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Orain D Ofner S Koller M Carcache DA Froestl W Allgeier H Rasetti V Nozulak J Mattes H Soldermann N Floersheim P Desrayaud S Kallen J Lingenhoehl K Urwyler S 《Bioorganic & medicinal chemistry letters》2012,22(2):996-999
A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage. 相似文献
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Enzyme‐linked immunosorbent assay by enhanced chemiluminescence detection for the standardization of estrogenic miroestrol in Pueraria candollei Graham ex Benth
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Gorawit Yusakul Orapin Udomsin Hiroyuki Tanaka Satoshi Morimoto Thaweesak Juengwatanatrakul Waraporn Putalun 《Luminescence》2015,30(5):568-575
Miroestrol (ME) is a potent phytoestrogen from the P. candollei tuberous root. It has been approved for use in clinical trials due to its beneficial effect on disorders associated with estrogen deficiency. To ensure medical efficacy and safety, high performance analytical methods for ME analysis are required to standardize products from the P. candollei root. An enhanced chemiluminescence enzyme‐linked immunosorbent assay (ECL‐ELISA) was developed and validated using a polyclonal antibody against ME and a chemiluminescent system of luminol–H2O2–horseradish peroxidase‐4‐(1‐imidazolyl) phenol. The ECL‐ELISA system exhibited linearity over a concentration range of 0.31–10.00 ng mL?1, for which the relative standard variation (%RSD) was less than 10% for both intra‐ and interplate determinations. The ECL‐ELISA is reliable for the determination of ME as reflected by the high recovery percentage (101.22–103.06%). As a comparative analysis, the ME content in each sample determined by ECL‐ELISA was correlated with high coefficients of determination with colorimetric ELISA (R2 = 0.998) and high performance liquid chromatography (HPLC) (R2 = 0.998) methods. The ECL‐ELISA method could be applied to all of the commercial products containing P. candollei root, when the products contain between 0.706 ± 0.046 and 13.123 ± 0.794 µg g?1 dry wt. of ME. This method is useful as a high performance analytical method for the quantity control of ME in raw materials and end products at both the research and industrial levels. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
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Koller M Lingenhoehl K Schmutz M Vranesic IT Kallen J Auberson YP Carcache DA Mattes H Ofner S Orain D Urwyler S 《Bioorganic & medicinal chemistry letters》2011,21(11):3358-3361
Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models. 相似文献
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Carsten Spanka Ralf Glatthar Sandrine Desrayaud Markus Fendt David Orain Thomas Troxler Ivo Vranesic 《Bioorganic & medicinal chemistry letters》2010,20(1):184-188
High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivity over other glutamate receptors. Compound 16m exhibits a favorable PK profile in rats, robust anxiolytic-like effects in three different animal models of fear and anxiety, as well as a good PK/PD correlation. 相似文献
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Waraporn Putalun Orapin Udomsin Gorawit Yusakul Thaweesak Juengwatanatrakul Seiichi Sakamoto Hiroyuki Tanaka 《Biotechnology letters》2010,32(5):721-724
Methyl jasmonate, 50 μM, 0.5 mg yeast extract/l and 100 mg chitosan/l stimulated plumbagin production in Drosera burmanii whole plant cultures after 6 days of elicitation. Yeast extract (0.5 mg/l) was the most efficient enhancing plumbagin production
in roots of D. burmanii to 8.8 ± 0.5 mg/g dry wt that was 3.5-fold higher than control plants. 相似文献
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Udomsin Orapin Yusakul Gorawit Kraithong Witsarut Udomsuk Latiporn Kitisripanya Tharita Juengwatanatrakul Thaweesak Putalun Waraporn 《Plant Cell, Tissue and Organ Culture》2019,136(1):141-151
Plant Cell, Tissue and Organ Culture (PCTOC) - Pueraria candollei var. mirifica (PM), a rejuvenating herb of Thailand, has been applied efficaciously to relieve symptoms of estrogen deficiency in... 相似文献
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Manuel Koller David A. Carcache David Orain Peter Ertl Dirk Behnke Sandrine Desrayaud Grit Laue Ivo Vranesic 《Bioorganic & medicinal chemistry letters》2012,22(20):6454-6459
1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic scaffold allowed to improve the physico-chemical parameters for optimization of the aqueous solubility while retaining high in vitro potency. 相似文献
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An Enzyme‐linked Immunosorbent Assay for Genistein 7‐O‐[α‐rhamnopyranosyl‐(1→6)]‐β‐glucopyranoside Determination in Derris scandens using a Polyclonal Antibody
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