University of Minnesota

The State University of New York

University of California

Simon M Efange

Stanley M Parsons

Yung-Chi Cheng

Thomas J Bardos

Alan C Schroeder

A method for non-invasively mapping cholinergic innervation in a living brain comprises injecting the brain with a radiolabelled vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein 'azavesamicols' in which the cyclohexyl group of vesamicol is replaced with heterocycle of similar size, the piperidyl ring. The radiolabel is then detected externally with a photoscanning device.

Azavesamicols

The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein 'azavesamicols' in which the cyclohexyl group of vesamicol is replaced with a heterocycle of similar size, the piperidyl ring. The compounds bind to the vesamicol receptor, a cytoplasmically-oriented site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

Novel anticholinergics which are related to vesamicol are particularly useful when radiolabeled for evaluating cholinergic innervation in the living human brain. The cholinergic deficit in the Alzheimer's brain should be identifiable with these radioligands.

Radiopharmaceutical agents for the detection of Alzheimers disease

The compounds are vesamicol (hydroxylated phencyclidine (PCP) isomer trans-2-(4-phenyl-piperidino)cyclohexanol) derivatives with anticholinergic properties termed herein 'spirovesamicols' which are spirofused piperidines. The compounds bind to the vesamicol receptor, a site on the cholinergic synaptic vesicle, which is associated with the vesicular transporter of acetylcholine.

Spirovesamicols

Radiopharmaceutical agents for the detection of Alzheimer's disease

The nuceoside 1-(2-Deoxy-.beta.-D-ribofuranosyl)-5-(iodo)-2-pyrimidinone possesses a high level of antiviral activity and a low level of toxicity to the host cell making it an especially effective therapeutic agent for HSV-2.

5-ioso-2-pyrimidinone nucleoside

Compounds for inhibiting the replication of DNA viruses which induce the formation of thymidine kinase enzyme of the formula: ##STR1## wherein R.sub.1 is a radical selected from the group consisting of chloro, iodo, hydroxy, alkoxyalkyl, hydroxyalkyl, methylamino, formyl, nitro, and unsubstituted hydrocarbon groups of 2 to about 3 carbon atoms or halosubstituted hydrocarbon groups of 1 to about 3 carbon atoms; R.sub.2 is hydrogen or hydroxy; and R.sub.3 is hydroxy, --OP(O)(OH).sub.2, amino, or --OCOR.sub.4 where R.sub.4 is alkyl or alkoxyalkyl of 2 to about 18 carbon atoms.

Growing community of inventors

Plymouth, MN, United States of America

Simon M Efange