The influence of different cellular environments on PET radioligand binding: an application to D2/3-dopamine receptor imaging.
Bottom Line: Extension of in vivo competition imaging to other receptor systems has been relatively unsuccessful.These studies suggest that sensitivity to endogenous dopamine release in vivo is related to a decrease in affinity in the endosomal environment compared with those found at the cell surface.This pharmacological approach is fully translatable to other receptor systems.
Affiliation: Centre for Neuropsychopharmacology, Division of Brain Sciences, Imperial College London, UK. Electronic address: firstname.lastname@example.org.Show MeSH
Mentions: When both “Percentage Bound per Fraction” and “Percentage Total Protein per Fraction” are both taken into account i.e. using Equation (3), relative specific activity (RSA) values are generated. The total striatal homogenate RSA values for [3H]spiperone were found to be significantly greater than those obtained for both [3H]raclopride and [3H]PhNO (Fig. 1A, Table 3). Similar to the distribution of “Percentage total homogenate Bound per Fraction”, RSA distribution was highest in the P2-plasma membrane fraction for all ligands (Table 3).
Affiliation: Centre for Neuropsychopharmacology, Division of Brain Sciences, Imperial College London, UK. Electronic address: email@example.com.