The antifungal compound was identified as phenyllactic acid (PLA), and it was found to have a minimum inhibitory concentration on Phytophthora drechsleri Tucker of 18 mg/mL. Bio-control activity tests indicated that PLA has a wide spectrum of antagonistic effects against Fusarium oxysporum, Botrytis cinerea, Glomerella cingulata, Penicillium citrinum, Penicillium digitatum, particularly against F. oxysporum. PLA is the most notable antimicrobial compound with broad and effective antimicrobial activity against both bacteria and fungi that has been
isolated and identified to date. These results indicate that B. coagulans TQ33 has the potential for application in biological pesticides.”
“Introduction: In vivo brain receptor occupancy has been the key assay in driving preclinical drug discovery SRT1720 solubility dmso program and there is a need to hasten this screening step. Radiolabeled methods, which are time consuming and expensive, are most widely employed to measure receptor occupancy. Thus we sought to develop and validate an alternative novel approach for measuring rat brain alpha(4)beta(2) neuronal nicotinic acetylcholine receptor occupancy using high performance liquid chromatography combined with tandem mass spectrometric detector (LC-MS/MS).
Methods: Tracer optimization studies like in vivo dose and time dependent brain regional distribution;
saturation binding and blocking study with nicotine and atropine were carried out GDC-0994 cost for ZW-104 in rats. Assay validity was tested by pretreatment with potent alpha(4)beta(2) ligands; TC-1734, cytisine, ABT-089, ABT-594 and A-366833. Receptor occupancy along with plasma and brain exposure levels of alpha(4)beta(2) ligand was measured in the same set of animals.
Results: The regional distribution of ZW-104 in rat was found to be, thalamus > frontal cortex > striatum > hippocampus > cerebellum, and is in accordance with the distribution and regional densities of alpha(4)beta(2)
nAChRs measured using [F-18]ZW-104 in mice and baboons. Pretreatment with nicotine ARS-1620 mouse and alpha(4)beta(2) ligands dose dependently reduced the binding of ZW-104 in the thalamus. Non-nicotinic antagonist atropine did not alter the binding of ZW-104 in the thalamus, indicating the tracer specificity. The ED50 values calculated for occupancy were found to be 3.01, 0.83, 14.81, 0.001 and 0.11 mg/kg for TC-1734, cytisine, ABT-089, ABT-594, and A-366833, respectively.
Discussion: These findings demonstrate that non-radiolabeled ZW-104 is suitable for determining the alpha(4)beta(2) receptor occupancy in rat brain. The LC-MS/MS based receptor occupancy assay is a rapid method and allows the generation of occupancy data along with the brain and plasma concentration in the same group of animals. (C) 2012 Elsevier Inc. All rights reserved.