Discovery of novel adenosine receptor agonists that exhibit subtype selectivity

A Knight, JL Hemmings, I Winfield… - Journal of medicinal …, 2016 - ACS Publications
novel synthetic adenosine derivatives for their agonist activity against the A 1 R, A 2A R,
and A 2B R. We explored subtype … cell assays have identified novel adenosine nucleosides …

Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity

J Roppe, ND Smith, D Huang, L Tehrani… - Journal of medicinal …, 2004 - ACS Publications
… In conclusion, a series of novel non-alkyne mGlu5 receptor antagonists have been discovered.
Tetrazole derivatives 47 and 48 have a profile comparable with that of alkyne derivative …

Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral …

AL Rodriguez, MD Grier, CK Jones, EJ Herman… - Molecular …, 2010 - ASPET
discovery of multiple novel scaffolds possessing diverse activities as mGluR5 allosteric
modulators. These novel … Furthermore, these novel compounds are active in vivo and show that …

Molecular Modeling of the Three-Dimensional Structure of Dopamine 3 (D3) Subtype Receptor:  Discovery of Novel and Potent D3 Ligands through a Hybrid …

J Varady, X Wu, X Fang, J Min, Z Hu… - Journal of medicinal …, 2003 - ACS Publications
… approach to discover novel D 3 ligands. Using this approach, we were able to discover 4 …
of 20 compounds selected for testing in the D 3 receptor binding assay. Testing of eight other …

Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists

V Katritch, VP Jaakola, JR Lane, J Lin… - Journal of medicinal …, 2010 - ACS Publications
… The virtual screening in this study did not explicitly target subtype selectivity, yielding hits
that bind equally well to both A2A and A1 adenosine receptor subtypes. Most hit compounds, …

Discovery and Characterization of Novel Subtype-Selective Allosteric Agonists for the Investigation of M1 Receptor Function in the Central Nervous System

EP Lebois, TM Bridges, LM Lewis… - ACS chemical …, 2010 - ACS Publications
subtype for memory and attention mechanisms. Unfortunately, it has been difficult to develop
selective activators of M 1 and other individual mAChR subtypes, … have discovered a novel

Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist

HP Nothacker, Z Wang, Y Zhu, RK Reinscheid… - Molecular …, 2000 - ASPET
… characterization of a novel human CysLT receptor subtype that we have named the CysLT
2 receptor and report the tissue distribution of its expression. The receptor shows a selective …

Discovery of novel melanocortin4 receptor selective MSH analogues

HB Schiöth, F Mutulis, R Muceniece… - British journal of …, 1998 - Wiley Online Library
… 4 receptor selectivity. The preference order of the different MC receptor subtypes for the novel
[… as they bind the MC 4 receptor with high and the MC 1 receptor with low relative affinities. …

Angiotensin receptor subtype mediated physiologies and behaviors: new discoveries and clinical targets

JW Wright, BJ Yamamoto, JW Harding - Progress in neurobiology, 2008 - Elsevier
… degradation of active angiotensin peptides and three receptor subtypes (AT 1 , AT 2 and AT
… recently discovered receptor subtype, AT 4 . Descriptions of classic and novel physiologies …

Receptor subtypes or species homologues: relevance to drug discovery

JM Hall, MP Caulfield, SP Watson, S Guard - Trends in pharmacological …, 1993 - cell.com
… encoded by the rat gene rg.20, and it has been suggested that this represents a novel
receptor subtype - the CQDadrenoeepto?‘. On the other hand, rg2U shares greater than 90% se…