Biomaterial Database

Radioreceptor assay for determination of the antimuscarinic drug ipratropium bromide in man. 1987

H A Ensinger, and D Wahl, and V Brantl

Department of Biochemistry, Boehringer Ingelheim KG, Ingelheim/Rhein, Federal Republic of Germany.

A radioreceptor assay for the determination of ipratropium bromide in human plasma has been developed, using [3H] N-methyl-scopolamine as a radioligand to label muscarinic cholinergic receptors in a membrane preparation of rat cerebral cortex. There was no interference due to the cross-reactivity of 3 metabolites of ipratropium with the parent compound (5.2, 1.5 and 0.004%, respectively). The validity of the assay was checked between 20 pg/ml and 1000 pg/ml drug. In a pilot study plasma levels following a single oral dose of 30 mg were determined to examine the applicability of the radioreceptor assay to clinical and pharmacokinetic studies, and for measurement of plasma levels after therapeutic oral doses. The peak plasma concentration in three healthy volunteers (means = 322 pg/ml) occurred within 1-3 h.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009241	Ipratropium	A muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.	N-Isopropylatropine,(endo,syn)-(+-)-3-(3-Hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-(1-methylethyl)-8-azoniabicyclo(3.2.1)octane,Atrovent,Ipratropium Bromide,Ipratropium Bromide Anhydrous,Ipratropium Bromide Monohydrate,Ipratropium Bromide, (endo,anti)-Isomer,Ipratropium Bromide, (exo,syn)-Isomer,Ipratropium Bromide, endo-Isomer,Itrop,Sch-1000,Sch-1178,N Isopropylatropine,Sch 1000,Sch 1178,Sch1000,Sch1178
D011869	Radioligand Assay	Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).	Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011976	Receptors, Muscarinic	One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.	Muscarinic Acetylcholine Receptors,Muscarinic Receptors,Muscarinic Acetylcholine Receptor,Muscarinic Receptor,Acetylcholine Receptor, Muscarinic,Acetylcholine Receptors, Muscarinic,Receptor, Muscarinic,Receptor, Muscarinic Acetylcholine,Receptors, Muscarinic Acetylcholine
D012044	Regression Analysis	Procedures for finding the mathematical function which best describes the relationship between a dependent variable and one or more independent variables. In linear regression (see LINEAR MODELS) the relationship is constrained to be a straight line and LEAST-SQUARES ANALYSIS is used to determine the best fit. In logistic regression (see LOGISTIC MODELS) the dependent variable is qualitative rather than continuously variable and LIKELIHOOD FUNCTIONS are used to find the best relationship. In multiple regression, the dependent variable is considered to depend on more than a single independent variable.	Regression Diagnostics,Statistical Regression,Analysis, Regression,Analyses, Regression,Diagnostics, Regression,Regression Analyses,Regression, Statistical,Regressions, Statistical,Statistical Regressions
D002540	Cerebral Cortex	The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulci. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.	Allocortex,Archipallium,Cortex Cerebri,Cortical Plate,Paleocortex,Periallocortex,Allocortices,Archipalliums,Cerebral Cortices,Cortex Cerebrus,Cortex, Cerebral,Cortical Plates,Paleocortices,Periallocortices,Plate, Cortical
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001286	Atropine Derivatives	Analogs and derivatives of atropine.	Atropines
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus