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Comparison of the binding constant (Ksub(D)) of /sup 125/I-labelled 3-(4-iodophenoxy)-1-isopropylaminopropan-2-ol obtained on. beta. -adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Ksub(B)) obtained on guinea-pig isolated atria and trachea

Journal Article:

Abstract

The dissociation constant of binding (Ksub(D) of /sup 125/I-labelled 3-(4-iodophenoxy)-isopropylaminopropan-2-ol (IIP) to guinea pig myocardial membrane preparations was 2.2 x 10/sup -8/M. In pharmacological experiments with non-labelled material and 60 min contact time, IIP produced a parallel shift in the orciprenaline concentration-response line on guinea-pig isolated tracheal and atrial preparations. The dissociation constant (Ksub(B) of IIP was 2.9 x 10/sup -8/M on atria (pA/sub 2/ 7.54) and 3.3 x 10/sup -8/M on trachea (PA/sub 2/ 7.48). These values indicate that IIP is not a selective B-adrenoceptor blocking drug. In addition, agreement was found between the affinity constant of this antagonist for B-adrenoceptors as determined by a direct binding study and an indirect pharmacological study.
Authors:
O'Donnell, S R; [1]  Woodcock, E A
  1. Queensland Univ., Brisbane (Australia). Dept. Of Physiology
Publication Date:
Feb 01, 1978
Product Type:
Journal Article
Reference Number:
AIX-09-386179; EDB-78-098582
Resource Relation:
Journal Name: J. Pharm. Pharmacol.; (United Kingdom); Journal Volume: 30:2
Subject:
59 BASIC BIOLOGICAL SCIENCES; 62 RADIOLOGY AND NUCLEAR MEDICINE; MYOCARDIUM; PHARMACOLOGY; TRACHEA; AMINES; BIOCHEMICAL REACTION KINETICS; COMPARATIVE EVALUATIONS; ETHERS; GUINEA PIGS; HEART; IN VITRO; IODINE 125; LABELLED COMPOUNDS; ORGANIC IODINE COMPOUNDS; PROPANOLS; SYMPATHOMIMETICS; TISSUES; UPTAKE; ALCOHOLS; ANIMALS; BETA DECAY RADIOISOTOPES; BODY; CARDIOVASCULAR SYSTEM; DAYS LIVING RADIOISOTOPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; HYDROXY COMPOUNDS; INTERMEDIATE MASS NUCLEI; IODINE ISOTOPES; ISOTOPES; KINETICS; MAMMALS; MUSCLES; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANIC HALOGEN COMPOUNDS; ORGANIC OXYGEN COMPOUNDS; ORGANS; RADIOISOTOPES; REACTION KINETICS; RESPIRATORY SYSTEM; RODENTS; VERTEBRATES; 550501* - Metabolism- Tracer Techniques; 550601 - Medicine- Unsealed Radionuclides in Diagnostics
OSTI ID:
6784792
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: JPPMA
Submitting Site:
INIS
Size:
Pages: 96-100
Announcement Date:
Jul 01, 1978

Journal Article:

Citation Formats

O'Donnell, S R, and Woodcock, E A. Comparison of the binding constant (Ksub(D)) of /sup 125/I-labelled 3-(4-iodophenoxy)-1-isopropylaminopropan-2-ol obtained on. beta. -adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Ksub(B)) obtained on guinea-pig isolated atria and trachea. United Kingdom: N. p., 1978. Web.
O'Donnell, S R, & Woodcock, E A. Comparison of the binding constant (Ksub(D)) of /sup 125/I-labelled 3-(4-iodophenoxy)-1-isopropylaminopropan-2-ol obtained on. beta. -adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Ksub(B)) obtained on guinea-pig isolated atria and trachea. United Kingdom.
O'Donnell, S R, and Woodcock, E A. 1978. "Comparison of the binding constant (Ksub(D)) of /sup 125/I-labelled 3-(4-iodophenoxy)-1-isopropylaminopropan-2-ol obtained on. beta. -adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Ksub(B)) obtained on guinea-pig isolated atria and trachea." United Kingdom.
@misc{etde_6784792,
title = {Comparison of the binding constant (Ksub(D)) of /sup 125/I-labelled 3-(4-iodophenoxy)-1-isopropylaminopropan-2-ol obtained on. beta. -adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Ksub(B)) obtained on guinea-pig isolated atria and trachea}
author = {O'Donnell, S R, and Woodcock, E A}
abstractNote = {The dissociation constant of binding (Ksub(D) of /sup 125/I-labelled 3-(4-iodophenoxy)-isopropylaminopropan-2-ol (IIP) to guinea pig myocardial membrane preparations was 2.2 x 10/sup -8/M. In pharmacological experiments with non-labelled material and 60 min contact time, IIP produced a parallel shift in the orciprenaline concentration-response line on guinea-pig isolated tracheal and atrial preparations. The dissociation constant (Ksub(B) of IIP was 2.9 x 10/sup -8/M on atria (pA/sub 2/ 7.54) and 3.3 x 10/sup -8/M on trachea (PA/sub 2/ 7.48). These values indicate that IIP is not a selective B-adrenoceptor blocking drug. In addition, agreement was found between the affinity constant of this antagonist for B-adrenoceptors as determined by a direct binding study and an indirect pharmacological study.}
journal = {J. Pharm. Pharmacol.; (United Kingdom)}
volume = {30:2}
journal type = {AC}
place = {United Kingdom}
year = {1978}
month = {Feb}
}