Mini reviews in medicinal chemistry
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POCD describes a decline in cognitive function after surgery with a predominance in the elderly patient. Although there is general agreement that POCD is likely to be multifactorial, whether its occurrence is a result of the effects of surgery or general anesthesia remains unclear. This review provides a synopsis of the available clinical and preclinical data and summarizes recent research relevant to the occurrence of POCD and possible pharmacologic algorithms for its prevention and treatment.
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Review
Treating age-related macular degeneration - interaction of VEGF-antagonists with their target.
The neutralization of VEGF is the current treatment of choice for age-related macular degeneration. Current approaches include anti-VEGF-antibodies and -Fab Fragments, aptamers, soluble receptors (Traps) and siRNA. The molecular properties of VEGF and its antagonists are reviewed and the pathways of action of these substances are discussed.
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Review
Structural and physicochemical profiling of morphine and related compounds of therapeutic interest.
A concise account of the physicochemical properties of morphine and its derivatives of therapeutic interest is provided. Such properties include macroscopic and microscopic acid/base parameters, lipophilicity, solubility, permeability that all influence the fate of drugs in the body. The dependence of these parameters on pH is discussed and subsequent implications in drug administration and formulation are presented.
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Clofarabine is a second generation of purine nucleoside analogues designed to combine the most favorable pharmacokinetic properties of fludarabine and cladribine. Clofarabine acts by inhibiting DNA polymerases and ribonucleotide reductase as well as by inducing apoptosis in cycling and non-cycling cells. Phase I/II clinical studies revealed its efficacy in hematological malignancies, and in 2004 clofarabine was approved by the United States Food and Drug Administration for the treatment of pediatric relapsed or refractory acute lymphoblastic leukemia after at least two prior chemotherapy regimens. The mechanism of action, pharmacology and clinical activity of clofarabine is the subject of this review.
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The diagnosis and assessment of brain damage is currently based on the clinical examination and the modern neuro-imaging techniques. Electrophysiology, haemodynamic monitoring and invasive neuromonitoring constitute additional tools for monitoring of the brain function and clinical course of the patient. However, despite the substantial progress, clinical and neuro-monitoring methods are quite often not sufficient to evaluate and quantify the severity of the initial and secondary destructive processes and hence they cannot guide efficient therapeutic measures and prognosticate effectively the outcome. ⋯ Lactate dehydrogenase, creatine kinase, neuron specific enolase, have been proposed as potential markers of brain injury. More recently, other glial markers such as the Myelin Basic Protein, the glial fibrillary acidic protein and the S-100B protein have been measured in blood and used as surrogate biochemical markers for brain injury. This review summarizes published findings on the above brain specific serum biochemical markers with emphasis on those with clinical utility.