The Mclean Hospital Corporation

Northeastern University

Neuro Imaging Technologies, LLC

Research Biochemicals Limited Partnership

The Brigham and Women's Hospital, Inc.

The United States of America As Represented by the Department of Health

University of Rochester

Amersham Plc

Astra Pharmaceutical Products, Inc.

Ge Healthcare Limited

John L Neumeyer

Richard A Milius

Robert B Innis

Ross J Baldessarini

Yu-Gui Si

Xiao-Hui Gu

Jean M Bidlack

Anna Waclawa Sromek

Gilles Tamagnan

Shaoyin Wang

Kenneth Alan Jacobson

John W Daly

Sandor Szabo

Gilles D Tamagnan

Ao Zhang

Yigong Gao

Paul Andre Tenthorey

Philip LeQuesne

Wolfgang Pfleidover

The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind Dreceptors. The compounds are useful for imaging Dreceptors and for the treatment of diseases, such as Parkinson's disease, sexual dysfunction, and depressive disorders.

2-alkoxy-11-hydroxyaporphine derivatives and uses thereof

The invention features derivatives of R(&#x2212;)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease and sexual dysfunction therewith.

R(&#x2212;)-2-methoxy-11-hydroxyaporphine and derivatives thereof

The invention features derivatives of R(&#x2212;)-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

R(&#x2212;)-11-hydroxyaporphine derivatives and uses thereof

The invention features derivatives of R(&#x2014;)-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

R(&#x2014;)-11-hydroxyaporphine derivatives and uses thereof

The invention is based in part on the discovery that nonselective &#x3ba; agonists that possess &#x3bc; receptor-mediated effects in addition to their &#x3ba; agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective &#x3ba; agonists. The invention includes a number of new compounds having both nonselective &#x3ba; opioid receptor agonist activity and additional activity at &#x3bc; opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Treatment of cocaine abuse using N-substituted derivatives of morphinan

This invention features opioid compounds having activity at kappa and mu receptors, methods for preparing the mu/kappa opioids, and methods for the treatment of pain or a dopamine dysregulation disease, such as schizophrenia, attention deficit hyperactivity disorder (ADHD), attention deficit hyperactivity disorder (ADD), Parkinson's disease, hyperprolactinemia, depression, and addiction.

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N-substituted derivatives of morphinan and uses thereof

Iodinated neuroprobes for mapping monoamine reuptake sites in the brain, and particularly iodinated neuroprobes that can also serve as radiotracers for use in single-photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging of such reuptake sites, are disclosed. Precursors of radiolabeled iodinated neuroprobes, both with and without a radiotracer atom, and kits for preparing the radiolabeled iodinated neuroprobes are also disclosed.

Neuroprobes for mapping monoamine reuptake sites

An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein R= ##STR2## wherein n=2-8; R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; and X=an isotope of Cl, an isotope of Br, an isotope of F, an isotope of I, or Sn(R'.sub.1 R'.sub.2 R'.sub.3), wherein

Halogenated neuroprobe for mapping monoamine reuptake sites

Neuroprobes that include rhenium, manganese, and technetium for use in mapping monoamine reuptake sites are disclosed. Non-radioactive tricarbonylrheniumcyclopentadienyl (TRCp) or non-radioactive tricarbonylmanganesecyclopentadienyl (TMCp) phenyltropane analogs are synthesized for use as testing surrogates for radioactive technetium congeners. Ferrocenyl analogs of phenyltropane are disclosed as useful precursors for the preparation of novel tricarbonyltechnetiumcyclopentadienyl (TTCp) phenyltropane analogs in radioactive form.

Synthesis of ferrocenyl phenyltropane analogs and their

An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein: R=aryl, substituted aryl, heterocyclic, CO(CH.sub.2).sub.n Y, (CH.sub.2).sub.n CHF.sub.2, and (CF.sub.2).sub.n Y, wherein:

Iodinated neuroprobe for mapping monoamine reuptake sites

The present invention provides sulfur-containing xanthine derivatives which are 1,3-disubstituted with a C.sub.1 -C.sub.12 alkyl, which may be further substituted with a hydroxy, amino, or halo group, and are 8-substituted with either a cycloalkyl, furyl, thienyl, or substituted phenyl group. These derivatives possess increased selectivity or potency at adenosine receptors.

Sulfur-containing xanthine derivatives as adenosine antagonists

An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein R=a C.sub.n H.sub.2n+1 group where n=0-6, an alkenyl group, a monofluoroalkyl group including .sup.n F where n=18 or 19, or a .sup.m C.sub.n H.sub.2n+1 group where n=1-6 and where m=11 or 14 for at least one .sup.m C;

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Wayland, MA, United States of America

John L Neumeyer