AMI-193 - CAS 510-74-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor
AMI-193 has been found to be a selective 5-HT antagonist and could be also used as a starting reagent in some pharmaceutical synthesis.
≥99% by HPLC
White Solid
Spiramide; R 5808; R-5808; R5808; 8-[3-(4-Fluorophenoxy)propyl]-1-phenyl-1,3,8-triazaspiro[4.5]-decanone
Canonical SMILES:
1.Role of prolactin in growth of the rat mammary tumor MTW9.
Platica M;Doody J;Mandeli JP;Hollander VP Int J Cancer. 1991 Apr 22;48(1):109-12.
The growth of MTW9 mammary tumors exhibits different degrees of responsiveness to ovariectomy, ranging from sensitivity to resistance. This range of response is a function of time elapsing from tumor inoculation until performance of ovariectomy provided that prolactin (PRL) level is kept continuously high. In vivo studies showed that the MTW9 tumors developed by chronic administration of spiramide were sensitive to ovariectomy by 60 days, but they became resistant to ovariectomy by 100 days. However, when spiramide treatment was discontinued after tumor appearance, the tumors were still sensitive to ovariectomy by 100 days. Chromatofocusing (CF) profile of cytosolic estrogen receptors (ER) correlated with the responsiveness to ovariectomy. A 2-peak profile for tumors sensitive to ovariectomy, and only a one-peak profile for tumors resistant to ovariectomy, were seen. Although the prolactin level in rats bearing the tumors was higher than in the normal rats, no correlation between the PRL level and the change in CF profile of ER over time was seen. Also, these changes could not be correlated with the tumor size. In vitro studies showed that incubation of cytosolic ER from a sensitive tumor (2 peaks) with PRL led to a CF profile with only one peak, characteristic of a resistant tumor.
2.New diterpene alkaloids from the roots of Spiraea japonica.
He HP;Shen YM;Zhang JX;Zuo GY;Hao XJ J Nat Prod. 2001 Mar;64(3):379-80.
Chemical investigation on an ethanol extract from the roots of Spiraea japonica var. acuta resulted in the isolation of three new diterpene alkaloids named spiramide (1) and spiratine A (2) and spiratine B (3). Structures of 1-3 were elucidated primarily on the basis of 1D and 2D NMR experiments.
3.Identification of known drugs targeting the endoplasmic reticulum stress response.
Bi K;Nishihara K;Machleidt T;Hermanson S;Wang J;Sakamuru S;Huang R;Xia M Anal Bioanal Chem. 2015 Jul;407(18):5343-51. doi: 10.1007/s00216-015-8694-2. Epub 2015 Apr 30.
The endoplasmic reticulum (ER), a multifunctional organelle, plays a central role in cellular signaling, development, and stress response. Dysregulation of ER homeostasis has been associated with human diseases, such as cancer, inflammation, and diabetes. A broad spectrum of stressful stimuli including hypoxia as well as a variety of pharmacological agents can lead to the ER stress response. In this study, we have developed a stable ER stress reporter cell line that stably expresses a β-lactamase reporter gene under the control of the ER stress response element (ESRE) present in the glucose-regulated protein, 78 kDa (GRP78) gene promoter. This assay has been optimized and miniaturized into a 1536-well plate format. In order to identify clinically used drugs that induce ER stress response, we screened approximately 2800 drugs from the NIH Chemical Genomics Center Pharmaceutical Collection (NPC library) using a quantitative high-throughput screening (qHTS) platform. From this study, we have identified several known ER stress inducers, such as 17-AAG (via HSP90 inhibition), as well as several novel ER stress inducers such as AMI-193 and spiperone. The confirmed drugs were further studied for their effects on the phosphorylation of eukaryotic initiation factor 2α (eIF2α), the X-box-binding protein (XBP1) splicing, and GRP78 gene expression.
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CAS 510-74-7 AMI-193

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