Results 91 to 100 of about 19,808 (220)

Modulation of Tau Protein Neurotoxic Hallmarks by Novel σ1R Agonists/HDAC Inhibitor Dual‐Acting Compounds

open access: yesChemMedChem, Volume 21, Issue 5, 13 March 2026.
This study explores the development of dual‐acting compounds combining σ1R agonists and histone deacetylase inhibitors (HDACi). Key findings include compound 2d and 3a's high affinity for σ1R and favorable pharmacokinetic profile and an in vivo determined σ1R agonist profile by reversing the effect of the σ1R antagonist BD‐1063.
Antonino N. Fallica   +16 more
wiley   +1 more source

Synthesis of [11C]MK-1064 as a new PET radioligand for imaging of orexin-2 receptor [PDF]

open access: yes, 2016
The reference standard MK-1064 {5″-chloro-N-((5,6-dimethoxypyridin-2-yl)methyl)-[2,2′:5′,3″-terpyridine]-3′-carboxamide} was synthesized from methyl 2-chloro-5-iodonicotinate and 5-(chloropyridin-3-yl)boronic acid in 4 steps with 33% overall chemical ...
Gao, Mingzhang   +2 more
core   +1 more source

Cancer‐on‐Chip and Integrative Tumor Microenvironment Sensor Technologies for Progressing Precision Radiotherapy

open access: yesAdvanced Sensor Research
Precision radiotherapy, such as targeted radioligand therapy, accentuates the precise delivery of radiation to tumor cells while limiting radiation damage to surrounding normal cells.
Shuvashis Dey   +6 more
doaj   +1 more source

PET quantification of [18F]MPPF in the canine brain using blood input and reference tissue modelling [PDF]

open access: yes, 2019
Numerous studies have shown that the serotonin(1A) (5-HT1A) receptor is implicated in the pathophysiology and treatment of several psychiatric and neurological disorders.
Bosmans, Tim   +10 more
core   +1 more source

Radioligand therapy (RLT) used to treat cardiac metastasis of pancreatic neuroendocrine tumor

open access: yesClinical Case Reports
Key Clinical Message Radioligand Therapy (RLT) in the form of [177Lu] Lu‐DOTA‐TATE (Lutathera®) is a promising treatment for pancreatic neuroendocrine tumors (pNETs) with cardiac metastasis.
Kieran J. Ved   +5 more
doaj   +1 more source

Selective in vitro targeting of GRP and NMB receptors in human tumours with the new bombesin tracer 177Lu-AMBA [PDF]

open access: yes, 2018
Purpose: To investigate the in vitro binding properties of a novel radiolabelled bombesin analogue, 177Lu-AMBA, in human neoplastic and non-neoplastic tissues selected for their expression of the bombesin receptor subtypes GRP-R, NMB-R and BRS-3. Methods:
Eltschinger, Véronique   +4 more
core  

The pathophysiological consequences of somatostatin receptor internalization and resistance [PDF]

open access: yes, 2003
Somatostatin receptors expressed on tumor cells form the rationale for somatostatin analog treatment of patients with somatostatin receptor-positive neuroendocrine tumors.
Hofland, L.J. (Leo)   +1 more
core   +3 more sources

Automated Scale-Down Development and Optimization of [68Ga]Ga-DOTA-EMP-100 for Non-Invasive PET Imaging and Targeted Radioligand Therapy of c-MET Overactivation in Cancer

open access: yesBiologics
Background/Objectives: Overactivation of the HGF/c-MET pathway is implicated in various cancers, making its inhibition a promising therapeutic strategy.
Silvia Migliari   +7 more
doaj   +1 more source

Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals? [PDF]

open access: yes, 2018
Purpose: Gallium-68 is a metallic positron emitter with a half-life of 68min that is ideal for the in vivo use of small molecules, such as [68Ga-DOTA,Tyr3]octreotide, in the diagnostic imaging of somatostatin receptor-positive tumours.
Antunes, P.   +6 more
core  

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