A comparison of the binding constant (Kd) of 125I-labelled 3-(4-iodophenoxy)-1-isopropylamino-propan-2-ol obtained on β-adrenoceptors in guinea-pig myocardial membranes, with its dissociation constants (Kb) obtained on guinea-pig isolated atria and trachea
- 1 September 1978
- journal article
- research article
- Published by Oxford University Press (OUP) in Journal of Pharmacy and Pharmacology
- Vol. 30 (1), 96-100
- https://doi.org/10.1111/j.2042-7158.1978.tb13170.x
Abstract
The dissociation constant of binding (KD) of 125I-labelled 3-(4-iodophenoxy)-1-isopropyl-aminopropan-2-ol (IIP) to guinea-pig myocardial membrane preparations was 2·2 × 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 × 10−8m on atria (pA2 7·54) and 3·3 × 10−8m on trachea (pA2 7·48). These values indicate that IIP is not a selective β-adrenoceptor blocking drug. In addition, agreement was found between the affinity constant of this antagonist for β-adrenoceptors as determined by a direct binding study and an indirect pharmacological study.This publication has 16 references indexed in Scilit:
- The preparation and purification of 3-(4-iodophenoxy)-1-isopropylamino-2-propanol-125I, a beta adrenergic antagonistJournal of Labelled Compounds and Radiopharmaceuticals, 1977
- THE CONTRIBUTION OF EXTRANEURONAL UPTAKE TO THE TRACHEA‐BLOOD VESSEL SELECTIVITY OF β‐ADRENOCEPTOR STIMULANTS in vitro IN GUINEA‐PIGSBritish Journal of Pharmacology, 1976
- Identification of adenylate cyclase-coupled beta-adrenergic receptors with radiolabeled beta-adrenergic antagonistsBiochemical Pharmacology, 1975
- POTENCY AND SELECTIVITYin vitroOF COMPOUNDS RELATED TO ISOPRENALINE AND ORCIPRENALINE ON β‐ADRENOCEPTORS IN THE GUINEA‐PIGBritish Journal of Pharmacology, 1974
- Thyroid-stimulating Hormone Binding to Beef Thyroid MembranesPublished by Elsevier ,1974
- Factors influencing observed β-adrenergic receptor antagonism in guinea-pig tracheaEuropean Journal of Pharmacology, 1974
- 1‐Isopropylamino‐3‐(4‐indanoxy)‐2‐propanol HCl: a potent β‐adrenoceptor antagonistBritish Journal of Pharmacology, 1970
- The interaction of cocaine and propranolol with catecholamines on guinea pig tracheaEuropean Journal of Pharmacology, 1967
- EVALUATION OF THE CARDIAC EFFECTS OF SEVERAL BETA ADRENERGIC BLOCKING AGENTSAnnals of the New York Academy of Sciences, 1967
- THE PHARMACOLOGICAL DIFFERENTIATION OF ADRENERGIC RECEPTORS*Annals of the New York Academy of Sciences, 1967