[HTML][HTML] Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor

S Bhagwanth, RK Mishra… - Beilstein journal of …, 2013 - beilstein-journals.org
A variety of stable, small-molecule peptidomimetic ligands have been developed to
elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH 2 (PLG) modulates …

Synthesis of an MIF-1 analogue containing enantiopure (S)-α-trifluoromethyl-proline and biological evaluation on nociception

I Jlalia, N Lensen, G Chaume, E Dzhambazova… - European Journal of …, 2013 - Elsevier
The synthesis and the effect of a novel MIF-1 analogue on nociception during acute pain in
rat model are reported. The synthesis of this enantiopure trifluoromethyl group containing …

PAOPA, a potent analogue of Pro-Leu-glycinamide and allosteric modulator of the dopamine D2 receptor, prevents NMDA receptor antagonist (MK-801)-induced …

B Dyck, K Guest, C Sookram, D Basu, R Johnson… - Schizophrenia …, 2011 - Elsevier
The aim of this study was to investigate whether a potent analogue of the endogenous brain
peptide l-prolyl-l-leucyl-glycinamide (PLG),(3 (R)-[(2 (S)-pyrrolidinylcarbonyl) amino]-2-oxo …

Microwave-assisted solution phase peptide synthesis in neat water

A Mahindra, K Nooney, S Uraon, KK Sharma, R Jain - RSC advances, 2013 - pubs.rsc.org
An environmentally benign protocol for solution phase peptide synthesis has been
developed in neat water using TBTU/HOBt/DIEA as a coupling combination under …

Effects of the dopamine D2 allosteric modulator, PAOPA, on the expression of GRK2, arrestin-3, ERK1/2, and on receptor internalization

D Basu, Y Tian, J Bhandari, JR Jiang, P Hui… - PLoS …, 2013 - journals.plos.org
The activity of G protein-coupled receptors (GPCRs) is intricately regulated by a range of
intracellular proteins, including G protein-coupled kinases (GRKs) and arrestins …

Preclinical pharmacokinetic and toxicological evaluation of MIF-1 peptidomimetic, PAOPA: examining the pharmacology of a selective dopamine D2 receptor allosteric …

ML Tan, D Basu, JM Kwiecien, RL Johnson, RK Mishra - Peptides, 2013 - Elsevier
Schizophrenia is a mental illness characterized by a breakdown in cognition and emotion.
Over the years, drug treatment for this disorder has mainly been compromised of orthosteric …

Transformation of Pro-Leu-Gly-NH2 Peptidomimetic Positive Allosteric Modulators of the Dopamine D2 Receptor into Negative Modulators

S Bhagwanth, S Mishra, R Daya, J Mah… - ACS Chemical …, 2012 - ACS Publications
The synthesis of dimethyl derivatives of 5.6. 5 spiro bicyclic lactam Pro-Leu-Gly-NH2
peptidomimetics was carried out to test the hypothesis that by placing methyl groups on the …

Effect of Chronic Treatment with D2 Allosteric Modulator PAOPA on the Expression of Cerebral Dopamine Neurotrophic Factor (CDNF) in Select Brain Regions

Y Tian, R Daya, J Bhandari, H Joshi… - International Journal of …, 2021 - Springer
Impairment in dopaminergic pathways has been implicated in several detrimental
neuropsychiatric and neurodegenerative disorders, including schizophrenia and …

Change in expression of vesicular protein synapsin II by chronic treatment with D2 allosteric modulator PAOPA

D Basu, Y Tian, P Hui, J Bhandari, RL Johnson… - Peptides, 2015 - Elsevier
The hallmark symptoms of schizophrenia include profound disturbances in thought,
perception, cognition etc., which negatively impacts an individual's quality of life. Current …

[引用][C] Characterization of the Mechanism of Action for Novel Dopamine D2 Receptor Allosteric Modulators

D Basu - 2013