binding component and a pseudo-Hill coefficient less than unity. The “apparent” K D , value of [ 125I]-BIM at β-adrenoceptor binding sites was 85.7 ± 57.9 pM.
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