Human
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine Derivatives as Highly Potent and Selective Human A(2B) Adenosine Receptor Antagonists
Tue, 2014-07-01 09:49 — Abdel Naser ZaidA new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A(2B) adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A(2B), A(1), A(2A), and A(3) adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A(2B) adenosine receptor K(i)=7nM and good selectivity (A(1), A(2A), A(3)/A(2B)>140). Synthesis and SAR of this novel class of compounds is presented herein.
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Neuronal Types in the Human Anterior Ventral Thalamic Nucleus: A Golgi Study
Mon, 2014-01-20 13:10 — Malik Mohamad SabubahNeurons in the anterior ventral (AV) thalamic nucleus of human adults were impregnated by Golgi-Kopsch impregnation method. Results showed that at least three morphological types of neurons could be recognized in the human AV thalamic nucleus. Type I neurons were medium to large with rich dendritic arborization. Both tufted and radiating dendritic branching patterns were seen in almost every neuron of this type. Only the initial axonal segments of these cells were impregnated suggesting that these axons were heavily myelinated. Type II neurons were medium in size with poor to moderate dendritic arborization. Many of these cells possess a few dendritic grape-like appendages. Long segments (up to 300 μm) of their axons were impregnated suggesting that these axons were either unmyelinated or thinly myelinated. These axons change their direction and form loops very often. No local branches were seen for these axons suggesting that they could be projection axons. Type III neurons were small with only one or two dendrites with poor arborization. No axons for these cells were seen in this study. The three neuronal types in the human AV thalamic nucleus were compared with neuronal types already described in other thalamic nuclei of human and non-human species. The results of this study might provide a morphological basis for further electrophysiological and / or pathological studies.
Transcriptomic and Quantitative Proteomic Analysis of Transporters and Drug Metabolizing Enzymes in Freshly Isolated Human Brain Microvessels
Wed, 2013-10-16 13:26 — Ramzi H. F. Shawahna
Extent of Potential Drug Interactions Among Patients Receiving Anti-Hypertensive Medications
Wed, 2010-04-21 09:54 — Ansam Feras Sawalha
To investigate the frequency of potential antihypertensive drug interactions among patients with cardiovascular diseases receiving antihypertensive medications.
Methods: The study took place in Nablus, Palestine starting April through October 2003. Patients with cardiovascular diseases (n=876) or who were receiving one or more antihypertensive medications were evaluated. All drugs prescribed for the patients were obtained from their medical files. A drug interaction database was developed based on updated Drug Interaction Facts to examine potential and level of drug interactions in each patient's regimen. Data were entered and analyzed using SPSS software.
Results: The number of "unique" pairs of potential drug interactions among the antihypertensive agents present in the data was 433. These included 16 cases (3.7%) level one; 34 cases (7.8%) level 2; 116 cases (26.8%) level 3; 136 cases (31.4%) level 4, and 131 (30.3%) level 5 interactions. Both increasing age and number of drugs were significantly associated with the potential for significant interactions at all levels with a p value less than 0.025.
Conclusions: This study found a high frequency of potential drug interactions with agents typically used for hypertension. Similar investigations need to be carried out among patients with other types of chronic diseases. Drug interaction software might be necessary in governmental pharmacy departments.
