Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors

…, HA Ensinger, CL Chio, ME Lajiness… - European Journal of …, 1995 - Elsevier
Pramipexole (SND 919; 2-amino-4,5,6,7-tetrahydro-6-propylamino-benzthiazole-dihydrochloride)
is a potent dopamine autoreceptor agonist. We have carried out an analysis of the …

Activation of heterologously expressed D3 dopamine receptors: comparison with D2 dopamine receptors.

CL Chio, ME Lajiness, RM Huff - Molecular pharmacology, 1994 - ASPET
Recombinant rat D3 dopamine receptors heterologously expressed in Chinese hamster
ovary (CHO) cells are functionally coupled to endogenous G proteins. The affinity of the …

Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine d3 receptor-selective agonist (4a r, 10b r)-(+)-trans-3, 4, 4a, 10b-tetrahydro-4-n …

…, TG Heffner, LD Wise, ME Lajiness… - Journal of medicinal …, 2000 - ACS Publications
Benzopyranoxazine (+)-7 (PD 128907) is the most dopamine (DA) D 3 receptor-selective
agonist presently known. The only structural feature which distinguishes 7 from the analogous …

Dopamine D3 Receptor Antagonists. 1. Synthesis and Structure−Activity Relationships of 5,6-Dimethoxy-N-alkyl- and N-Alkylaryl-Substituted 2-Aminoindans

…, CL Haber, RM Huff, ME Lajiness… - Journal of medicinal …, 2001 - ACS Publications
5,6-Dimethoxy-2-(N-dipropyl)-aminoindan (3, PNU-99194A) was found to be a selective
dopamine D 3 receptor antagonist with potential antipsychotic properties in animal models. To …

Somatic mutations in GRM1 in cancer alter metabotropic glutamate receptor 1 intracellular localization and signaling

JL Esseltine, MD Willard, IH Wulur, ME Lajiness… - Molecular …, 2013 - ASPET
The activity of metabotropic glutamate receptors (mGluRs) is known to be altered as the
consequence of neurodegenerative diseases such as Alzheimer, Parkinson, and Huntington …

[HTML][HTML] Assay Guidance Manual

KE Garbison, BA Heinz, ME Lajiness… - Eli Lilly & Company …, 2004 - europepmc.org
This eBook is a comprehensive, crucial resource for investigators optimizing assays to
evaluate collections of molecules with the overall goal of developing probes that modulate the …

[PDF][PDF] D2 dopamine receptor stimulation of mitogenesis in transfected Chinese hamster ovary cells: relationship to dopamine stimulation of tyrosine phosphorylations.

ME Lajiness, CL Chio, RM Huff - Journal of Pharmacology and …, 1993 - Citeseer
Several neurotransmitters that act through G protein-linked receptors have been shown to
affect the growth rate of dividing cells. An analysis of the early signaling events that mediate …

Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists

…, TG Heffner, LD Wise, ME Lajiness… - Journal of medicinal …, 2000 - ACS Publications
The 2-aminothiazole moiety has proven its value in medicinal chemistry as a stable and
lipophilic bioisosteric replacement of a phenol group. This approach has provided dopamine (DA…

Signal transduction pathways modulated by D2-like dopamine receptors

RM Huff, CL Chio, ME Lajiness, LV Goodman - Advances in pharmacology, 1997 - Elsevier
Publisher Summary he D2-like subfamily of dopamine receptors is a target for drugs used to
treat Parkinson's disease and schizophrenia. Dopamine receptors regulate ion channels to …

Somatic mutations in CCK2R alter receptor activity that promote oncogenic phenotypes

MD Willard, ME Lajiness, IH Wulur, B Feng… - Molecular Cancer …, 2012 - AACR
The roles of cholecystokinin 2 receptor (CCK2R) in numerous physiologic processes in the
gastrointestinal tract and central nervous system are well documented. There has been some …