The effect of assay type and assay configuration on the pharmacological profile of a range of ligands acting at the D2 dopamine receptor was investigated in this thesis. The ligands explored have previously been shown to display a spectrum of efficacy at the D2 dopamine receptor. In competition ligand binding studies versus [³H]spiperone in HEK-293CREβlacD₂ˡ cell membranes, receptor-G protein coupling was increased in the absence of Na⁺, however the pK/ values for some agonists were higher in the presence of Na⁺, which suggested that different ligands are able to induce different receptor conformations.EThOS - Electronic Theses Online ServiceGBUnited Kingdo
The signalling of the D2 receptor (D2R), a G protein coupled receptor (GPCR), is a complex process c...
The search for synthetic selective compounds for G-protein-coupled receptors has provided a myriad o...
1 Mechanisms of inverse agonist action at the D-2(short) dopamine receptor have been examined. 2 Dis...
Background and purpose: Low efficacy partial agonists at the D-2 dopamine receptor may be useful for...
Dopamine (DA) is an endogenous neurotransmitter acting in the central nervous system. DA plays a key...
This study investigated, for the D-2 dopamine receptor, the relation between the ability of agonists...
In previous studies, we have shown that agonists influence the ability of D-2 dopamine receptors to ...
1 The human dopamine D-2long (D-2L) receptor was expressed with four different G proteins in Sf9 cel...
The dopamine D2 receptor (D2R) is known to elicit effects through activating two major signaling pat...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
1 Mechanisms of inverse agonist action at the D-2(short) dopamine receptor have been examined. 2 Di...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
The human D-2short (D-2S) dopamine receptor has been expressed together with the G proteins Gi2 and ...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
WT; [ H]spiperone binding studies showed a reduction in total number of binding sites (40%) but not...
The signalling of the D2 receptor (D2R), a G protein coupled receptor (GPCR), is a complex process c...
The search for synthetic selective compounds for G-protein-coupled receptors has provided a myriad o...
1 Mechanisms of inverse agonist action at the D-2(short) dopamine receptor have been examined. 2 Dis...
Background and purpose: Low efficacy partial agonists at the D-2 dopamine receptor may be useful for...
Dopamine (DA) is an endogenous neurotransmitter acting in the central nervous system. DA plays a key...
This study investigated, for the D-2 dopamine receptor, the relation between the ability of agonists...
In previous studies, we have shown that agonists influence the ability of D-2 dopamine receptors to ...
1 The human dopamine D-2long (D-2L) receptor was expressed with four different G proteins in Sf9 cel...
The dopamine D2 receptor (D2R) is known to elicit effects through activating two major signaling pat...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
1 Mechanisms of inverse agonist action at the D-2(short) dopamine receptor have been examined. 2 Di...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
The human D-2short (D-2S) dopamine receptor has been expressed together with the G proteins Gi2 and ...
Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge, given that a...
WT; [ H]spiperone binding studies showed a reduction in total number of binding sites (40%) but not...
The signalling of the D2 receptor (D2R), a G protein coupled receptor (GPCR), is a complex process c...
The search for synthetic selective compounds for G-protein-coupled receptors has provided a myriad o...
1 Mechanisms of inverse agonist action at the D-2(short) dopamine receptor have been examined. 2 Dis...