Buscopan labeled with carbon-14 and deuterium.

Hyosine butyl bromide, the active ingredient in Buscopan, is an anticholinergic and antimuscarinic drug used to treat pain and discomfort caused by abdominal cramps. A straightforward synthesis of carbon-14- and deuterium-labeled Buscopan was developed using scopolamine, n-butyl-1- C bromide, and n-butyl- H bromide, respectively. In a second carbon-14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety to follow its metabolism.

Radioimmunological determination of fenoterol. Part II: Antiserum and tracer for the determination of fenoterol.

A radioimmunological method for the determination of the concentration of fenoterol in biological samples is described. The mixture of antibodies against the enantiomers of fenoterol obtained with the selected hapten shows a high affinity for racemic fenoterol and for the monoiodo125-fenoterol used as a tracer, which is also present as a racemate. The limit of detection of the radioimmunoassay for fenoterol (racemate) in biological samples (plasma, urine) is 10-20 pg/ml.

Synthesis of the bronchospasmolytic agent flutropium bromide and of some homologous and configuration isomeric compounds.

A technically practicable synthesis of unknown N-beta-fluoroalkyl-substituted benzilic acid nortropine esters, among them (8r)-8-(2-fluoroethyl)-3 alpha-hydroxy-1 alpha H, 5 alpha H-tropanium bromide benzilic acid ester (flutropium bromide, Ba 598 BR), and their configuration isomeric quaternary salts via benzilic acid imidazolide is described. The quaternization which takes place with sufficiently high stereo-selectivity leads to configuration isomers which differ not only in their physico-chemical properties but also in their profile of pharmacological action.

Blood level, distribution, excretion, and metabolite pattern of [14C]-brotizolam in the rat, dog, and rhesus monkey.

Following oral and intravenous administration the absorption, distribution, metabolite pattern and excretion of 14C-labeled brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin), a new hypnotic, was studied in rats, dogs, and rhesus monkeys. Given orally to these species, [14C]-brotizolam was rapidly and extensively absorbed. The distribution of the radiolabeled drug was very fast indicated by blood level curves as well as by rat whole body autoradiography.