A radioreceptor assay for propranolol and 4-hydroxypropranolol. [Human]

Journal Article · Tue Jul 01 04:00:00 EDT 1980 · Clin. Pharmacol. Ther.; (United States)

DOI:https://doi.org/10.1038/clpt.1980.127· OSTI ID:5502945

Rochester, C L; Gammon, D E; Shane, E; Bilezikian, J P

A radioreceptor assay for the measurement or propranolol and 4-hydroxypropranoloel levels in plasma is described. Maximum sensitivity for propranolol was 1.2 +/- 0.15 ng/ml and for 4-hydroxypropranolol 4.2 +/- 0.4 ng/ml. Interassay and intra-assay variations for both were under 10%. Modifications in the radioreceptor assay permitted the measurements of total beta-adrenergic blocking activity and the separate contributions of parent drug and metabolite. When 4-hydroxypropranolol was stabilized, a composite level of total beta-adrenergic blocking activity in plasma was obtained. When the 4-hydroxy metabolite activity in plasma was oxidized, only the stable parent drug was detected. The differences in values between measurements made under these conditions was equivalent to the amount of 4-hydroxypropranolol in the sample. The radioreceptor assay was also used to measure the amount of free propranolol and 4-hydroxypropranolol. Under identical experimental conditions, more 4-hydroxypropranolol than propranolol circulated in the free form. These observations establish the feasibility of adapting the radioreceptor assay for propranolol to the measurement of total beta-adrenergic blocking activity and its components in plasma as well as to the measurement of free drug and metabolite levels.

• Research Organization: Columbia Univ. Coll. of Physicians and Surgeons, New York, NY
• OSTI ID: 5502945
• Journal Information: Clin. Pharmacol. Ther.; (United States), Journal Name: Clin. Pharmacol. Ther.; (United States) Vol. 28:1; ISSN CLPTA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
AUTONOMIC NERVOUS SYSTEM AGENTS
BIOLOGICAL MATERIALS
BLOOD
BLOOD PLASMA
BODY FLUIDS
DRUGS
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
MATERIALS
METABOLISM
METABOLITES
MODIFICATIONS
PATIENTS
RADIORECEPTOR ASSAY
SYMPATHOLYTICS
TRACER TECHNIQUES
VARIATIONS