PMID: 24112Feb 1, 1978

A comparison of the binding constant (KD) of 125I-labelled 3-(4-iodophenoxy)-1-isopropylamino-propan-2-ol obtained on beta-adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (KB) obtained on guinea-pig isolated atria and trachea

The Journal of Pharmacy and Pharmacology
S R O'Donnell, E A Woodcock

Abstract

The dissociation constant of binding (KD) of 125I-labelled 3-(4-iodophenoxy)-1-isoproplyaminopropan-2-ol (IIP) to guinea-pig myocardial membrane preparations was 2.2 x 10-8M. In pharmacological experiments with the 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 (KB) of IIP was 2.9 x 10-8M on atria (pA2 7.54) and 3.3 x 10-8M on trachea (pA2 7-48). These values indicate that IIP is not a selective beta-adrenoceptor blocking drug. In addition, agreement was found between the affinity constant of this antagonist for beta-adrenoceptors as determined by a direct binding study and an indirect pharmacological study.

References

May 1, 1974·European Journal of Pharmacology·C K BucknerM O'Connor
Feb 10, 1967·Annals of the New York Academy of Sciences·J R Blinks
May 1, 1970·British Journal of Pharmacology·B Levy, M Wasserman
Feb 10, 1967·Annals of the New York Academy of Sciences·R F Furchgott
Nov 1, 1967·European Journal of Pharmacology·L A Chahl, S R O'Donnell

Related Concepts

Adrenergic beta-Antagonists
Cavia porcellus
Iodobenzenes
Tissue Membrane
Myocardium
Propanolamines
Norepinephrine Receptors
Beta-adrenergic receptor
Trachea

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