Receptor distribution studies

Carletti, Renzo; Tacconi, Stefano; Mugnaini, Manolo; Gerrard, Philip

doi:10.1016/j.coph.2017.07.008

Cited by 8 publications

(6 citation statements)

References 67 publications

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“…Nowadays, tomographic methods like positron emission tomography (PET) or single photon emission computed tomography (SPECT) turned into a routine technique for assessing tissue distribution and in vivo receptor occupancy of advanced clinical candidates. [30] However, radioactive synthesis has its specific peculiarities and can clearly not be performed early stages of drug discovery. Also it can deliver valuable information on target and drug distribution patterns as well as snapshots of binding of the drug candidate to specific targets or off-targets, but is not ideally suited for monitoring pharmacodynamics drug responses in chronic studies due to the damaging effects of radioactivity.…”

Section: In Vivo Imaging Of Drug Actionmentioning

confidence: 99%

The Impact of Chemical Biology on Drug Discovery

Plettenburg

2019

Israel Journal of Chemistry

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Section: In Vivo Imaging Of Drug Actionmentioning

confidence: 99%

The Impact of Chemical Biology on Drug Discovery

Plettenburg

2019

Israel Journal of Chemistry

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“…The lipid bilayer provides the membrane with fluidity and elasticity. Studying lipid rafts present on cell surface proteins can provide detailed information on their functionality, e.g., T‐cell signaling, treatment of viral infection, receptor‐mediated channel activity, and therapeutic targets for cancer (Bobkov & Semenova, 2022; Carletti et al., 2017; Codini et al., 2021; Gold & Reth, 2019; Li et al., 2022; Magee et al., 2002; Nagy et al., 2001).…”

Section: Introductionmentioning

confidence: 99%

Novel Transmission Electron Microscopic Method to Quantify Protein Clustering on the Cell Surface

Kormos,

Daróczi,

Szöllősi

et al. 2024

Current Protocols

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The cell surface distribution patterns (clustering) of membrane proteins have been widely investigated in cell biology. Here we describe a novel transmission electron microscopic (TEM) protocol designed to improve the quality of information obtained about the protein distribution patterns detected. This novel method makes it possible to study the clustering of all transmembrane proteins on one half of the cytoplasmic membrane of a whole cell. To achieve better imaging, we combine various methods, including critical‐point drying, fixation of gold beads with a carbon layer, and a newly developed chemical thinning method. In addition, in our image‐processing algorithm, we implemented pair correlation and pair cross‐correlation functions, providing more details and better quantitative accuracy in characterizing the size and numbers of possible protein clusters. © 2024 The Authors. Current Protocols published by Wiley Periodicals LLC.Basic Protocol 1: Sample preparation and transmission electron micrographyAlternate Protocol: Direct cell labeling for transmission electron micrographyBasic Protocol 2: Analysis of TEM images to detect immunogold‐labeled proteins

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“…NMDA receptors are ubiquitously distributed in the mammalian CNS but show regional subunit composition [ 12 ]. In particular, NMDA-R2B receptor expression in the adult rat brain is limited to the forebrain [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

Memantine effects on ingestion microstructure and the effect of administration time: A within-subject study

Galistu

D’Aquila

2020

PLoS ONE

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In a between-subject comparison of two memantine administration schedules we observed that treatment with the NMDA receptor antagonist memantine before testing sessions reduced ingestion of a 10% sucrose solution in rats, due to reduced licking burst size, thus suggesting a blunted hedonic response. Conversely, daily post-session administration reduced burst number, indicating a reduced level of behavioural activation, likely due to the development of conditioned taste aversion (CTA). In this study, the effect of pre-session and post-session memantine administration was investigated within-subjects. Memantine was administered in daily intraperitoneal injections for 13 days, on alternate days, either 1-h before–“before testing” sessions—or immediately after a 30-min session–“after testing” sessions. The effects on the microstructure of licking for a 10% sucrose solution were examined in the course of treatment and for 21 days after treatment discontinuation. The results show reduced burst size in the “before testing” sessions, without effects on the intra-burst lick rate, an index of motoric effects. Moreover, burst number was reduced since the third session of both administration conditions until the end of treatment. Interestingly, the effect of memantine of reducing the activation of ingestive behaviour was less pronounced in this study with respect to that observed with the previous study post-session administration schedule, in spite of the longer treatment. This apparent paradox might be explained if one considers these effects as instances of a memory-related effect, such as the development of CTA. In the framework of this hypothesis, the “before testing” sessions, not being followed by memantine administration, can be considered as extinction sessions performed every other day. Moreover, the animals treated with memantine at the highest dose failed to recover to pre-treatment ingestion levels 21 days after treatment discontinuation, while the animals treated after testing sessions in the previously published study showed a complete recovery well before the 15 th day test. Within the same interpretative framework, this might depend by the reduced number and frequency of the extinction trials—i.e. the number of the sessions run after treatment discontinuation—in the present study. These results provide further support to the conclusion that memantine administration before sessions reduce burst size, an effect which is likely due to blockade of NMDA receptors occurring during behavioural testing. The observation that this effect can be obtained even in absence of a reduced intra-burst lick rate, which rules out the involvement of motor impairment, provides an important piece of evidence in support to the interpretation of this effect as a blunted hedonic response. Moreover, these results provide further evidence that burst number reduction is due to a memory-related effect induced by memantine administration after sessions.

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Receptor distribution studies

Cited by 8 publications

References 67 publications

The Impact of Chemical Biology on Drug Discovery

The Impact of Chemical Biology on Drug Discovery

Novel Transmission Electron Microscopic Method to Quantify Protein Clustering on the Cell Surface

Memantine effects on ingestion microstructure and the effect of administration time: A within-subject study

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