Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells

Bioorganic & Medicinal Chemistry Letters
2004.0

Abstract

The binding affinities of agonists at heteromeric nicotinic receptors composed of rat alpha2, alpha3 and alpha4 subunits in combination with beta2 or beta4 subunits were examined in stably transfected HEK 293 cells. In most cases, the affinities of agonists were higher at receptors composed of an alpha subunit in combination with the beta2 subunit than the beta4 subunit, and in some cases this difference was quite large (>250 times), suggesting the possibility of developing subtype-selective ligands and therapeutically useful drugs.

Knowledge Graph

Similar Paper

Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells
Bioorganic & Medicinal Chemistry Letters 2004.0
Ligand Selectivity for the Acetylcholine Binding Site of the Rat α4β2 and α3β4 Nicotinic Subtypes Investigated by Molecular Docking
Journal of Medicinal Chemistry 2005.0
Synthesis, Binding, and Modeling Studies of New Cytisine Derivatives, as Ligands for Neuronal Nicotinic Acetylcholine Receptor Subtypes
Journal of Medicinal Chemistry 2009.0
Epibatidine analogues as selective ligands for the αxβ2-containing subtypes of nicotinic acetylcholine receptors
Bioorganic & Medicinal Chemistry Letters 2005.0
Synthesis, Pharmacology, and Biostructural Characterization of Novel α<sub>4</sub>β<sub>2</sub>Nicotinic Acetylcholine Receptor Agonists
Journal of Medicinal Chemistry 2013.0
Preparation and affinity profile of novel nicotinic ligands
Bioorganic &amp; Medicinal Chemistry Letters 2008.0
bis-Azaaromatic quaternary ammonium analogues: ligands for α4β2* and α7* subtypes of neuronal nicotinic receptors
Bioorganic &amp; Medicinal Chemistry Letters 2002.0
Synthesis, Nicotinic Acetylcholine Receptor Binding Affinities, and Molecular Modeling of Constrained Epibatidine Analogues
Journal of Medicinal Chemistry 2003.0
Identification of 9-fluoro substituted (−)-cytisine derivatives as ligands with high affinity for nicotinic receptors
Bioorganic &amp; Medicinal Chemistry Letters 2010.0
Octahydropyrrolo[3,4-c]pyrrole: A Diamine Scaffold for Construction of Either α4β2 or α7-Selective Nicotinic Acetylcholine Receptor (nAChR) Ligands. Substitutions that Switch Subtype Selectivity
Journal of Medicinal Chemistry 2009.0