Abstract: The invention relates to radioactively labeled derivatives of (R)-1-(1-phenylethyl)-1H-imidazole-5-carboxylic acid esters, uses, and methods for preparing these compounds.

Abstract: Compounds derived from phenylethyl imidazole carboxylic acid esters have shown selective accumulation of radioactivity in the adrenal cortex, when labeled with a radioactive halogen. In particular, these compounds bind selectively to adrenocortical tissue facilitating the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Trace amounts are injected intravenously and accumulate rapidly in the adrenals, maintaining a high radioactivity plateau, which permits external imaging using computed SPECT (single photon emission) or PET (positron emission) techniques. Independent of the position and type of the radioactive label, the compounds according to the invention are potent inhibitors of steroid P450c11 hydroxylation and bind with high affinity on sites of cortisol secretion. In order to avoid saturation of receptor sites, high specific activity labeling is mandatory for application in patients.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: The subject matter of this invention is a process for solid albumin particles so that such spheric particles may act as a carrier for radioactivity, drugs, insecticides, dyes, metal salts, etc. In order to prepare such spheric particles, the substance to be incorporated therein is transformed into a precipitate. This precipitate is then mixed with an aqueous solution of albumin. The mixture thus prepared is then injected into cotton seed oil while stirring so as to obtain a fine dispersion of the albumin droplets and the precipitate in the oil, then the mixture is heated above 100.degree.C to evaporate water and to form spheric albumin particles having the precipitate encapsulated therein.