scholarly journals Erratum to: Somatostatin receptor sst1–sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands

2001 ◽  
Vol 28 (9) ◽  
pp. 1433-1433
Author(s):  
Jean Reubi ◽  
Beatrice Waser ◽  
Jean-Claude Schaer ◽  
Jean A. Laissue
Keyword(s):  
Somatostatin Receptor ◽  
Receptor Autoradiography ◽  
Human Tissues ◽  
Selective Ligands ◽  
Subtype Selective

Differential α2A- and α2C-adrenoceptor protein expression in presynaptic and postsynaptic density fractions of postmortem human prefrontal cortex

2018 ◽  
Vol 33 (2) ◽  
pp. 244-249 ◽  
Author(s):  
Amaia M Erdozain ◽  
Iria Brocos-Mosquera ◽  
Ane M Gabilondo ◽  
J Javier Meana ◽  
Luis F Callado
Keyword(s):  
Prefrontal Cortex ◽  
Protein Expression ◽  
Therapeutic Potential ◽  
Postsynaptic Density ◽  
Subcellular Fractionation ◽  
Similar Distribution ◽  
Density Fractions ◽  
Physiological Relevance ◽  
Selective Ligands ◽  
Subtype Selective

Background: Three different α2-adrenoceptor (α2-AR) subtypes have been described. The α2A-AR and α2C-AR subtypes are highly expressed in the human prefrontal cortex, where they modulate neurotransmission. However, due to the lack of subtype-selective ligands, the physiological relevance of both subtypes has not been fully resolved. Aims: In this context, the aim of the present study was to characterize the protein expression of both α2-AR subtypes, in different synaptic fractions of postmortem human prefrontal cortex. Methods: A subcellular fractionation of the samples was performed and the protein expression of α2A- and α2C-ARs was measured in presynaptic membranes and postsynaptic density fractions by Western blot. Results: The results revealed that the α2A-AR subtype is mainly located postsynaptically (95±3%) whereas the remaining 5±3% is in the presynapse. Conversely, the α2C-AR subtype showed a similar distribution between pre- and postsynaptic membranes, with a slightly higher percentage present in the presynapse (60±2% vs. 40±2%). Conclusions: These findings could explain some contradictory effects reported for α2-AR agonists and antagonists in the human prefrontal cortex. Furthermore, the present data could contribute to elucidating the therapeutic potential of selectively targeting α2A- or α2C-AR subtypes.

Highly Potent and Subtype Selective Ligands Derived byN-Methyl Scan of a Somatostatin Antagonist

2001 ◽  
Vol 44 (8) ◽  
pp. 1305-1311 ◽  
Author(s):  
W. G. Rajeswaran ◽  
Simon J. Hocart ◽  
William A. Murphy ◽  
John E. Taylor ◽  
David H. Coy
Keyword(s):  
Selective Ligands ◽  
Somatostatin Antagonist ◽  
Subtype Selective

Somatostatin receptor incidence and distribution in breast cancer using receptor autoradiography: Relationship to egf receptors

1990 ◽  
Vol 46 (3) ◽  
pp. 416-420 ◽  
Author(s):  
J. C. Reubi ◽  
B. Waser ◽  
J. A. Foekens ◽  
J. G. M. Klijn ◽  
S. W. J. Lamberts ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Somatostatin Receptor ◽  
Receptor Autoradiography ◽  
Egf Receptors

Synthesis and biological evaluation of novel cyclopropyl derivatives as subtype-selective ligands for estrogen receptor

2018 ◽  
Vol 70 (7) ◽  
pp. 910-918 ◽  
Author(s):  
Zunyuan Wang ◽  
Yewei Yang ◽  
Xiaoliang Zheng ◽  
Tao Zhang ◽  
Wenhai Huang ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Biological Evaluation ◽  
Selective Ligands ◽  
Subtype Selective ◽  
Synthesis And Biological Evaluation

Serotonergic modulation of neuronal activity in rat midbrain periaqueductal gray

2013 ◽  
Vol 109 (11) ◽  
pp. 2712-2719 ◽  
Author(s):  
Hyo-Jin Jeong ◽  
Karen Lam ◽  
Vanessa A. Mitchell ◽  
Christopher W. Vaughan
Keyword(s):  
Brain Slices ◽  
Periaqueductal Gray ◽  
Membrane Excitability ◽  
Inhibitory Effects ◽  
Whole Cell Patch Clamp ◽  
Outward Currents ◽  
Selective Ligands ◽  
Inward Currents ◽  
Subtype Selective ◽  
Serotonergic Modulation

Serotonin (5-HT) modulates pain and anxiety from within the midbrain periaqueductal gray (PAG). In the present study, the effects of 5-HT- and 5-HT1/2 subtype-selective ligands on rat PAG neurons were examined using whole cell patch-clamp recordings in brain slices. In voltage clamp, 5-HT produced outward and inward currents in distinct subpopulations of neurons that varied throughout different subregions of the PAG. The 5-HT1A agonist R(+)-8-OH-DPAT (1 μM) produced outward currents in subpopulations of PAG neurons. By contrast, sumatriptan (1 μM) and other 5-HT1B, -D, and -F subtype agonists had little or no postsynaptic activity. The 5-HT2A/C agonists DOI (3 μM) and TCB-2 (1 μM) produced inward currents in subpopulations of PAG neurons, and DOI enhanced evoked inhibitory postsynaptic currents via a presynaptic mechanism. In current clamp, both R(+)-8-OH-DPAT and sumatriptan produced an excitatory increase in evoked mixed postsynaptic potentials (PSPs). In addition, R(+)-8-OH-DPAT, but not sumatriptan, directly hyperpolarized PAG neurons. By contrast, the 5-HT2 agonist DOI depolarized subpopulations of neurons and produced an inhibitory decrease in evoked mixed PSPs. These findings indicate that 5-HT1A and 5-HT1B/D ligands have partly overlapping inhibitory effects on membrane excitability and synaptic transmission within the PAG, which are functionally opposed by 5-HT2A/C actions in specific PAG subregions.

Deciphering the specific role of Gαi/o isoforms: functional selective oxytocin ligands and somatostatin SST5 receptor mutants

2013 ◽  
Vol 41 (1) ◽  
pp. 166-171 ◽  
Author(s):  
Marta Busnelli ◽  
Erika Peverelli ◽  
Giovanna Mantovani ◽  
Anna Spada ◽  
Bice Chini
Keyword(s):  
Somatostatin Receptor ◽  
Receptor Activation ◽  
G Protein Coupled Receptors ◽  
Receptor Coupling ◽  
Biological Responses ◽  
Selective Ligands ◽  
Specific Effector ◽  
G Protein Coupled

Receptor coupling to different G-proteins and β-arrestins has been described for a number of GPCRs (G-protein-coupled receptors), suggesting a multi-state model of receptor activation in which each receptor can assume a number of different active conformations, each capable of promoting the coupling to a specific effector. Consistently, functional-selective ligands and biased agonists have been described to be able to induce and/or stabilize only a subset of specific active conformations. Furthermore, GPCR mutants deficient in selective coupling have been reported. Functional selective ligands and receptor mutants thus constitute unique tools to dissect the specific roles of different effectors, in particular among the Gi/o family. In the present mini-review, we focus on (i) the identification of functional selective OXT (oxytocin)-derived peptides capable of activating single Gi/o isoforms, namely Gi1 or Gi3; and (ii) the characterization of an SS (somatostatin) receptor SST5 mutant selectively impaired in its GoA coupling. These analogues and receptor mutants represent unique tools for examining the contribution of Gi/o isoforms in complex biological responses and open the way for the development of drugs with peculiar selectivity profiles.

Somatostatin receptor subtype expression in human tissues: a prediction for diagnosis and treatment of cancer?

1997 ◽  
Vol 27 (8) ◽  
pp. 645-647 ◽  
Author(s):  
I. VIRGOLINI ◽  
T. PANGERL ◽  
C. BISCHOF ◽  
P. SMITH-JONES ◽  
M. PECK-RADOSAVLJEVIC
Keyword(s):  
Somatostatin Receptor ◽  
Diagnosis And Treatment ◽  
Receptor Subtype ◽  
Human Tissues
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