Posted by admin on Nov 30, 2016 in |
Previous studies have demonstrated that the activation of adenosine A2B receptors increases adenosine 3′-cyclic monophosphate (cAMP) accumulation in rat skeletal muscle cells, which is probably an important yet unknown mechanism contributing to the regulation of skeletal muscle functions. via rat L6 skeletal muscle cells, it has been elucidated further potential molecular signaling responsible for adenosine A2B receptor modulations via quantitative real-time PCR assays (probe-based). The results of the present study has shown for the first time that NECA alters the expression of PGC-1α significantly in both one week and 19 hours starved skeletal muscle cells (P<0.05 and P<0.01, respectively) (2.5 and -0.58 fold change compared to vehicle, respectively). Adenosine A2B receptors mediate NECA-modulated PGC-1α mRNA gene expression in skeletal muscle cells. To our knowledge, this is the first study demonstrating an induction of PGC-1α gene by CGS 21680 significantly (P<0.001) (around 1.8 fold change compared to vehicle). In the current study, NECA (10 μM) increases NR4A1 and NR4A3 mRNA gene expression significantly (P<0.05) (around 2.7 and 5.2 -fold change...
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Posted by admin on Nov 30, 2016 in |
Adenosine is a strong modulator of gene expression, which underpins some of its potential expected effects in skeletal muscle in terms of fatty acid metabolism. Accumulating evidence highlights a critical role for the adenosine system in the regulation of fatty acid metabolism and obesity. However, its molecular signaling role in fatty acid transport and oxidation in skeletal muscle is less clear. The aim of the present study was to examine whether acute and chronic treatment of skeletal muscle cells in vitro with stable adenosine analogue NECA, selective adenosine A2B receptors antagonist/inverse agonist PSB 603, and/or selective adenosine A2A receptors agonist CGS 21680 affects mRNA expression of key metabolic genes in skeletal muscle. Rat L6 skeletal muscle cells were treated with NECA, PSB 603 and CGS 21680 for determination the mRNA expression of genes involved in fatty acid transport and oxidation (CPT1B, ACCβ and LCAD) using QRT-PCR (Probe-based). The results of the present study have shown for the first time that NECA alters the expression of a number of genes...
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Posted by admin on Nov 30, 2016 in |
In present investigation of some ethyl1-((5-amino-1, 3, 4-thiadiazol-2-yl) methyl) – 5 – ethyl-2, 6-dimethyl – 4 – phenyl-1, 4-dihydro pyridine-3-carboxylate are designed and docked active site of cavity 1# of open channel voltage gated calcium channel protein (3DVE). The compounds evaluated in silico (docking) to distinguish their hypothetical binding mode using the X-ray crystal structure of Ca2+/CAM-CaV2.2 IQ domain complex 3DVE obtained from protein data bank as target protein Respectively. In this docking studies carried out the comparative docking experiments of designed compounds with known calcium blockers Ethosuximide, gabapentine with dock score calculated -4.9318,-4.6489 respectively. Obtained results were evaluated in terms of dock score into the active site of receptor. One of the conformers of compound Cl 123(C1)and AN 123 (C15),CH=CH 123 (C6),Fur 123 (C9) found to have lowest dock scores-3.2496 and -3.1749 , -2.8439, – 2.6359 respectively and said to have more affinity for active site of Ca2+/CAM-CaV2.2 IQ domain complex receptor than other molecules. More the negative value of the energy of binding the better is affinity...
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Posted by admin on Nov 30, 2016 in |
Synthesis of 6-Methyl-2, 4-dihydro-3H-pyrazol-3-one- 4- (4-substituted) Benzylpiperazine derivatives IVP a-e was carried out by bromination of Ethyl aceto acetate (I) with KBr. The reaction was carried out in the presence of Hydrochloric acid and tolune to produce Bromo-ethyl aceto acetate (II), it is further condensed with substituted Benzylpiperazines in presence of ethanol to obtain condensed compound (III). This upon cyclization with excess of hydrazine hydrate will produce title compounds. All the title compounds IVP a-e were screened for possible antibacterial activity against P. Vulgaris, S. Aureas, E. Coli, B. Subtillus and antifungal activity against Altenaria, Culvalaria, C. Albicans and A. Niger. Among the compounds synthesized IVPb and IVPc demonstrated good antibacterial activity, IVb, IVc, and IVe showed good antifungal activity. The activities of the synthesized compounds are compared with the standard and other test compounds. The structures of synthesized compounds were established by elemental analysis, IR, H NMR and Mass spectral...
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Posted by admin on Nov 30, 2016 in |
Aim: The objective of this survey was to assess the awareness pattern of analgesic administration and the various factors impacting the prescription of analgesics. Materials and methods: Pretested interviewer administered questionnaire was distributed to 100 study subjects consisting of post graduates and dental practitioners in Chennai. The questionnaire was designed to contain questions regarding the most commonly prescribed analgesic in various dental procedures and the various factors taken into account by the dentist while prescribing these analgesic drugs. The data was analysed using SPSS software. Results: In this study, the most commonly prescribed analgesic was paracetamol (78%). 63 % of the dentists preferred non-opioids, 28% preferred opioids and the remaining 9% prescribed both opioids and non-opioids.87% of the dentists have chosen combinations of analgesics. The most commonly prescribed combination was paracetamol with diclofenac(59%). 83% of the dentists preferred topical analgesics. 94% of the dentists took into account, the medical condition of the patient while prescribing analgesics. Special care for pediatric patients was given by 97% of the dentists. Among...
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