Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 14 of 14 for “"brain uptake"”.
-
Development of amyloid beta binding bifunctional chelators for diagnosis of Alzheimer’s disease
… the characteristic pathological feature found by brain autopsy in patients with AD, is the main cause of AD. Amyloid plaques are insoluble aggregates consist of amyloid β (Aβ), a soluble peptide which main alloforms are 40 and 42 amino acid residues long. After being cleaved from amyloid precursor …
-
I.~fluorine-18 Labeled Corticosteroids and Progestins for Receptor-Based Imaging of the Brain and of Breast Tumors. II.~Synthesis and NMR Spectrum of (carbon-13(18))-Meso-Hexestrol
… in adrenalectomized, mature male rats showed no brain uptake for three compounds, while the fourth was taken up by the brain but did not selectively localize in target tissues (hippocampus, cortex). Two compounds showed partially competable uptake in the pituitary, suggesting that failure to …
-
Exendin 4 Conjugation and Sequence Modification to Treat Type 2 Diabetes and Obesity
… (GLP-1R) in vitro and on PD/PK (including brain uptake and function) in vivo?</p> <p>Goal: To remove side-effects (nausea, weight loss) of Ex-4 without loss of glucoregulation.</p> <p>Q2. (Chapter 3) Can B12 dietary uptake proteins such as gastric intrinsic factor offer protection to …
-
Study of a Transferrin Receptor Brain Shuttle for the Delivery of Nanobodies Against GABAA Receptors
The blood-brain barrier (BBB) represents a major obstacle in drug development, restricting the access of drugs into the central nervous system (CNS) following systemic administration. This challenge is particularly evident for biological drug classes, such as antibody-based therapies, contributing …
-
Design and Synthesis of a Novel Neuroprotective Brain-Targeting Amylin Receptor Antagonist
… log P (-1.2 for AC253) and are not optimized for brain uptake. From the structure-activity relationship studies, we have designed a 16-mer analog (R16) from the N-terminal region of AC253 as a novel AmyR antagonist for better activity and blood-brain permeability. The goal of this study is to …
-
Design and evaluation of novel PET and SPECT tracers for imaging the monoamine system and the P-gp transporter
… and physiological functions in the living brain. In vivo brain mapping with PET or SPECT can be of great importance in drug development as well as in the effective diagnosis, treatment and management of neurological and psychiatric disorders and substance abuse. Therefore, the development …
-
Targeting Tau Aggregation for the Diagnosis and Treatment of Alzheimer’s Disease
The aggregation of tau protein in the brain is a defining pathological characteristic of several diseases, known as tauopathies, the most common of which is Alzheimer’s disease. Because the temporal and spatial progression of tau lesions correlates with neurodegeneration and cognitive decline, they …
-
Targeting Organic Anion Transporting Polypeptide 1A4 (Oatp1a4) for Effective Drug Delivery at the Blood-Brain Barrier
… system (CNS) is greatly limited by the blood-brain barrier (BBB). Physical and biochemical properties of the BBB have rendered treatment of CNS diseases extremely difficult. Targeting endogenous BBB transporters from the ATP-binding cassette (ABC) superfamily (i.e., P-glycoprotein (P-gp)) or …
-
Homing of 111In-Labeled Bone Marrow Mesenchymal Stem Cells in Acute Brain Trauma Model
… mesenchymal stem cells (BMSCs) in an acute brain trauma model by 111In-tropolone labeling and to perform the effect of 111In-labeling on the viability and functions of BMSCs. Rat BMSCs were labeled with 37 MBq 111In-tropolone. Their labeling efficiency and in vitro retention rate were …
-
Synthetic and Natural Environmental Compounds as Potential Facilitators of Mptp-Induced Parkinsonism
… as motor and cognitive behavior. Differences in brain uptake mechanisms and metabolism of Mn and MPTP, could explain why combined administration of Mn and MPTP differentially affect dopaminergic activity in the nigrostriatal and mesocortical pathways.
-
Improving CNS Delivery of Genistein for the Treatment of Sanfilippo Syndrome
… for poor penetration of genistein into the brain. We aim to develop strategies to increase genistein concentration in the CNS, decrease the level of heparan sulfate in the CNS and thus effectively treat MPS III. Towards our goals, two major specific aims were proposed: (1) To improve …
-
Development of Novel PET Radiotracers for Neuroinflammation and COVID-19: Targeting FPR2, I2BS and ACE2
… Chronic neuroinflammation leads to disruptive brain functioning and can cause neurodegenerative diseases. Coronavirus disease 2019 (COVID-19) is an infectious disease spread rapidly across the world, threatening global health and causing huge economic losses. This work involves the development …
-
Development of multifunctional compounds for the modulation and detection of amyloid beta species
… plaques and neurofibrillary tangles in the brain is the hallmark of AD. Amyloid β (Aβ) peptides, the main component of amyloid plaques, are formed from the cleavage of amyloid precursor protein (APP) by β- and γ-secretases. The main alloforms of Aβ are Aβ40 and Aβ42, containing 40 and 42 …
-
Synthesis of fluorinated cannabinoid derivatives; Towards PET radiotracers for imaging the cannabinoid receptor
… (CB1R) which is highly expressed in the human brain1,2. Defects in CB1R expression or endocannabinoid transmission have been associated with several neuropsychiatric disorders thus establishing CB1R as a potential drug target or biomarker of disease3. However, tools to study the function of the …