Determination of in vivo Bmax and Kd for 11C-GR103545, an agonist PET tracer for κ-opioid receptors: a study in nonhuman primates

…, D Weinzimmer, J Ropchan, L Blumberg… - Journal of Nuclear …, 2013 - Soc Nuclear Med
The κ-opioid receptors (KOR) are involved in mood disorders and addictive conditions. In
vivo imaging studies of this receptor in humans have not been reported because of the lack of …

[11C] GR103545: novel one-pot radiosynthesis with high specific activity

…, J Ropchan, D Labaree, YS Ding, L Blumberg… - Nuclear medicine and …, 2011 - Elsevier
INTRODUCTION: GR103545 is a potent and selective kappa-opioid receptor agonist.
Previous studies in non-human primates demonstrated favorable properties of [ 11 C]GR103545 …

Prodrugs of pioglitazone for extended-release (XR) injectable formulations

CN Sanrame, JF Remenar, LC Blumberg… - Molecular …, 2014 - ACS Publications
N-Acyloxymethyl derivatives of pioglitazone (PIO) have been prepared and characterized
as model candidates for extended-release injectable formulations. All PIO derivatives …

Structure–activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor

AS Antipas, LC Blumberg, WH Brissette… - Bioorganic & medicinal …, 2010 - Elsevier
Blumberg † , William H. Brissette , Matthew F. Brown , Jeffrey M. … MJ Munchhof, YA
Abramov, AS Antipas, LC Blumberg, WH Brissette, MF Brown, JM Casavant, JL Doty, J …

Chemoselective 1, 3-dipolar cycloadditions of azomethine ylide with conjugated dienes

LC Blumberg, B Costa, R Goldstein - Tetrahedron Letters, 2011 - Elsevier
Methods are described of synthesizing various 3-carboxy-4-vinyl pyrrolidines, versatile
building blocks for our drug discovery efforts. The 1,3-dipolar cycloaddition between activated …

Piperazinyl CCR1 antagonists—optimization of human liver microsome stability

MF Brown, KB Bahnck, LC Blumberg… - Bioorganic & medicinal …, 2007 - Elsevier
Piperazinyl CCR1 antagonists—optimization of human liver microsome stability - ScienceDirect
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Pyrimidine benzamide-based thrombopoietin receptor agonists

…, Q Li, F Zhang, AS Antipas, LC Blumberg… - Bioorganic & medicinal …, 2007 - Elsevier
A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The
lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been …

The identification of orally bioavailable thrombopoietin agonists

MJ Munchhof, AS Antipas, LC Blumberg… - Bioorganic & Medicinal …, 2009 - Elsevier
Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor
agonists. Unfortunately, the structural features required for the desired activity conferred …

Novel N-5-(acyloxyalkoxy) carbonyl prodrugs of olanzapine with physicochemical properties for extended-release

LC Blumberg, TA Zeidan, A Maddaford, NC Warren… - RSC …, 2013 - pubs.rsc.org
An unexpected regioisomer was observed during the synthesis of olanzapine prodrugs. N-5-(acyloxyalkoxy)carbonyl-functionalized
olanzapine derivatives were found to have …

Differential effects of opioid receptor modulators on motivational and stress-coping behaviors in the back-translational rat IFN-α depression model

…, MN Islam, DJ Eyerman, KL Smith, L Blumberg… - bioRxiv, 2019 - biorxiv.org
Rationale Many patients respond inadequately to antidepressant drug treatment; the search
for alternate pharmacological treatment mechanisms is ongoing. Until the 1950’s, opium …