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Persistent beta-adrenoceptor blockade with alkylating pindolol (BIM) in guinea-pig left atria and trachea.

Abstract：

:The actions of alkylating pindolol (N8-bromoacetyl-N1-3'-(4-indolyloxy)-2'-hydroxypropyl[z]-1,8- diamino-p-menthane; BIM) have been examined on beta-adrenoceptors in guinea-pig left atria and trachea. In organ bath experiments, addition of BIM (greater than or equal to 0.1 microM), 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" pA2 value for BIM was 9.23 +/- 0.20 (slope = 0.98 +/- 0.20). Changes in the maximal density of beta-adrenoceptor binding sites were determined in guinea-pig left atrial membranes using [125I]-cyanopindolol. BIM (0.1, 1.0 and 10 microM) produced 14, 23 and 41% reductions in Bmax with no change in KD. 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" KD value of [125I]-BIM at beta-adrenoceptor binding sites was 85.7 +/- 57.9 pM.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Molenaar P,Russell F,Pitha J,Summers R

doi

10.1016/0006-2952(88)90390-5

subject

Has Abstract

pub_date

1988-10-01 00:00:00

pages

3601-7

issue

19

eissn

0006-2952

issn

1873-2968

pii

0006-2952(88)90390-5

journal_volume

37

pub_type

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