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Medical Purposes (medical + purpose)
Selected AbstractsThe endocannabinoid system and rimonabant: a new drug with a novel mechanism of action involving cannabinoid CB1 receptor antagonism , or inverse agonism , as potential obesity treatment and other therapeutic useJOURNAL OF CLINICAL PHARMACY & THERAPEUTICS, Issue 3 2007S. Xie Pharm D student Summary There is considerable evidence that the endocannabinoid (endogenous cannabinoid) system plays a significant role in appetitive drive and associated behaviours. It is therefore reasonable to hypothesize that the attenuation of the activity of this system would have therapeutic benefit in treating disorders that might have a component of excess appetitive drive or over-activity of the endocannabinoid system, such as obesity, ethanol and other drug abuse, and a variety of central nervous system and other disorders. Towards this end, antagonists of cannabinoid receptors have been designed through rational drug discovery efforts. Devoid of the abuse concerns that confound and impede the use of cannabinoid receptor agonists for legitimate medical purposes, investigation of the use of cannabinoid receptor antagonists as possible pharmacotherapeutic agents is currently being actively investigated. The compound furthest along this pathway is rimonabant, a selective CB1 (cannabinoid receptor subtype 1) antagonist, or inverse agonist, approved in the European Union and under regulatory review in the United States for the treatment of obesity. This article summarizes the basic science of the endocannabinoid system and the therapeutic potential of cannabinoid receptor antagonists, with emphasis on the treatment of obesity. [source] An investigation of the 125I-radioiodination of colchicine for medical purposesJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 1 2009K. M. El-Azony Abstract A procedure for radioiodination of colchicine with iodine-125 is carried out via an electrophilic substitution reaction. The reaction parameters studied were colchicine concentration, pH of the reaction mixture, reaction time, temperature, different oxidizing agents and different organic media to optimize the conditions for the labeling of colchicine and to obtain a high radiochemical yield of the 125I-colchicine (125I-Col). Using 3.7,MBq of Na125I, 1.25,mM of colchicine as substrate, 1.1,mM of chloramine-T (CAT) as oxidizing agent in ethanol at 60°C for 5,min, a maximum radiochemical yield of 125I-Col (60%) was obtained. The specific activity of 125I-Col obtained was 44.4,MBq/0.5,mmol, and the labeled compound was not completely separated and purified from Col by means of high-pressure liquid chromatography (HPLC), so the uncertainty in the purity may affect the distribution and clearance routes due to the expected competition between 125I-Col and Col. The biological distribution in normal mice indicates the suitability of radioiodinated colchicine for imaging of muscles. Copyright © 2008 John Wiley & Sons, Ltd. [source] Cutaneous effects of infrared radiation: from clinical observations to molecular response mechanismsPHOTODERMATOLOGY, PHOTOIMMUNOLOGY & PHOTOMEDICINE, Issue 5 2003Stefan M. Schieke Human skin is exposed to infrared (IR) radiation (760 nm,1 mm) from natural as well as artificial sources that are increasingly used for cosmetic or medical purposes. Epidemiological data and clinical observations, however, indicate that IR radiation cannot be considered as totally innocuous to human skin. In particular, IR radiation, similar to ultraviolet radiation, seems to be involved in photoaging and potentially also in photocarcinogenesis. The molecular consequences resulting from IR exposure are virtually unknown. Recent studies, however, have begun to shed light on the basic molecular processes such as cellular signal transduction and gene expression triggered by exposure to IR radiation. In response to IR irradiation, mitogen-activated protein kinase signaling pathways were activated mediating the upregulation of matrix metalloproteinase-1 expression. This previously unrecognized molecular ,IR response' shows that IR radiation is capable of specifically interfering with cellular functions and provides a molecular basis for biological effects of IR on human skin. [source] Overexpression, crystallization and preliminary X-ray crystallographic analysis of d -ribose-5-phosphate isomerase from Clostridium thermocellumACTA CRYSTALLOGRAPHICA SECTION F (ELECTRONIC), Issue 11 2009Junho Jung Rare sugars are used for many industrial and medical purposes and are produced by the interconversion between aldoses and ketoses catalyzed by sugar and sugar-phosphate isomerases. Recently, Clostridium thermocellumd -ribose-5-phosphate isomerase (CTRPI), an aldose,ketose isomerase, was cloned in order to synthesize d -allose and its substrate specificity was further characterized for industrial usage. CTRPI has a novel substrate specificity that differs from those of other isomerases, which have broad substrate specificities. CTRPI prefers aldose substrates such as l -talose, d -ribose and d -allose. CTRPI was purified and crystallized in order to determine its three-dimensional structure and thus to elucidate its enzymatic reaction mechanism and understand its substrate specificity. The crystal belonged to the trigonal space group P3221, with unit-cell parameters a = b = 69.5, c = 154.4,Å, and diffracted to 1.9,Å resolution. According to Matthews coefficient calculations, the crystallographic structure consists of a dimer in the asymmetric unit, with a VM of 3.2,Å3,Da,1 and a solvent content of 61.7%. [source] | |||||||||||||