A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain

@article{Hellewell1990ASB,
  title={A sigma-like binding site in rat pheochromocytoma (PC12) cells: decreased affinity for (+)-benzomorphans and lower molecular weight suggest a different sigma receptor form from that of guinea pig brain},
  author={Susan B. Hellewell and Wayne D. Bowen},
  journal={Brain Research},
  year={1990},
  volume={527},
  pages={244-253}
}
Two highly selective radiolabeled probes for sigma receptors were found to bind with high affinity and capacity to membranes from undifferentiated PC12 cells. [3H]1,3-di-o-tolylguanidine [( 3H]DTG) bound with Kd = 23.7 +/- 4.6 nM and Bmax = 2025 +/- 660 fmol/mg protein. The Kd and Bmax for [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H](+)-3-PPP) were 86.3 +/- 21.6 nM and 1539 +/- 242 fmol/mg protein, respectively. These binding parameters were comparable to those observed in guinea… 
Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling
Rat liver and kidney were investigated for the presence of sigma (σ) receptor subtypes by radioligand binding with three highly selective σ probes and by photoaffinity labeling using
[3H]-(+)-pentazocine binding to sigma recognition sites in human cerebellum.
TLDR
The data suggest that [3H]-(+)-pentazocine labels sigma-1 sites in human cerebellum under appropriate assay conditions, and reversible binding with association and dissociation rate constants determined for two classes of sites is demonstrated.
[3H](+)-Pentazocine binding to rat brain σ1 receptors
Abstract [3H](+)-Pentazocine binding has been characterized in the rat brain. It binds to a single population of binding sites with affinity of about 7 nM and density of 280 fmol/mg protein.
Multiple [3H]DTG binding sites in guinea pig cerebellum: evidence for the presence of non-specific binding.
TLDR
A substantial component of 1,3-di(2-[5-3H]tolyl)guanidine binding in the guinea pig cerebellum is to non-specific, proteinaceous binding sites with some of the pharmacological characteristics of the sigma 2 binding site.
Autoradiographic distribution of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine (DTG) binding sites in guinea pig brain: a comparative study
TLDR
The distribution of [3H](+)-pentazocine binding sites in the guinea pig brain was examined using in vitro autoradiography and certain nuclei exhibited markedly different ratios of binding of the two ligands.
Comparison of binding parameters of σ1 and σ2 binding sites in rat and guinea pig brain membranes: novel subtype-selective trishomocubanes
Abstract Comparisons of binding parameters of [3H](+)-pentazocine and [3H]1,3-di-o-tolylguanidine (DTG) at σ binding sites in guinea pig and rat brain membranes demonstrated that [3H](+)-pentazocine
Is the sigma 2 receptor in rat brain related to the K+ channel of class III antiarrhythmic drugs?
TLDR
Evidence is provided that the (+)-[3H]-3-PPP binding sites in rat brain possess the characteristics of K+ channels of class III antiarrhythmic drugs.
(+)-[C-11]-cis-N-benzyl-normetazocine: a selective ligand for sigma receptors in vivo.
TLDR
The in vivo biodistribution profile of the novel sigma (sigma) receptor ligand (+)-[C-11]-cis-N-benzyl-normetazocine ([C- 11]-(+)-NBnNM) in mouse brain was examined and offers excellent potential to study sigma receptors in living human brain via positron emission tomography.
Functional assessment and partial characterization of [3H](+)-pentazocine binding sites on cells of the immune system
TLDR
Results indicate a stereoselective receptor for (+)-pentazocine which is coupled to biological processes of lymphocytes, and these compounds enhance or suppress lymphocyte proliferation depending on the mitogen and concentration of ligand.
Characterization of the binding of [3H](+)-pentazocine to σ recognition sites in guinea pig brain
Abstract The selective σ compound (+)-pentazocine was radiolabeled and its binding characteristics in guinea pig brain membranes were investigated. [ 3 H](+)-Pentazocine bound to a single
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